GPCR Screening with Confidence

Comprehensive GPCR Assay Solutions for Drug Discovery

Why go anywhere else? Why go anywhere else? We cover the entire range of GPCR assay possibilities.

Shop at the GPCR Super Store. From PerkinElmer — your one stop solution provider. PerkinElmer — a Source of Confidence for Your GPCR Research and Discovery

G-Protein Coupled Receptors (GPCRs) continue to be significant therapeutic Contents targets, and thus GPCR assays and screening campaigns remain major •Assay Platforms for GPCR Binding Assays ...... 2 components of drug discovery research • NEN for GPCR Binding Assays ...... 4 programs worldwide. The need for • Cloned Receptors for GPCR Binding Assays...... 4 reliable, proven, and versatile assay • Adenylyl Cyclase Activation/Inhibition and technologies and reagents is a key cAMP Quantitation ...... 5 component for successful and productive •Detection Instrumentation to Measure research. That’s why PerkinElmer GPCR Assays ...... 11 has assembled the world’s most •Ordering Information: comprehensive product offering for DELFIA Ligands and Reagents...... 16 GPCR research and drug discovery, covering the entire range of GPCR GPCR-Specific NEN Radioligands...... 17 assay possibilities. SignalScreen® Cloned Receptors ...... 18 Membrane Target Systems Cloned Receptors .....23

Our products and expertise span receptor ligand FlashBlue™ Scintillating Beads and binding assays through functional cellular assays. FlashPlate Microplates...... 27 Our range of assay platforms and detection technologies Adenylyl Cyclase Assay Systems for includes essential radioisotopic technologies and state- Cell-Based Functional cAMP Measurement...... 28 of-the-art luminescence and fluorescence alternatives. cAMP Assay Systems for cAMP Quantitation These are supported by a comprehensive range of in Plasma, Urine and Cell Culture Samples ...... 28 reagents including NEN® Radioligands, DELFIA® GTP Binding Assay Systems...... 28 ligands and cloned receptor membranes, assay systems IP Functional Assay System ...... 29 using our AlphaScreen™, LANCE™, DELFIA, FlashPlate® 3 2 Reporter Gene Luminescence Assay Systems ...... 29 and [FP]™ technologies, plus versatile, scalable detec- tion instrumentation. Combined with our demonstrated Microplates for Filtration Assays and dedication to new product introductions— ligands, Cell-Based Assays ...... 29 receptors, functional assays, and technologies— you can be confident we’ll always be there to support this essential research area. You won’t find this commitment to GPCR research anywhere else.

With PerkinElmer behind your GPCR assays, you can screen with confidence, today and in the future. Why go anywhere else?

www.perkinelmer.com 1 Your Choice of Assay Platforms for GPCR Binding Assays

PerkinElmer supports the widest range of assay tech- And, we’re the first to offer a viable and robust alterna- niques for GPCR binding assays. Our scintillation tive to radioisotopic assays, using our DELFIA technology, proximity assay platforms include FlashBlue™ beads a heterogeneous time resolved fluorescence assay and FlashPlate and Image FlashPlate microplates. platform. All of these options can now supplement These are all compatible with our extensive line of traditional filtration assays to increase the performance NEN Radioligands and SignalScreen® and Membrane and productivity of your GPCR assays. Target Systems (MTS) cloned receptor preparations.

PerkinElmer Assay Platforms for Receptor Ligand Binding Assays

Selection Criteria DELFIA FlashBlue FlashPlate Image Filtration Technology Beads Microplates FlashPlate Assays Microplates Homogeneous No Yes Yes Yes No Non-Rad Yes No No No No Format 96- and 384- 96- and 384- 96- and 384- 384-shallow 96-well plates well plates well plates well plates well plates Throughput >40,000 >20,000 >20,000 >50,000 >15,000 (wells in an 8-hour day) Recommended DELFIA Clear Bottom or N/A N/A UniFilter® Microplate Type AcroWell™ White OptiPlate Filter Plates Filter Plates Microplates Stability of Signal >24 hours >24 hours >24 hours >24 hours >24 hours

DELFIA® TRF Technology

Our DELFIA technology is a robust, time-resolved, Systems (MTS) cloned receptors. For easy assay setup, fluorometric assay (TRF) technology based on dissociative use DELFIA L*R Wash Solution and DELFIA L*R fluorescence enhancement using lanthanide chelates. Binding Buffer. After incubation unbound ligand is Invented by and available exclusively from PerkinElmer, removed by filtration, then signal is enhanced using it’s been widely adopted for many HTS applications DELFIA Enhancement Solution. It’s simple and reliable. due to its extremely high sensitivity and wide dynamic range. Receptor binding assays using DELFIA technology have been proven to be a robust non-radioactive alterna- tive to traditional receptor- binding assays.

Europium-labeled ligands are stable reagents for DELFIA receptor-ligand binding assays. The binding assay may be done in an AcroWell FilterPlate using PerkinElmer’s SignalScreen or Membrane Target

2 FlashBlue™ GPCR Scintillating Beads

Our FlashBlue GPCR beads are scintillating beads binding assays, radioligand molecules bound to the specifically designed and proven for high throughput membranes’ receptors activate the scintillating beads homogeneous GPCR-radioligand binding assays. Three and trigger a blue light emission. Assays can be read microns in diameter, they consist of a polystyrene core on PerkinElmer’s TopCount® and MicroBeta® Liquid covered by a hydrophilic coating that minimizes non- Scintillation and Luminescence Counters in 96- and specific binding. Wheat germ agglutinin (WGA) is 384-well formats, as well as our TriCarb LSC for covalently attached to the surface of FlashBlue GPCR tube-based assays. beads for the capture of cellular membranes. In GPCR

FlashPlate® and Image FlashPlate® Microplates

FlashPlate Microplates

125 3 35 33 14 Our popular FlashPlate microplates are designed for of a variety of isotopes (e.g., I, H, S, P and C) high-volume, homogeneous radioligand binding assays, without the addition of liquid scintillation cocktail. based on the principle of scintillation proximity. The FlashPlate microplates can be read on TopCount or interior of each well is permanently coated with a MicroBeta counters. thin layer of plastic scintillant, enabling detection

Image FlashPlate Microplates Our 384-well Image FlashPlate microplate is coated The FlashPlate platform is especially suitable for with a special scintillant that emits in the red region of receptor binding assays using highly purified membrane the spectrum. This characteristic allows detection with preparations and/or receptor preparations known imaging readers, such as the PerkinElmer ViewLux™ to contain moderate to higher concentrations of ultraHTS Microplate Imager, enabling very high testing receptor protein. Use of FlashPlate pre-coated with throughput. Image FlashPlate also eliminates or greatly wheat germ agglutinin allows greater flexibility in reduces interference from colored compounds. These receptor choice and optimal ease-of-use. plates have shallower wells to permit lower volume assays and, therefore, use less reagent, which is ideal for further miniaturization.

ScreenReady Targets™ ScreenReady Targets™ provide optimum performance of recombinant GPCR membranes pre-coated onto with FlashPlate microplates. They’re ready-to-use, fully FlashPlate microplates, the appropriate radioligand, 125 validated GPCR receptor binding assays that employ I and a validated assay protocol. For more information, 3 and H radioligands. This easy-to-use platform consists please contact [email protected].

www.perkinelmer.com 3 NEN Radioligands Keep Pace with Drug Discovery

From the company that pioneered development work with you, scientist to scientist, to prepare a of the essential tools for receptor ligand binding, custom radioligand that meets your specifications. 3 125 PerkinElmer now offers over 400 NEN H and I A confidentiality agreement is available if required. ligands. A continuous pipeline of new product We are committed to your success. introductions ensures we’ll always keep pace with Please refer to the tables on pages 17–18 for a listing of discoveries and trends in receptor research and our available GPCR membranes with their compatible drug discovery. Each of our ultrapure radioligands NEN Radioligands. PerkinElmer also offers a number is fully characterized for pharmacological action of radioligands, some exclusive, specific for GPCRs and validated in a receptor binding assay. that are not found in the aforementioned tables. For If you don’t find exactly what you need, we invite our complete radioligand offering, please visit our you to take advantage of our custom services. We’ll website at www.perkinelmer.com/nenradioligands.

World’s Most Comprehensive Line of Cloned Receptors for GPCR Binding Assays

PerkinElmer offers more than 170 cloned receptor They provide excellent targets for GPCR assays using membrane preparations, with a constant flow of new the technique of your choice, including: receptors as they are identified. Our line includes • Receptor radioligand binding assays with FlashPlate over 150 GPCRs as well as several kinase, microplates, FlashBlue beads, or classical filtration transporter, and ion channel receptors. For your methods. convenience, the latter are included at the end of the GPCR receptor listing. • TRF filtration assays using DELFIA technology.

Our SignalScreen Cloned Receptor Membrane Each batch of receptors is rigorously characterized and Preparations and Membrane Target Systems (MTS) tested by saturation radioligand binding and pharma- are produced from cells that express recombinant or cological analyses to ensure excellent performance. endogenous receptors and are provided to you as Recommended protocols and lot specific information quality-assured frozen membrane products. such as receptor density (Bmax) and affinity (Kd) are included in all shipments.

The AcroWell Filter Plate is characterized by exceptionally low fluorescence background and is ideal for use in DELFIA GPCR binding assays.

4 Adenylyl Cyclase Activation/Inhibition and cAMP Quantitation

Assays Recommended for Cell-Based Functional cAMP Determination

PerkinElmer offers three systems to directly measure proximity platform; FlashPlate, a homogeneous scintilla- levels of cAMP produced by modulation of adenylyl tion proximity platform; or [FP]2,a simple fluorescence cyclase activity by GPCRs. Choose homogeneous assays polarization technology. All three of these systems may α α based on AlphaScreen, a luminescence homogeneous be used to study G s-GPCRs and G i-GPCRs.

Selection Criteria for Functional cAMP Determination

AlphaScreen FlashPlate [FP]2 Technology Technology Technology Homogeneous Yes Yes Yes Non-Rad Yes No Yes Density Format 96-, 384- and 96- and 384- 96-, 384- and 1536-well plates well plates 1536-well plates Throughput >70,000 points/day >20,000 points/day >100,000 points/day Sample Type Whole cell or membrane Whole cell or membrane Whole cell or preparations preparations membrane preparations Recommended Plate Type White opaque FlashPlate microplates Black opaque OptiPlate Microplates provided precoated with OptiPlate anti-cAMP antibody Microplates

Typical Standard Curve* IC50 = 6.0 nM IC50 = 13.9 nM IC50 = 27.3 nM Z´ = 0.77 Z´ = 0.98 Z´ = 0.87 Stability of Signal >24 hours >24 hours >22 hours

* Comparison of cAMP Assay Technologies for High Throughput Screening. Patricia Kasila and Harry Harney. PerkinElmer Life and Analytical Sciences.

Scientific Poster 4083

www.perkinelmer.com 5 AlphaScreen™ cAMP Assay Kit Our exclusive AlphaScreen (Amplified Luminescent Proximity Homogeneous Assay) is a highly sensitive luminescence homogeneous assay technology that allows the screening of a large range of biological interactions and activities. It forms the basis for a high throughput, sensitive functional cAMP assay with wide dynamic range. (AlphaScreen technology is read on PerkinElmer’s EnVision™ Multilabel Reader.)

The reliable AlphaScreen cAMP assay has been designed to directly measure levels of cAMP produced cAMP detection with AlphaScreen upon modulation of adenylyl cyclase activity by GPCRs. Detection of cAMP is based on the competition between cAMP produced by cells and a biotinylated Increased intracellular concentrations of cAMP following cAMP probe recognized by streptavidin-Donor beads Gs-coupled GPCR activation by an agonist results in and anti-cAMP conjugated Acceptor beads. The beads the displacement of the biotinylated cAMP probe and are brought into proximity and a signal is produced. leads to a proportional signal decrease.

125 FlashPlate Adenylyl Cyclase Activation [ I]- Assay Systems Our solid phase scintillation proximity FlashPlate well, and a simple protocol that measures a true microplate technology has become the “gold standard” second messenger response without extraction. This for cAMP functional assays in HTS labs. It enables homogeneous, easy-to-automate assay provides fast direct measurement of receptor-mediated adenylyl and reliable qualification of lead compounds-perfect cyclase activation/inhibition using live cells all in one for HTS applications.

[FP]2 cAMPfire® Assay ™ Our [FP]2 cAMPfire® kits are a fast, easy way to auto- The [FP]2 cAMPfire assay uses “red-shifted” Alexa mate your HTS assays, allowing you to screen over Fluor™ 594-cAMP tracer* with an emission peak at 100,000 cAMP assay points in one day. Based on 618 nm, providing improved sensitivity over traditional fluorescent polarization technology, the entire assay, FITC-labeled tracers.

including the production of cellular cAMP and the * The cAMP conjugate in this product is sold under license from detection of cAMP by the fluorescence polarization Molecular Probes, Inc., for research use only and is covered by immunoassay is performed in the same microplate, pending and issued patents. with no wash or separation steps.

PerkinElmer’s [FP]2 procedure lets you quickly run homogeneous GPCR assays.

6 Assays Recommended for cAMP Determination in Plasma, Urine or Tissue Culture Media Samples

Selection Criteria for cAMP Determination DELFIA Technology FlashPlate Technology Radioimmunoassay Homogeneous No Yes No Non-Rad Yes No No Density Format 96- and 384-well plates 96- and 384-well plates N/A Throughput >40,000 points/day >20,000 points/day >500/day Sample Type Plasma, urine or Plasma, urine or Plasma, urine, cell culture samples tissue samples cell culture or tissue samples Complementary Microplates provided precoated FlashPlate microplates N/A, run in glass Plate Type with anti-rabbit IgG provided precoated with test tubes anti-cAMP antibody Stability of Signal >24 hours >24 hours >24 hours

DELFIA cAMP Assay Kits Our DELFIA cAMP kit, based on time resolved fluores- when using the simple assay protocol. When using cence, provides a sensitive, nonisotopic immunoassay the high sensitivity protocol the sensitivity is at least for the quantitative determination of cAMP in cell 0.1 pg/well (0.28 fmol/well). culture samples, plasma and urine. The assay can be run with three different protocols — basic, simple, and high sensitivity. The basic and high sensitivity protocols involve adherent cells. In the simple protocol, with cells in suspension, all the steps from sample preparation to measurement of fluorescence are preformed on a DELFIA plate. The sensitivity of the 384-well kit is at least 0.1 ng/well (0.28 pmol/well) DELFIA cAMP assay principle

125 FlashPlate [ I]- cAMP Assay Systems Our FlashPlate cAMP Assay Kits measure cAMP in allows for a more sensitive assay of cAMP. The assay biological fluids, including plasma, urine, and tissue is accurate over a wide range of values and has a high samples. The assay is performed using acetylated or degree of specificity. non-acetylated standards and samples. Acetylation

125 Cyclic AMP [ I]- RIA Kit For customers with lower sample throughput require- assay is based upon competitive ligand binding ments, our traditional radioimmunoassay kit measures between iodinated cAMP tracer and cAMP contained cAMP in plasma, urine and tissue or cell culture in the biological test sample. The assay can be run samples. The assay uses a simplified double antibody with or without acetylation, depending on the level of technique in which the first and second antibody are sensitivity required, with the acetylated version having supplied pre-reacted, eliminating an assay step. The a sensitivity as low as 0.025 pmol/mL.

www.perkinelmer.com 7 GTP Binding Assays

Selection Criteria for GTP Binding Assays

Filter Plates DELFIA FlashBlue Image FlashPlate FlashPlate Technology Beads Microplates Microplates Homogeneous No No Yes Yes Yes Detection Technology Radioisotopic Time Resolved Radioisotopic Radioisotopic Radioisotopic (Liquid Scintillation Fluorescence (Scintillation (Scintillation (Scintillation Counting) Proximity) Proximity) Proximity) Density Format 96-well plates 96- and 96- and 384-shallow 96- and 384-well plates 384-well plates well plates 384-well plates Throughput >15,000 >20,000 >20,000 >50,000 >20,000 points/day points/day points/day points/day points/day Complementary 96-well 96-well OptiPlate WGA Image WGA Plate Type UniFilter Plate AcroWell or (TopCount); FlashPlate FlashPlate AcroPrep™ Isoplate Microplate Microplate Filter Plates (MicroBeta) Stability of Signal >24 hours >24 hours >24 hours >24 hours >24 hours

DELFIA GTP Binding Kit Our DELFIA GTP Binding Kit lets you optimize the subunits following GPCR activation by agonists. conditions for screening novel agonists against a All GPCR membrane preparations need different GPCR of interest. The kit is a time-resolved fluorometric conditions for GTP binding. The kit provides the assay based on GDP-GTP exchange on G-protein instructions and tools for optimizing these conditions.

Homogeneous GTP Binding Assay Using Image FlashPlate and FlashPlate Technology Our WGA (wheat germ agglutinin)-coated Image tions without the need for filtration and wash steps FlashPlate and FlashPlate microplates form the basis required in the most commonly used methodologies. for homogeneous assay measurement of the binding Also available are our ScreenReady Targets, (GPCR of GTP to GPCRs. This assay allows for quantitative membrane pre-coated FlashPlates). For more infor- 35 determination of agonist induced activation of [ S]- mation, please inquire with Custom Services at GTPγS binding to isolated GPCR membrane prepara- [email protected].

8 Homogeneous GTP Binding Assay Using FlashBlue Scintillating Beads Our FlashBlue GPCR scintillating beads offer a rapid, membranes. In the GTPγS binding assay, radionu- high performance, high throughput homogeneous cleotide molecules bound to isolated membrane prepa- GTPγS-radionucleotide binding assay alternative. rations activate the scintillating beads and trigger a blue Three microns in diameter, these beads consist of a light emission. Assays can be read on PerkinElmer’s polystyrene core covered by a hydrophilic coating TopCount and MicroBeta Liquid Scintillation and that minimizes non-specific binding. Wheat germ Luminescence Counters in 96- and 384-well formats, agglutinin (WGA) is covalently attached to the surface as well as our TriCarb® LSC for tube-based assays. of FlashBlue GPCR beads for the capture of cellular

35 [ S]-GTPγS Radionucleotide Filter Binding Assay Commonly performed GTP binding assays are done by receptor membranes, successful GTP binding assays 35 using filtration to remove unbound [ S]-GTPγS prior to can be performed in lower throughput with a high 35 scintillation counting. Using our [ S]-GTPγS and our degree of sensitivity.

IP3 Functional Assay

AlphaScreen

An innovative application of AlphaScreen, our exclusive and GST-IP3 bp are recognized by the streptavidin- homogeneous luminescence proximity assay platform, Donor and anti-GST conjugated Acceptor beads, allows measurement of IP3 in a cellular functional respectively. The beads are brought into proximity and assay. It is particularly relevant for analysis of Gq- a signal is detected. Increased intracellular concentra- coupled GPCRs. Detection of IP3 with AlphaScreen tions of IP3 following GPCR activation by an agonist is based on the competition between IP3 produced by results in the displacement of the b-IP3 and leads to cells and a biotinylated IP3 analog (b-IP3) binding to a a proportional signal decrease.

GST-tagged IP3 binding protein (GST-IP3-bp). The b-IP3

IP3 detection with AlphaScreen

www.perkinelmer.com 9 Reporter Gene Assays

PerkinElmer offers three “mix-and-measure” lumines- batches, saving valuable time. The homogeneous cence reporter gene assay systems for use in functional assay format simplifies the testing process with single GPCR screening applications. Based on the use of microplate preparation. Choose the system that best firefly luciferase, these assays provide long-lived meets your sensitivity and throughput needs. luminescent signals that enable you to process in

Selection Criteria for Reporter Gene Assays

luclite britelite steadylite HTS Half-life (hours) 4 to 5 0.5 4 to 5 Sensitivity Moderate Ultra-High High Phenol Red Sensitivity High Moderate Moderate Automatable Yes Yes Yes Plate Format (wells) 96 96 96 384 384 384 1536 1536 Wicking Low Low Low

luclite® Luminescence Reporter Gene Assay System luclite® is a simple, efficient reporter gene assay kit that enabling you to run more samples in a single experiment. uses a proprietary mixture of several substances with The complete assay—from seeding of cells to measure- luciferase to produce a linear signal lasting at least 5 ment—is done in a single microplate, without any hours. This long Constant-Quanta™ glow signal allows additional cell lysis or separation steps. you to run several microplates at the same time, britelite™ Ultra-High Sensitivity Luminescence Reporter Gene Assay System britelite™ — PerkinElmer’s homogeneous ultra-high Light output and signal decay of britelite compared sensitivity reporter gene assay kit — provides an to luclite extremely strong signal for remarkably accurate and thorough firefly luciferase readings. By producing signals approximately 10 to 15 times brighter than luclite, britelite detects and clearly highlights a wide range of luciferase content levels, making it ideal for continuous-process, robotic systems. britelite’s robust chemistry achieves high assay sensitivity with a 30-minute signal half-life. With simple, seeding-to- measurement same plate preparation, britelite performs in high throughput and ultra-high throughput environ- ments, using 384- or 1536-well microplate formats.

The difference in light output and signal decay is illustrated for 1 x E-10 gram luciferase.

10 steadylite HTS™ High Sensitivity Long-Lived Glow Luminescence Reporter Gene Assay System

steadylite HTS™ is a homogeneous high-sensitivity, Sensitivity of steadylite HTS compared to luclite long-lived glow assay with a signal half-life of 4 to 5 hours that is specifically designed for large batch processing.

With a signal twice as bright as the long-lived glow system luclite, steadylite HTS is able to detect lower levels of luciferase —perfect for more sensitive analyses in 1536-well plates measured on high throughput imagers such as PerkinElmer’s ViewLux. The optimized mixing properties of steadylite HTS also reduce inaccuracies caused by incomplete mixing and Shows a dilution series of luciferase enzyme in Dulbecco’s PBS/0.1% BSA, measured in a white 96-well OptiPlate using the PerkinElmer capillary action (wicking), consistently producing TopCount NXT Microplate Scintillation and Luminescence Counter. more precise readings. steadylite HTS has a lower detection limit for luciferase than luclite.

Versatile Detection Instrumentation to Measure Your GPCR Assays

PerkinElmer provides versatile, scalable instrumenta- application-focused instrumentation means you can be tion solutions that you can count on to perform consis- confident our advice and support will be on target with tently and reliably in your screening applications. And, your needs. To inquire about ordering instrumentation, our years of experience in building state-of-the-art call 1-800-762-4000.

Choice of Instrumentation

Assay Platform ViewLux EnVision MicroBeta TopCount VICTOR3

DELFIA [FP]2 Image FlashPlate FlashPlate FlashBlue LANCE AlphaScreen Luminescence

www.perkinelmer.com 11 ViewLux™ UltraHTS Microplate Imager Our ViewLux™ UltraHTS Microplate Imager, based on sophisticated imaging technology, provides high sensitivity and fast measurement of fluorescence polarization (FP), fluorescence intensity, time-resolved fluorescence (TRF), luminescence and absorbance assays. Because the instrument reads entire plates in one exposure, throughput isn’t affected by plate density.

ViewLux is the ideal tool for our high sensitivity DELFIA, homogeneous LANCE™, luminescence and [FP]2 technologies. In addition, ViewLux is also the first system with the potential for true high throughput processing of radioisotopic assays by exploiting the high ViewLux quantum efficiency of our Image FlashPlate technology.

EnVision™ Multilabel Plate Readers Our versatile EnVision Multilabel Plate Readers are fast, application-oriented instruments for assay development and high throughput screening. Their unique modular design lets you choose the optical modules for the detection technologies and applications you need to run. EnVision Readers handle all fluorescence, luminescence, absorbance, fluorescence polarization, radiometric and time-resolved fluorescence detection technologies, including AlphaScreen technology.

MicroBeta® Liquid Scintillation and Luminescence Counter EnVision The MicroBeta Liquid Scintillation and Luminescence Counter handles a variety of applications in different sample formats. This makes the MicroBeta counter ideal for traditional GPCR filtration assays or scintillation proximity assays using, for example, our FlashBlue beads.

MicroBeta’s versatility is due, in part, to its unique detector design. Each detector consists of two photo- multiplier tubes (PMT) positioned above and below the sample. These count the sample from the top and bottom at the same time. The result is true coincidence counting, the classically employed method for liquid scintillation counting that results in exceptional sensitivity while maintaining low backgrounds.

MicroBeta

12 TopCount® Liquid Scintillation and Luminescence Counter The TopCount Liquid Scintillation and Luminescence Counter provides high performance, high throughput scintillation counting ideal for GPCR applications in 96- and 384-well microplates. It is perfect for counting scintillator-coated plates, such as FlashPlate microplates.

TopCount’s high efficiency and low background counting results from its unique counting technology. A patented single photomultiplier tube (PMT) time resolved counting method results in virtually crosstalk- free counting when used with opaque plates. High sensitivity is reached by using TR-LSC technology, a method that discriminates between background and true counts by analyzing the decay period of each TopCount scintillation event. The results are high signal-to-noise ratios, superior sensitivity, and linearity over a wide dynamic range.

3 3 ™ VICTOR ™ and VICTOR V Multilabel Plate Readers 3 Our VICTOR ™ Plate Readers are multilabel, multitask counters for all light-emitting and light-absorbing detection technologies including fluorescence (top and bottom), luminescence, absorbance, UV absorbance, time-resolved fluorometry, and fluorescence polariza- tion. You can choose the detection technologies and options you need and upgrade as your needs change. A small bench top unit, VICTOR3 can operate as a stand-alone instrument or integrate into robotic systems. VICTOR3 PerkinElmer — Your GPCR Source

PerkinElmer supports all your GPCR applications with and drug discovery efforts. Quite simply, we believe products and expertise ranging from receptor ligand you’ll find no better source for everything you need for binding assays to functional cellular assays. Our assay GPCR applications. With PerkinElmer as your GPCR platforms and detection technologies include essential source, why go anywhere else? For more information radioisotopic technologies and state-of-the-art lumi- or to order, visit www.perkinelmer.com/las or nescence and fluorescence alternatives to maximize call 1-800-762-4000. the performance and productivity of your research

www.perkinelmer.com 13 Optimized Assay Systems for GPCR Ligand Binding and Sign

PerkinElmer’s offerings take you beyond the ligand-GPCR binding event to an ability to assess the actual cellular response by systems for functional cellular assays and second messengers mean you can confidently employ functional screens in your d

14 nal Transduction Measurements y directly monitoring the signal transduction cascade. Optimized assay drug discovery program or disease research with all classes of GPCR targets.

www.perkinelmer.com 15 Ordering Information

DELFIA® Ligands and Reagents

Product Description Quantity Cat. No. , A synthetic amide, similar to amphibian bombesin with 150 pmol AD0227 Eu-labeled a europium chelate coupled to the amino end of the peptide. 3+ The sequence of DELFIA Eu-labeled bombesin is: Ac-Eu Ahx-

PQRLGNQWAVGHLM-NH2. Supplied lyophilized. EGF, A recombinant human protein with a europium chelate coupled to the 350 pmol AD0217 Eu-labeled amino end of the protein. Supplied lyophilized. 1,400 pmol AD0218 , A synthetic human galanin peptide with a europium chelate coupled to 200 pmol AD0215 Eu-labeled the amino end of the peptide. Supplied lyophilized. 850 pmol AD0216 Interleukin-2, A recombinant human protein with a europium chelate coupled to the 650 pmol CR401-650 Eu-labeled amino end and/or groups of the protein. Supplied ready for use in 50 mmol/L Tris-HCl buffered salt solution. Interleukin-4, A recombinant protein with a europium chelate coupled to the amino 60 pmol CR403-060 Eu-labeled end and/or lysine groups of the protein. Supplied ready to use in 50 mmol/L Tris-HCl buffered salt solution. Interleukin-5, A recombinant human protein with a europium chelate coupled to the 400 pmol CR402-400 Eu-labeled amino end and/or lysine groups of the protein. Supplied ready for use in 50 mmol/L Tris-HCl buffered salt solution. Interleukin-8, A recombinant human protein (72 amino acid form) with a europium 160 pmol AD0213 Eu-labeled chelate coupled to the amino end of the protein. Supplied lyophilized. 700 pmol AD0214 , A synthetic peptide amide, similar to the human or porcine motilin, 60 pmol AD0208 Eu-labeled with a europium chelate coupled to the carboxyl end of the peptide. 240 pmol AD0209 The sequence of DELFIA Eu-labeled motilin is: 3+ H-FVPIFTYGELQRMQEKERNKGQ-Eu -NH2. Supplied lyophilized. NDP-αMSH, A synthetic peptide amide, analog of αMSH, with a europium chelate 200 pmol AD0225 Eu-labeled coupled to the carboxyl end of the peptide. The sequence of DELFIA 800 pmol AD0226 α 3+ Eu-labeled NDP- MSH is: Ac-SYS-Nle-EH(D)FRWGKPV-Eu -NH2. Supplied lyophilized. , A synthetic peptide, similar to human neurotensin with a europium 200 pmol AD0219 Eu-labeled chelate coupled to the amino end of the peptide. The sequence of 750 pmol AD0220 3+ DELFIA Eu-labeled neurotensin is: Ac-Eu -ELTENKPRRPYIL-OH. Supplied lyophilized. Neurokinin A, A synthetic peptide amide, similar to human neurokinin A with a 300 pmol AD0221 Eu-labeled europium chelate coupled to the amino end of the peptide. The sequence 1,200 pmol AD0222 3+ of DELFIA Eu-labeled neurokinin A is: H-Eu -HKTDSFVGLM-NH2. Supplied lyophilized. Substance P, A synthetic peptide amide, similar to human substance P with a 200 pmol AD0223 Eu-labeled europium chelate coupled to the amino end of the peptide. The sequence 800 pmol AD0224 3+ of DELFIA Eu-labeled substance P is: H-Eu -RPKPQQFFGLM-NH2. Supplied lyophilized. TNFα, A recombinant human protein with a europium chelate coupled to the 600 pmol CR400-600 Eu-labeled amino end and/or lysine groups of the protein. Supplied ready for use in 50 mmol/L Tris-HCl buffered salt solution. DELFIA Develops complete fluorescence by dissociation enhancement after 50 mL 1244-104 Enhancement the completion of the binding reaction. Suitable for the detection of 250 mL 1244-105 Solution both europium and samarium. 50 mL of Enhancement Solution is 1,000 mL 4001-001 sufficient for 250 wells of a standard 96-well microplate.

16 Product Description Quantity Cat. No. DELFIA L*R A 25-fold concentrate containing 250 mmol/L Tris-HCl buffered salt 250 mL CR135-250

Wash Solution solution (pH 7.5) with 125 mmol/L MgCl2, and 0.05% sodium azide

Concentrate (25X) (NaN3) as preservative. Store at 2–8 °C until expiration. DELFIA L*R A 10-fold concentrate optimized to give minimum fluorescence 250 mL CR134-250 Binding Buffer background and non-specific binding in DELFIA ligand receptor binding Concentrate assays. It contains 500 mmol/L Tris-HCI buffered salt solution (pH 7.5)

with 50 mmol/L MgCl2, 250 µmol/L ethylenediaminetetraacetic acid (EDTA), 2% bovine serum albumin (BSA), and 0.05% sodium azide

(NaN3) as preservative. AcroWell 96-well polypropylene filter plate, pore size 0.45 µm, 10 plates P5020 Filter Plate for DELFIA assays.

GPCR-Specific NEN Radioligands

(List of GPCR ligands that do not have corresponding membranes offered by PerkinElmer.) Description Cat. No.

125 4 I, [ I]Tyr -, (Human) NEX101

125 2 Angiotensin IV, [ I]-Tyr -, (Human) NEX295

125 Antisauvagine-30 [ I]-[1-His-2]- NEX399

3 Baclofen, (-)-[butyl-4- H(N)]- NET867

125 CCL15, [ I]-, (Human, Recombinant) NEX401

125 CGP 42112A, [ I]- NEX324

125 6-Ckine (CCL21), [ I]-, Bolton-Hunter Labeled, (Human, Recombinant) NEX387

125 Complement C3a, [ I]-, Bolton-Hunter Labeled, (Human) NEX356

125 CTACK, [ I]- , (Human, Recombinant) NEX391

125 Eotaxin, [ I]-, (Human, Recombinant) NEX314

125 Exendin (9-39), [ I]- NEX335

125 125 Follicle Stimulating Hormone, [ I]-, ([ I]-FSH) NEX173

125 Fractalkine, [ I]-, (Human, Recombinant) NEX368

125 GLP-1(7-36), [ I]- NEX308

125 GLP-2, [ I]-, Bolton-Hunter Labeled NEX390

125 , [ I]-, Receptor Grade NEX207

125 H2 , [ I]-, Bolton-Hunter Labeled NEX409

125 125 Human Chorionic Gonadotropin, [ I]-, ([ I]-HCG) NEX106

125 I309, [ I]-, Bolton-Hunter Labeled, (Human, Recombinant) NEX364

125 IP-10, [ I]-, Bolton-Hunter Labeled, (Human, Recombinant) NEX348

125 I-TAC, [ I]-, (Human, Recombinant) NEX376

10 9 3 Kallidin(Des-Arg ,Leu ), [3,4-prolyl-3,4- H(N)]- NET1096

10 3 Kallidin(Des-Arg ), [3,4-prolyl-3,4- H(N)]- NET1064

125 6 Luteinizing Hormone-Releasing Hormone, [ I]-[D-Trp ]- NEX365

125 5 125 Luteinizing Hormone-Releasing Hormone, [ I]Tyr -, ([ I]-LHRH) NEX163

125 Mamba Intestinal Toxin-1 (MIT-1), [ I]-, Bolton-Hunter Labeled NEX410 125 Melatonin, 2-[ I]- NEX236 3 Methylhistamine Dihydrochloride, N-α-[methyl- H]- NET1027

www.perkinelmer.com 17 Description Cat. No.

125 MIP-3β, [ I]-, (Human, Recombinant) NEX370 125 MIP-3α, [ I]-, (Human, Recombinant) NEX371 125 10 S (NPS), [ I-Tyr ]-, (Human) NEX411 125 A, [ I]- NEX367 125 125 Ornithine Vasotocin Analog, [ I]-, ([ I]-OVTA) NEX254 125 2 Oxytocin, [ I]Tyr - NEX187 3 Oxytocin, [tyrosyl-2,6- H]- NET858 125 PACAP27, [ I]- NEX294 125 , [ I]-, (Human) NEX315 125 8,21 34 125 (1-34) Amide, [ I-Nle ,Tyr ]-, (Rat), ([ I]-rPTH Amide) NEX353 125 8,18 34 Parathyroid Hormone (1-34), [ I]-[Nle , Tyr ]-, (Human) NEX397 125 Analog, [ I]iodoazido-, (Iodoarylazidoprazosin) NEX219 3 Prazosin, [7-methoxy- H]- NET823 125 20 -Releasing Peptide, [ I]Tyr - NEX384 3 Prostaglandin E2, [5,6,8,11,12,14,15- H(N)]- NET428 3 Prostaglandin F2α, [5,6,8,9,11,12,14,15- H(N)]- NET433 125 QRFP-43, [ I]-, (Human) NEX408 125 RANTES, [ I]-, (Human, Recombinant) NEX292 125 SDF-1α, [ I]-, (Human, Recombinant) NEX346 125 TARC, [ I]-, (Human, Recombinant) NEX369 3 Thromboxane B2, [5,6,8,9,11,12,14,15- H(N)]- NET603 2 3 3 Thyrotropin Releasing Hormone (3-methyl-histidine ), [L-histidyl-4- H(N), L-propyl-3,4- H(N)]- NET705 125 2 125 Thyrotropin Releasing Hormone, [ I]His -, ([ I]-TRH) NEX153 125 2 8 Vasopressin, [ I]Tyr , Arg - NEX128

SignalScreen Cloned Receptors — Exclusively from PerkinElmer! Each SignalScreen package contains sufficient material for 200 units of receptor (50 units/tube, 4 tubes per package). One unit is defined as a point in a standard microplate filtration protocol run at a concentration of radioligand at or near its Kd. A complete product description and recommended protocol are included on the Product Information Sheet.

† Receptor Type Subtype Species Host Cat. No. Complementary Ligands Cat. No.

3 Adenosine A1 Rat Sf9 6110120001KT Cyclopentyl-1,3-Dipropylxanthine, 8-[dipropyl-2,3- H(N)]- NET974 3 Ethylcarboxamidoadenosine, 5'-N-[adenine-2,8- H]-, (NECA) NET811 3 A1 Rat CHO 6110511001KT Cyclopentyl-1,3-Dipropylxanthine, 8-[dipropyl-2,3- H(N)]- NET974 3 Ethylcarboxamidoadenosine, 5'-N-[adenine-2,8- H]-, (NECA) NET811 3 A1 Human CHO 6110542001KT Cyclopentyl-1,3-Dipropylxanthine, 8-[dipropyl-2,3- H(N)]- NET974 3 Ethylcarboxamidoadenosine, 5'-N-[adenine-2,8- H]-, (NECA) NET811 3 A2A Rat CHO 6110536001KT CGS 21680, [carboxyethyl- H(N)]- NET1021 3 Ethylcarboxamidoadenosine, 5'-N-[adenine-2,8- H]-, (NECA) NET811 125 125 A3 Rat CHO 6110531001KT AB-MECA, [ I]-(4-amino-3-[ I]iodobenzyl-5'-N-)- NEX312 α 3 2A Human Sf9 6110113001KT MK-912, [methyl- H]- NET1059 125 Iodoclonidine, p-[ I]- NEX253 125 (2-[(2,5-dichloro-4-[ I]-phenyl)imino]imidazolidine) 3 HCI, [benzene ring- H]- NET613 3 Epinephrine, L-[N-methyl- H]- NET623 3 , [methyl- H]- NET659 3 , levo-[ring-2,5,6- H]- NET678 3 , [methyl- H]- NET722 3 UK-14,304, [imidazolyl-4,5- H]- NET853 18 † Receptor Type Subtype Species Host Cat. No. Complementary Ligands Cat. No. α 3 Adrenergic Human Sf9 6110114001KT MK-912, [methyl- H]- NET1059 125 Iodoclonidine, p-[ I]- 125 (2-[(2,5-dichloro-4-[ I]-phenyl)imino]imidazolidine) NEX253 3 Clonidine HCI, [benzene ring- H]- NET613 3 Epinephrine, L-[N-methyl- H]- NET623 3 Yohimbine, [methyl- H]- NET659 3 Norepinephrine, levo-[ring-2,5,6- H]- NET678 3 Rauwolscine, [methyl- H]- NET722 3 UK-14,304, [imidazolyl-4,5- H]- NET853 β 3 1 Human Sf9 6110110001KT (-)-CGP-12177, [5,7- H]- NET1061 125 (-)-, [ I]- NEX189 125 Iodo-(±)-cyanopindolol, [ I]- NEX174 125 (-)-, [ I]- NEX211 3 , L-[4- H]- NET515 3 HCl, levo [ring, propyl- H]- NET720 β 3 2 Human Sf9 6110106001KT (-)-CGP-12177, [5,7- H]- NET1061 125 (-)-Cyanopindolol, [ I]- NEX189 125 Iodo-(±)-cyanopindolol, [ I]- NEX174 125 (-)-Pindolol, [ I]- NEX211 3 Propranolol, L-[4- H]- NET515 3 Dihydroalprenolol HCl, levo [ring, propyl- H]- NET720 α β γ 125 CRLR+ Human Sf9(G s 1 2) 6110136001KT Adrenomedullin (13-52), [ I]- NEX385 RAMP2

1 125 4 8 Angiotensin II AT1 Human Sf9 6110121001KT Angiotensin II, [Sar , I-Tyr , Ile ]- NEX248 125 4 Angiotensin II, [ I-Tyr ]- NEX105 3 Angiotensin II, (5-L-isoleucine) [tyrosyl-3,5- H(N)]- NET446 1 125 4 8 AT 1 Human CHO 6110533001KT Angiotensin II, [Sar , I-Tyr , Ile ]- NEX248 125 4 Angiotensin II, [ I-Tyr ]- NEX105 3 Angiotensin II, (5-L-isoleucine) [tyrosyl-3,5- H(N)]- NET446

65 75 77 125 Apelin APJ Human CHO 6110561001KT Apelin 13 [Glp , Nle , Tyr ], [ I]- NEX393 α β γ 3 Cannabinoid CB1 Human Sf9(G i3 1 2) 6110129001KT CP 55940, [side chain-2,3,4- H(N)]- NET1051 3 WIN 55212-2, [5,7-naphtyl- H]- NET1058 3 Anandamide, [arachidonyl-5,6,8,9,11,12,14,15- H]- NET1073 α β γ 3 CB2 Human Sf9(G i3 1 2) 6110130001KT CP 55940, [side chain-2,3,4- H(N)]- NET1051 3 WIN 55212-2, [5,7-naphtyl- H]- NET1058 3 Anandamide, [arachidonyl-5,6,8,9,11,12,14,15- H]- NET1073 α β γ 125 125 CGRP CRLR+ Human Sf9(G s 1 2) 6110135001KT Gene Related Peptide, [ I]-, ([ I]-hCGRP) NEX354 125 125 RAMP1 Calcitonin Gene Related Peptide (8-37), [ I]-, ([ I]-hCGRP) NEX319

125 Chemoattractant C5a Human CHO 6110526001KT Complement C5a , [ I]-, Bolton-Hunter Labeled NEX250 FPR1 Human CHO 6110527001KT Formyl-L-methionyl-L-leucyl-L-phenylalanine NET563 3 N-[phenylalanine-ring-3,4,5- H(N)]-, (Chemotactic Peptide) α β γ 125 125 Chemokine CXCR2 Human Sf9(G i3 1 2) 6110132001KT Interleukin-8, [ I]-, ([ I]-IL-8) NEX277 125 GRO Alpha/MGSA, [ I]- NEX321

125 125 CXCR2 Human CHO 6110524001KT Interleukin-8, [ I]-, ([ I]-IL-8) NEX277 125 GRO Alpha/MGSA, [ I]- NEX321 125 CCR1 Human CHO 6110525001KT MIP-1α, [ I]- NEX298 3 47 125 MIP-1β (Leu ,Gly ), [ I]- NEX299 125 CCR2b Human HEK293 6110550001KT MCP-1, [ I]-, Bolton-Hunter Labeled NEX332 125 JE, [ I]-, (Murine, recombinant MCP-1) NEX313

125 Chemoattractant C5a Human CHO 6110526001KT Complement C5a , [ I]-, Bolton-Hunter Labeled NEX250 FPR1 Human CHO 6110527001KT Formyl-L-methionyl-L-leucyl-L-phenylalanine 3 N-[phenylalanine-ring-3,4,5- H(N)]- (Chemotactic Peptide) NET563

125 CCKA Human Sf9 6110125001KT Cholecystokinin Octapeptide, [ I]-, Bolton-Hunter Labeled NEX203 125 ([ I]-CCK-8) 125 CCKA Human NIH-3T3 6110508001KT Cholecystokinin Octapeptide, [ I]-, Bolton-Hunter Labeled NEX203 125 ([ I]-CCK-8)

www.perkinelmer.com 19 † Receptor Type Subtype Species Host Cat. No. Complementary Ligands Cat. No. 3 D1 Human Sf9 6110101001KT SCH 23390, [N-methyl- H]- NET930 3 D1 Human L Cells 6110513001KT SCH 23390, [N-methyl- H]- NET930 3 D2L Human Sf9 6110137001KT Methylspiperone, [N-methyl- H]- NET856 125 Iodospiperone, 2'-[ I]- NEX284 125 R-(+)-trans-7-hydroxy-PIPAT, [ I]- NEX307 3 , [Benzene ring- H]-, (Spiroperidol) NET565 3 Dihydroxyphenylethylamine, 3,4-[ring-2,5,6- H]-, (Dopamine) NET673 3 Sulpiride, (-), [methoxy- H]- NET775 3 Raclopride, [methoxy- H]- NET975 3 YM-09151-2, [N-methyl- H]- NET1004 3 Quinpirole, [N-propyl- H]- NET1085 α β γ 3 D2S Human Sf9(G i3 1 2) 6110138001KT Methylspiperone, [N-methyl- H]- NET856 125 Iodospiperone, 2'-[ I]- NEX284 125 R-(+)-trans-7-hydroxy-PIPAT, [ I]- NEX307 3 Spiperone, [benzene ring- H]-, (Spiroperidol) NET565 3 Dihydroxyphenylethylamine, 3,4-[ring-2,5,6- H]-, (Dopamine) NET673 3 Sulpiride, (-), [methoxy- H]- NET775 3 Raclopride, [methoxy- H]- NET975 3 YM-09151-2, [N-methyl- H]- NET1004 3 Quinpirole, [N-propyl- H]- NET1085 3 D2S Human L Cells 6110554001KT Methylspiperone, [N-methyl- H]- NET856 125 Iodospiperone, 2'-[ I]- NEX284 125 R-(+)-trans-7-hydroxy-PIPAT, [ I]- NEX307 3 Spiperone, [benzene ring- H]-, (Spiroperidol) NET565 3 Dihydroxyphenylethylamine, 3,4-[ring-2,5,6- H]-, (Dopamine) NET673 3 Sulpiride, (-), [methoxy- H]- NET775 3 Raclopride, [methoxy- H]- NET975 3 YM-09151-2, [N-methyl- H]- NET1004 3 Quinpirole, [N-propyl- H]- NET1085 3 D3 Rat Sf9 6110139001KT Methylspiperone, [N-methyl- H]- NET856 3 Dihydroxyphenylethylamine, 3,4-[ring-2,5,6- H]-, (Dopamine) NET673 3 8-Hydroxy-DPAT, [propyl-2,3-ring-1,2,3- H]- NET929 3 D4.2 Human Sf9 6110112001KT YM-09151-2, [N-methyl- H]- NET1004 3 Spiperone, [benzene ring- H]-, (Spiroperidol) NET565 3 Dihydroxyphenylethylamine, 3,4-[ring-2,5,6- H]-, (Dopamine) NET673 3 D4.4 Human Sf9 6110122001KT YM-09151-2, [N-methyl- H]- NET1004 3 Spiperone, [benzene ring- H]-, (Spiroperidol) NET565 3 Dihydroxyphenylethylamine, 3,4-[ring-2,5,6- H]-, (Dopamine) NET673 3 D4.4 Human CHO 6110520001KT YM-09151-2, [N-methyl- H]- NET1004 3 Spiperone, [benzene ring- H]-, (Spiroperidol) NET565 3 Dihydroxyphenylethylamine, 3,4-[ring-2,5,6- H]-, (Dopamine) NET673 3 D4.7 Human Sf9 6110123001KT YM-09151-2, [N-methyl- H]- NET1004 3 Spiperone, [benzene ring- H]-, (Spiroperidol) NET565 3 Dihydroxyphenylethylamine, 3,4-[ring-2,5,6- H]-, (Dopamine) NET673 3 D5 Human Sf9 6110108001KT SCH 23390, [N-methyl- H]- NET930

125 13 ETA Human CHO 6110547001KT Endothelin-1, [ I-Tyr ]- NEX259

125 FPRL-1 FPRL-1 Human CHO 6110563001KT WKYMVm, [ I]-, Bolton-Hunter Labeled NEX386

GABA B1a Human CHO 6110545001KT B1b Human CHO 6110546001KT B1a Human HEK293 6110560001KT B1b Human HEK293 6110557001KT B1a + R2 Human HEK293 6110559001KT B1b + R2 Human HEK293 6110556001KT

125 Galanin GalR1 Human HEK293 6110537001KT Galanin, [ I]-, (Porcine) NEX243 125 EBNA Galanin, [ I]-, (Human) NEX333

20 † Receptor Type Subtype Species Host Cat. No. Complementary Ligands Cat. No. 3 H1 Human CHO 6110564001KT Pyrilamine, [pyridinyl 5- H]-, (Mepyramine) NET594 3 H2 Human HEK293 6110565001KT Tiotidine, [methyl- H]-, (ICI 125, 211) NET688

125 Motilin MTL-R1 Human CHO 6110544001KT Motilin, [ I]- NEX378

3 Muscarinic M1 Human Sf9 6110103001KT Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 Pirenzepine, [N-methyl- H]- NET780 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041 3 M1 Human CHO 6110503001KT Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 Pirenzepine, [N-methyl- H]- NET780 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041 3 M2 Human Sf9 6110104001KT Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 Pirenzepine, [N-methyl- H]- NET780 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041 3 M2 Human CHO 6110505001KT Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 Pirenzepine, [N-methyl- H]- NET780 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041 3 M3 Human Sf9 6110109001KT Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 Pirenzepine, [N-methyl- H]- NET780 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041 3 M3 Human CHO 6110504001KT Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 Pirenzepine, [N-methyl- H]- NET780 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041 3 M4 Human Sf9 6110105001KT Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 Pirenzepine, [N-methyl- H]- NET780 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041 3 M4 Human CHO 6110506001KT Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 Pirenzepine, [N-methyl- H]- NET780 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041

www.perkinelmer.com 21 † Receptor Type Subtype Species Host Cat. No. Complementary Ligands Cat. No.

3 Muscarinic M5 Human Sf9 6110116001KT Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 Pirenzepine, [N-methyl- H]- NET780 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041 3 M5 Human CHO 6110507001KT Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 Pirenzepine, [N-methyl- H]- NET780 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041 125 3 Neurokinin NK1 Human UC11 6110551001KT Substance P, [ I-Lys ]-, Bolton-Hunter Labeled NEX190 125 8 Substance P, [ I-Tyr ]- NEX152 3 Substance-P (9-Sar, 11-Met(O2)), [2-prolyl-3,4- H]- NET1025 3 SR140333, [phenoxy-6- H]- NET1101 3 Substance P, [leucyl-3,4,5- H(N)]- NET1115 3 NK2 Human CHO 6110510001KT SR 48968, [benzamide-4- H]- NET1077 125 4 , [ I-Lys ]-, Bolton-Hunter Labeled NEX218 125 125 125 Neurokinin A, [ I]-, ([ I]-Substance K; [ I]-NKA) NEX252 3 Substance P, [leucyl-3,4,5- H(N)]- NET1115 125 4 NK3 Human CHO 6110534001KT Eledoisin, [ I-Lys ]-, Bolton-Hunter Labeled NEX218 125 125 MePhe7-Neurokinin B, [ I-His]-, ([ I]-NKB) NEX285 3 Senktide, [phenylalanyl-3,4,5- H]- NET997

125 125 Y1 Human Sf9 6110133001KT Peptide YY, [ I]-, (Porcine), ([ I]-PYY) NEX240 125 31 34 Peptide YY, [ I]-(Leu , Pro ) NEX334 125 125 Peptide YY, [ I]-, (Human), [ I]-PYY) NEX341

125 3 Neurotensin NTS1 Human CHO 6110518001KT Neurotensin, [ I-Tyr ]- NEX198 3 Neurotensin, [3, 11-tyrosyl-3, 5- H(N)]- NET605 125 3 NT2 Human HEK293 6110566001KT Neurotensin, [ I-Tyr ]- NEX198 3 Neurotensin, [3, 11-tyrosyl-3, 5- H(N)]- NET605

125 14 Nociceptin ORL-1 Human CHO 6110540001KT Nociceptin, [ I-Tyr ]- NEX338 3 (OP4) Nociceptin, [leucyl-3,4,5- H]- NET1130

3 Opioid δ-opioid Mouse Sf9 6110115001KT Naltrindole, [5',7'- H]- NET1065 3 (OP1) Enkephalin (2-D-alanine-5-D-), [tyrosyl-3,5- H(N)]- NET648 3 Enkephalin, [tyrosyl-2,6- H(N)]-, (2-D-penicillamine, 5-D-penicillamine) (DPDPE) NET922 3 Deltorphin II(2-D-Ala), [tyrosyl-3,5- H]- NET1087 3 Diprenorphine, [15,16- H]- NET1121

3 δ-opioid Human HEK293 6110549001KT Bremazozine, (-)-[9- H(N)]- NET821 3 (OP1) Naltrindole, [5',7'- H]- NET1065 3 Enkephalin (2-D-alanine-5-D-leucine), [tyrosyl-3,5- H(N)]- NET648 3 Enkephalin, [tyrosyl-2,6- H(N)]-, (2-D-penicillamine, 5-D-penicillamine) (DPDPE) NET922 3 Deltorphin II(2-D-Ala), [tyrosyl-3,5- H]- NET1087 3 Diprenorphine, [15,16- H]- NET1121 3 κ-opioid Human HEK293 6110558001KT Diprenorphine, [15,16- H]- NET1121 3 (OP2) Naloxone, [N-Allyl-2,3- H]- NET719 3 U-69593, [Phenyl-3,4- H]- NET952 3 Naltrindole, [5',7'- H]- NET1065 3 µ-opioid Human CHO 6110535001KT Naloxone, [N-allyl-2,3- H]- NET719 3 (OP3) DAMGO, [tyrosyl-3,5- H(N)]- NET902 3 Naltrindole, [5',7'- H]- NET1065 3 Diprenorphine, [15,16- H]- NET1121

22 † Receptor Type Subtype Species Host Cat. No. Complementary Ligands Cat. No. 3 5-HT1A Human Sf9 6110117001KT 8-Hydroxy-DPAT, [propyl-2,3-ring-1,2,3- H]- NET929 3 MPPF, [methyl- H]- NET1109 3 5-HT1A Human CHO 6110501001KT 8-Hydroxy-DPAT, [propyl-2,3-ring-1,2,3- H]- NET929 3 MPPF, [methyl- H]- NET1109 125 5-HT2C Human HEK293 6110548001KT DOI, [ I]-(±)- NEX255 3 Spiperone, [benzene ring- H]-, (Spiroperidol) NET565 3 Hydrochloride, [ethylene- H]-, (R41 468) NET791 3 5-HT5A Human HEK293 6110529001KT Lysergic Acid Diethylamide, [N-methyl- H]- NET638 125 125 Lysergic Acid Diethylamide, 2-[ I]iodo-(+)-, ([ I]-LSD) NEX199 3 5-HT6 Rat Sf9 6110118001KT Lysergic Acid Diethylamide, [N-methyl- H]- NET638 125 125 Lysergic Acid Diethylamide, 2-[ I]iodo-(+)-, ([ I]-LSD) NEX199 3 5-HT6 Human Sf9 6110124001KT Lysergic Acid Diethylamide, [N-methyl- H]- NET638 125 125 Lysergic Acid Diethylamide, 2-[ I]iodo-(+)-, ([ I]-LSD) NEX199

3 5-HT6 Human HeLa 6110530001KT Lysergic Acid Diethylamide, [N-methyl- H]- NET638 125 125 Lysergic Acid Diethylamide, 2-[ I]iodo-(+)-, ([ I]-LSD) NEX199 3 5-HT7 Rat Sf9 6110119001KT Lysergic Acid Diethylamide, [N-methyl- H]- NET638 125 125 Lysergic Acid Diethylamide, 2-[ I]iodo-(+)-, ([ I]-LSD) NEX199 3 5-HT7 Human Sf9 6110127001KT Lysergic Acid Diethylamide, [N-methyl- H]- NET638 125 125 Lysergic Acid Diethylamide, 2-[ I]iodo-(+)-, ([ I]-LSD) NEX199 3 5-HT7 Human CHO 6110512001KT Lysergic Acid Diethylamide, [N-methyl- H]- NET638 125 125 Lysergic Acid Diethylamide, 2-[ I]iodo-(+)-, ([ I]-LSD) NEX199

Vasopressin V1A Human CHO 6110555001KT Vasopressin (linear), V-1A Antagonist NEX310 1 2 125 6 (Phenylacetyl , 0-Me-D-Tyr , [ I-Arg ]-) 3 Vasopressin, 8-arginine, [phenylalanyl-3,4,5- H(N)]- NET800 3 V1B Human CHO 6110543001KT Vasopressin, 8-arginine, [phenylalanyl-3,4,5- H(N)]- NET800 3 V2 Human CHO 6110541001KT Vasopressin, 8-arginine, [phenylalanyl-3,4,5- H(N)]- NET800 † The radioligands in bold are used for QC validation of the membrane product and are recommended.

Membrane Target Systems Each MTS package contains sufficient material for 400 assay units of receptor in a volume of 0.4 or 1.0 mL. One assay unit is defined as a point in a standard microplate filtration protocol run at a concentration of radioligand at or near its Kd. A complete product description and recommended protocol are included on the Product Information Sheet.

GPCRs

† Receptor Type Subtype Species Host Cat. No. Complementary Ligands Cat. No.

3 Adenosine A2A Human HEK293 RBHA2AM400UA CGS 21680, [carboxyethyl- H(N)]- NET1021 3 RBHA2AM100UA Ethylcarboxamidoadenosine, 5'-N-[adenine-2,8- H]-, (NECA) NET811 125 125 A3 Rat HEK293 RBRA3M400UA AB-MECA, [ I]-(4-Amino-3-[ I]iodobenzyl-5'-N-)- NEX312 EBNA α 3 Adrenergic 2A* Human HT-29 RBHL2AM400UA MK-912, [methyl- H]- NET1059 125 Iodoclonidine, p-[ I]- 125 (2-[(2,5-dichloro-4-[ I]-phenyl)imino]imidazolidine) NEX253 3 Clonidine HCI, [benzene ring- H]- NET613 3 Epinephrine, L-[N-methyl- H]- NET623 3 Yohimbine, [methyl- H]- NET659 3 Norepinephrine, levo-[ring-2,5,6- H]- NET678 3 Rauwolscine, [methyl- H]- NET722 3 UK-14,304, [imidazolyl-4,5- H]- NET853 β 125 2 Human HEK293 RBHBE2M400UA (-)-Cyanopindolol, [ I]- NEX189 125 EBNA Iodo-(±)-cyanopindolol, [ I]- NEX174 125 (-)-Pindolol, [ I]- NEX211 3 Propranolol, L-[4- H]- NET515 3 Dihydroalprenolol HCl, levo-[ring, propyl- H(N)]- NET720 3 (-)-CGP-12177, [5,7- H]- NET1061

www.perkinelmer.com 23 † Receptor Type Subtype Species Host Cat. No. Complementary Ligands Cat. No. β 125 Adrenergic 3* Human SK-N-MC RBHBE3M400UA (-)-Cyanopindolol, [ I]- NEX189 125 Iodo-(±)-cyanopindolol, [ I]- NEX174 125 (-)-Pindolol, [ I]- NEX211 3 Propranolol, L-[4- H]- NET515 3 Dihydroalprenolol HCl, levo-[ring, propyl- H(N)]- NET720 3 (-)-CGP-12177, [5,7- H]- NET1061 1 125 4 8 Angiotensin AT1* Human KAN-TS RBHAT1M400UA Angiotensin II, [Sar , I-Tyr , Ile ]- NEX248 125 4 Angiotensin II, [ I-Tyr ]- NEX105 3 Angiotensin II, (5-L-isoleucine)[tyrosyl-3,5- H(N)]- NET446

125 4 Bombesin BRS1 Human CHO RBHBS1M400UA Bombesin, [ I-Tyr ]- NEX258 6 125 11 13 14 Bombesin (6-14), [D-Tyr -[ I]- βAla , Phe , Nle ]- NEX377 125 4 BRS2 Human HEK283 RBHBS2M400UA Bombesin, [ I-Tyr ]- NEX258 6 125 11 13 14 Bombesin (6-14), [D-Tyr -[ I]- βAla , Phe , Nle ]- NEX377 6 125 11 13 14 BRS3 Human Balb 3T3 RBHBS3M400UA Bombesin (6-14), [D-Tyr -[ I]- βAla , Phe , Nle ]- NEX377

3 B2 Human CHO RBHB2M400UA Bradykinin, [2,3-prolyl-3,4- H(N)]- NET706

3 Cannabinoid CB1 Human HEK293 RBHCB1M400UA CP 55940, [side chain-2,3,4- H(N)]- NET1051 3 EBNA RBHCB1M100UA WIN 55212-2, [5,7-naphtyl- H]- NET1058 3 Anandamide, [arachidonyl-5,6,8,9,11,12,14,15- H]- NET1073 3 CB2 Human HEK293 RBXCB2M400UA CP 55940, [side chain-2,3,4- H(N)]- NET1051 3 EBNA RBXCB2M100UA WIN 55212-2, [5,7-naphtyl- H]- NET1058 3 Anandamide, [arachidonyl-5,6,8,9,11,12,14,15- H]- NET1073

125 0 CRF1 CRF1 Human HEK293 RBHCRF1M400UA , [ I-Tyr ]- NEX306 125 0 Corticotropin Releasing Factor, [ I-Tyr ]-, NEX216 125 0 (Human, Rat), [ I-]-Tyr CRF

3 Chemoattractant CRTH2 Human HEK293 RBHTH2M400UA Prostaglandin D2, [ H]- NET616

125 125 CGRP CGRP* Human SK-N-MC RBHGRPM400UA Calcitonin Gene Related Peptide, [ I]-, ([ I]-hCGRP) NEX354 125 125 Calcitonin Gene Related Peptide (8-37), [ I]-, ([ I]-hCGRP) NEX319

125 Chemokine CCR1 Human HEK293 RBHCC1M400UA MIP-1α, [ I]- NEX298 3 47 125 MIP-1β, (Leu ,Gly ), [ I]- NEX299 125 125 CXCR2 Human HEK293 RBHCX2M400UA Interleukin-8, [ I]-, ([ I]-IL-8) NEX277 125 EBNA GRO Alpha/MGSA, [ I]- NEX321 125 CXCR6 Human HEK293 RBHCX6M400UA CXCL16, [ I]- NEX398

125 Cholecystokinin CCKA Human NIH 3T3 RBHCKAM400UA Cholecystokinin Octapeptide, [ I]-, NEX203 125 Bolton-Hunter Labeled, ([ I]-CCK-8) 125 CCKB Human HEK293 RBHCKBM400UA Cholecystokinin Octapeptide, [ I]-, NEX203 125 Bolton-Hunter Labeled, [ I]-CCK-8) 125 12 I, [ I-Tyr ] NEX176

3 Dopamine D2s Human CHO RBHD2CM400UA Methylspiperone, [N-methyl- H]- NET856 125 RBHD2CM100UA Iodospiperone, 2'-[ I]- NEX284 125 R-(+)-trans-7-hydroxy-PIPAT, [ I]- NEX307 3 Spiperone, [benzene ring- H]-, (Spiroperidol) NET565 3 Dihydroxyphenylethylamine, 3,4-[ring-2,5,6-3 H]-, (Dopamine) NET673 3 Sulpiride, (-), [methoxy- H]- NET775 3 Raclopride, [methoxy- H]- NET975 3 YM-09151-2, [N-methyl- H]- NET1004 3 Quinpirole, [N-propyl- H]- NET1085 3 D4.2 Human CHO RBHD42M400UA Spiperone, [benzene ring- H]-, (Spiroperidol) NET565 3 RBHD42M100UA Dihydroxyphenylethylamine, 3,4-[Ring-2,5,6- H]-, (Dopamine) NET673 3 YM-09151-2, [N-methyl- H]- NET1004 3 D4.4 Human CHO RBHD44M400UA Spiperone, [Benzene ring- H]-, (Spiroperidol) NET565 3 Dihydroxyphenylethylamine, 3,4-[Ring-2,5,6- H]-, (Dopamine) NET673 3 YM-09151-2, [N-methyl- H]- NET1004 3 D4.7 Human CHO RBHD47M400UA Spiperone, [benzene ring- H]-, (Spiroperidol) NET565 3 Dihydroxyphenylethylamine, 3,4-[Ring-2,5,6- H]-, (Dopamine) NET673 3 YM-09151-2, [N-methyl- H]- NET1004 3 D5 Human HEK293 RBHD5M400UA SCH 23390, [N-methyl- H]- NET930

24 † Receptor Type Subtype Species Host Cat. No. Complementary Ligands Cat. No.

125 Galanin GAL1 Human HEK293 RBXGL1M400UA Galanin, [ I]-, (Porcine) NEX243 125 EBNA Galanin, [ I]-, (Human) NEX333 125 GAL2 Human CHO RBHGL2M400UA Galanin, [ I]-, (Human) NEX333 125 Galanin, [ I]-, (Porcine) NEX243

125 Gastric Inhibitory GIP Human HEK293 RBHGIPM400UA Gastric Inhibitory Polypeptide, [ I]- NEX402 Peptide

125 Ghrelin GHS-R Human HEK293 RBHGHSM400UA Ghrelin, [His[ I]]-, (Human) NEX388

125 GPR8 Human HEK293 RBHGP8M400UA Neuropeptide W23, [ I]- NEX403 125 Neuropeptide B23 (Des-Br), [ I]- NEX405

125 Melanin- MCH1 Human CHO RBHMCH1M400UA S36057, [ I-Tyr]- NEX396 125 concentrating Melanin-Concentrating Hormone, [ I]- NEX373 13 125 19 Hormone Melanin-Concentrating Hormone, [Phe , [ I]-Tyr ]- NEX375 125 MCH-1R Antagonist, [ I]- NEX406 α 4 7 125 Melanocortin MC3** Human HEK293 RBXMC3M400UA -MSH, Nle , D-Phe , [ I]- NEX352 125 SHU9119, [ I]- NEX362 α 4 7 125 MC4** Human HEK293 RBHMC4M400UA -MSH, Nle , D-Phe , [ I]- NEX352 125 RBHMC4M100UA SHU9119, [ I]- NEX362 125 AGRP (Ac 87-132), [ I]- NEX372 125 His-MT II, [ I]- NEX374 α 4 7 125 MC5 Human HEK293 RBXMC5M400UA -MSH, Nle , D-Phe , [ I]- NEX352 EBNA 125 Metastin Human CHO RBHMTSM400UA Metastin 45-54, [ I]- NEX395

125 Motilin MOT1 Human HEK293 RBHMOTM400UA Motilin, [ I]- NEX378

3 Muscarinic M1 Human CHO RBHM1M400UA Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 RBHM1M100UA Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 Pirenzepine, [N-methyl- H]- NET780 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041 3 M2 Human CHO RBHM2M400UA Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 RBHM2M100UA Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041 3 M3 Human CHO RBHM3M400UA Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 RBHM3M100UA Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041 3 M4 Human CHO RBHM4M400UA Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 RBHM4M100UA Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041 3 M5 Human CHO RBHM5M400UA Scopolamine Methyl Chloride, [N-methyl- H]- NET636 3 RBHM5M100UA Acetylcholine Iodide, [acetyl- H]- NET113 3 Quinuclidinyl Benzilate, L-[benzilic-4, 4'- H]- NET656 3 Oxotremorine-M Acetate, [methyl- H]- NET671 3 4-DAMP, [N-methyl- H]- NET1040 3 AF-DX 384, [2, 3-dipropylamino- H]- NET1041

www.perkinelmer.com 25 † Receptor Type Subtype Species Host Cat. No. Complementary Ligands Cat. No.

125 18 125 NMU1 Human HEK293 RBHNU1M400UA Neuromedin U-25, [ I-Tyr ]-, ([ I]-NMU-25) NEX383 125 Neuromedin U-8, [ I]- NEX392 125 NMU2 Human HEK293 RBHNU2M400UA Neuromedin U-8, [ I]- NEX392 125 18 125 Neuromedin U-25, [ I-Tyr ]-, ([ I]-NMU-25) NEX383

1 125 3 Neuropeptide FF NPFF1 Human CHO-DHFR(-) RBHNF1M400UA Neuropeptide FF, [D-Tyr [ I], N-MePhe ]- NEX381

1 125 3 NPFF2 Human CHO RBHNF2M400UA Neuropeptide FF, [D-Tyr [ I], N-MePhe ]- NEX381

125 125 Neuropeptide Y NPY1* Human SK-N- RBHNP1M400UA Peptide YY, (Porcine), [ I]-, ([ I]-PYY) NEX240 125 31 34 MC Peptide YY, [ I]-(Leu , Pro ) NEX334 125 125 Peptide YY, [ I]-, (Human), ([ I]-PYY) NEX341 125 125 NPY2* Human KAN-TS RBHNP2M400UA Peptide YY, [ I]-, (Porcine), [ I]-PYY) NEX240 125 31 34 Peptide YY, [ I]-(Leu , Pro ) NEX334 125 125 Peptide YY, [ I]-, (Human), ([ I]-PYY) NEX341

125 3 Neurotensin NTS1 Human HEK293 RBXNT1M400UA Neurotensin, [ I-Tyr ]- NEX198 3 Neurotensin, [3,11-tyrosyl-3, 5- H(N)]- NET605

3 Opioid δ-opioid Human CHO RBHODM400UA Naltrindole, [5',7'- H]- NET1065 3 (OP1) Enkephalin (2-D-alanine-5-D-leucine), [tyrosyl-3,5- H(N)]- NET648 3 Enkephalin, [tyrosyl-2,6- H(N)]-, (2-D-Penicillamine, 5-D-Penicillamine) (DPDPE) NET922 3 Deltorphin II(2-D-Ala), [tyrosyl-3,5- H]- NET1087 3 Diprenorphine [15,16- H]- NET1121 3 µ-opioid Human CHO RBHOMM400UA Diprenorphine [15,16- H]- NET1121 3 (OP3) RBHOMM100UA Naloxone, [N-allyl-2,3- H]- NET719 3 DAMGO, [tyrosyl-3,5- H(N)]- NET902 3 Naltrindole, [5',7'- H]- NET1065

3 ORL1 Human HEK293 RBHORLM400UA Nociceptin, [leucyl-3,4,5- H]- NET1130 125 14 (OP4) RBHORLM100UA Nociceptin, [ I-Tyr ]- NEX338

3 Prostanoid CRTH2 Human HEK293 RBHTH2M400UA Prostaglandin D2, [5,6,8,9,12,14,15- H(N)]- NET616 3 TP Human HEK293 RBHTPM400UA SQ 29548, [5,6- H]- NET936 EBNA

3 Serotonin 5-HT1A Human HEK293 RBHS1AM400UA 8-Hydroxy-DPAT, [propyl-2,3-ring-1,2,3- H]- NET929 3 EBNA MPPF, [methyl- H]- NET1109 3 5-HT5A Human CHO RBHS5AM400UA Lysergic Acid Diethylamide, [N-methyl- H]- NET638 125 125 RBHS5AM100UA Lysergic Acid Diethylamide, 2-[ I]iodo-(+)-, ([ I]-LSD) NEX199 3 5-HT6 Human HEK293 RBHS6M400UA Lysergic Acid Diethylamide, [N-methyl- H]- NET638 125 125 RBHS6M100UA Lysergic Acid Diethylamide, 2-[ I]iodo-(+)-, ([ I]-LSD) NEX199 3 5-HT6 Rat HEK293 RBRS6M400UA Lysergic Acid Diethylamide, [N-methyl- H]- NET638 125 125 Lysergic Acid Diethylamide, 2-[ I]iodo-(+)-, ([ I]-LSD) NEX199 3 5-HT7 Rat HEK293 RBRS7M400UA Lysergic Acid Diethylamide, [N-methyl- H]- NET638 125 125 Lysergic Acid Diethylamide, 2-[ I]iodo-(+)-, ([ I]-LSD) NEX199

125 1 Somatostatin SST4 Human HEK293 RBHST4M400UA Somatostatin, [ I-Tyr ]- NEX389 EBNA 125 1 SST5 Human HEK293 RBHST5M400UA Somatostatin, [ I-Tyr ]- NEX389 EBNA RBHST5M100UA

125 9 Urotensin UR2 Mouse CHO RBMUR2M400UA Urotensin II, [ I-Tyr ]-, (Human) NEX379 RBMUR2M100UA

1 Vasopressin V1A Human HEK293 RBHV1AM400UA Vasopressin (linear), V-1A Antagonist (Phenylacetyl , 2 125 6 0-Me-D-Tyr , [ I-Arg ]-) NEX310 3 Vasopressin, 8-arginine, [phenylalanyl-3,4,5- H(N)]- NET800 3 V1B Human HEK293 RBHV1BM400UA Vasopressin, 8-arginine, [phenylalanyl-3,4,5- H(N)]- NET800

125 VIP VIP* Human HT29 RBHVIPM400UA Vasoactive Intestinal Polypeptide, [ I]- NEX192

26 Tyrosine Kinase Receptors

† Receptor Type Subtype Species Host Cat. No. Complementary Ligands Cat. No.

125 Epidermal EGF* Human A431 RBHEGFM400UA Epidermal Growth Factor, [ I]- NEX160 Growth Factor

Transportors

† Receptor Type Subtype Species Host Cat. No. Complementary Ligands Cat. No.

3 Dopamine n.a. Human CHO RBHDATM400UA WIN 35428, [N-methyl- H]- NET1033 125 RBHDATM100UA RTI-55, [ I]- NEX272 125 RTI-121, [ I]- NEX318 3 Cocaine, Levo-[benzoyl-3,4- H(N)]- NET510 3 Mazindol, [4'- H]- NET816 3 GBR 12935, [propylene-2,3- H]- NET918

3 Norepinephrine n.a. Human MDCK RBHNETM400UA Nisoxetine Hydrochloride, [N-methyl- H]- NET1084 RBHNETM100UA

3 Serotonin n.a. Human HEK293 RBHSTM400UA Hydrochloride, [benzene ring- H(N)]- NET576 3 RBHSTM100UA Paroxetine, [phenyl-6'- H]- NET869 3 Citalopram, [N-methyl- H]- NET1039

Ion Channels

† Receptor Type Subtype Species Host Cat. No. Complementary Ligands Cat. No.

125 125 Nicotinic* Human IMR32 RBHNICM400UA Epibatidine, [ I]-, ([ I]-IPH) NEX358

3 Serotonin 5-HT3 Human HEK293 RBHS3M400UA GR 65630, [N-methyl- H]- NET1011 3 RBHS3M100UA BRL-43694, [9-methyl- H]- NET1030

† The radioligands in bold are used for QC validation of the membrane product and are recommended. * Non-recombinant

** For sales in the United States: These products can ONLY be sold to customers who hold a license from the University of Michigan (“Licensed Customers”). ** For sales outside of the United States: These products can ONLY be sold to Licensed Customers or to customers who are incorporated outside of the United States AND whose principal place of business is in such territory of incorporation.

FlashBlue Scintillating Beads and FlashPlate Microplates

Product Description Quantity Cat. No. FlashBlue GPCR Scintillating Beads 100 mg vial 100 mg FBB001100MG 500 mg vial 500 mg FBB001500MG 2.0 g vial 2.0 g FBB001002G Please inquire Bulk N/A Basic FlashPlate HTS, 384-well Basic plate, 384 wells 5 plates SMP400E001PK 20 plates SMP400001PK Basic FlashPlate Basic plate, 96 wells 5 plates SMP200E001PK 50 plates SMP200001PK Wheat Germ Agglutinin FlashPlate Wheat germ agglutinin-coated 2 plates SMP411001PK HTS PLUS, 384-well Basic FlashPlate, 384 wells 10 plates SMP411A001PK Wheat Germ Agglutinin FlashPlate PLUS Wheat germ agglutinin-coated 5 plates SMP105001PK Basic FlashPlate, 96-well Basic FlashPlate, 96 wells 20 plates SMP105A001PK Basic Image FlashPlate Basic plate, 384 wells 5 plates RMP100E001PK 20 plates RMP100001PK Wheat Germ Agglutinin Image FlashPlate, Wheat germ agglutinin-coated Image 5 plates RMP111E001PK 384-well FlashPlate, 384 wells 40 plates RMP111001PK

www.perkinelmer.com 27 Adenylyl Cyclase Assay Systems for Cell-Based Functional cAMP Measurement Product Description Quantity Cat. No. AlphaScreen cAMP Assay Kit Direct cellular cAMP assay 1,000 assay points 6760625D 10,000 assay points 6760625M 50,000 assay points 6760625R FlashPlate Adenylyl Cyclase Direct cellular cAMP assay 2-plate kit SMP701001KT Activation Assay System, Direct cellular cAMP assay 5-plate kit SMP701A001KT 125 [ I]-, 384-well Direct cellular cAMP assay, Buffer with IBMX 40-plate kit SMP701B001KT Direct cellular cAMP assay, 40-plate kit SMP701C001KT Buffer without IBMX FlashPlate Adenylyl Cyclase Direct cellular cAMP assay 2-plate kit SMP004001KT Activation Assay System, Direct cellular cAMP assay 5-plate kit SMP004A001KT 125 [ I]-, 96-well Direct cellular cAMP assay, Buffer with IBMX 40-plate kit SMP004B001KT Direct cellular cAMP assay, 40-plate kit SMP004C001KT Buffer without IBMX [FP]2 cAMPfire Assay Kit 384 wells 2-plate kit FPA203002KT 384 wells 40-plate kit FPA203040KT 384 wells for ViewLux 2-plate kit FPA204002KT 384 wells for ViewLux 40-plate kit FPA204040KT

cAMP Assay Systems for cAMP Quantitation in Plasma, Urine and Cell Culture Samples Product Description Quantity Cat. No. DELFIA cAMP Assay Kit 384 wells 2-plate kit CR92-102 384 wells 10-plate kit 4004-0010 96 wells 2-plate kit CR89-102 96 wells 10-plate kit 4003-0010 FlashPlate cAMP 96 wells 2-plate kit SMP001001KT 125 [ I]- Assay System 96 wells 5-plate kit SMP001A001KT 96 wells 100-plate pack SMP001J001KT

125 Cyclic AMP [ I]- RIA Kit Reagents sufficient for 200 assay 1 kit NEK033001KT tubes when protocol is followed.

GTP Binding Assays and Reagents

Product Description Quantity Cat. No. DELFIA GTP-Binding Kit Contains 10 AcroWell filter plates 10-plate kit AD167 (96-well) and all required reagents Wheat Germ Agglutinin Wheat germ agglutinin-coated 2 plates SMP411001PK FlashPlate HTS PLUS, 384-well Basic FlashPlate, 384 wells 10 plates SMP411A001PK Wheat Germ Agglutinin FlashPlate PLUS Wheat germ agglutinin-coated 5 plates SMP105001PK Basic FlashPlate, 96-well Basic FlashPlate, 96 wells 20 plates SMP105A001PK Wheat Germ Agglutinin Image Wheat germ agglutinin-coated 5 plates RMP111E001PK FlashPlate Image FlashPlate, 384 wells 40 plates RMP111001PK Basic Image FlashPlate Basic plate, 384 wells 5 plates RMP100E001PK 20 plates RMP100001PK FlashBlue GPCR Scintillating Beads 100 mg vial 100 mg FBB001100MG 500 mg vial 500 mg FBB001500MG 2.0 g vial 2.0 g FBB001002G Please inquire Bulk N/A 35 GTPγS Radionucleotide Guanosine 5'-(γ-thio)triphosphate, [ S]- 1 mCi (37 MBq) NEG030H001MC 35 GTPγS Radionucleotide Guanosine 5'-(γ-thio)triphosphate, [ S]- 250 µCi (9.25 MBq) NEG030H250UC UniFilter Plates See UniFilter selection table on page 29.

28 IP3 Functional Assays Product Description Quantity Cat. No.

AlphaScreen IP3 Assay Supplement Contains IP3 Binding Protein and Biotinylated 500 pts 6760621C

IP3 Analog. To perform the IP3 assay, the GST 10,000 pts 6760621M Detection Kit is also required (see below).

AlphaScreen GST To perform the IP3 assay, both the 500 pts 6760603C (Gluthatione-S-Transferase) AlphaScreen GST Detection Kit and 10,000 pts 6760603M

Detection Kit IP3 Assay Supplement are required. 50,000 pts 6760603R

Reporter Gene Assays Product Size Cat. No. luclite Assay Kit* 300 points 6016916 1,000 points 6016911 5,000 points 6016917 10,000 points 6016919 200,000 points 6016915 britelite Assay Kit** 10 mL 6016976 100 mL 6016971 500 mL 6016977 1,000 mL 6016979 steadylite HTS Assay Kit** 10 mL 6016986 100 mL 6016981 500 mL 6016987 1,000 mL 6016989

* Assay points per kit are based on 96-well microplates. The 10,000 and 200,000 point bulk assay kits are supplied without positive control and enhancer solutions. For additional information on bulk assay kit availability, contact your PerkinElmer representative. ** Assay volume is dependent on microplate density. Bulk quantity assay kits are also available. Please contact your PerkinElmer representative for additional details.

Microplates for Filtration Assays and Cell-Based Assays

Product Description Quantity Cat. No. UniFilter Plate White, shallow 24-well, 50 plates 6005176 GF/B filter-bottom, Barex® White, shallow 96-well, 5 plates (sample pack) 6005244 GF/B filter-bottom, Barex White, shallow 96-well, 50 plates 6005177 GF/B filter-bottom, Barex White, shallow 96-well, 5 plates (sample pack) 6005243 GF/C filter-bottom, Barex White, shallow 96-well, 50 plates 6005174 GF/C filter-bottom, Barex CellEx Poly-D-Lysine 384-well, black frame with clear-bottom, 10 plates 6005672 coated microplates sterile with lid (individually wrapped) 30 plates (2 x 15 6005670 microplate sleeves) 120 plates (8 x 15 6005679 microplate sleeves)

For a complete overview of our entire microplate offering, please see our Microplates Guide (007097_01), available on our website at www.perkinelmer.com.

www.perkinelmer.com 29 PerkinElmer Life and Analytical Sciences 710 Bridgeport Avenue Shelton, CT 06484-4794 USA Phone: (800) 762-4000 or (+1) 203-925-4602 www.perkinelmer.com

For a complete listing of our global offices, visit www.perkinelmer.com/lasoffices

©2004 PerkinElmer, Inc. All rights reserved. The PerkinElmer logo and design are registered trademarks of PerkinElmer, Inc. AlphaScreen, cAMPfire, CellEx, EnVision, FlashBlue, [FP]2, LANCE, ScreenReady Targets, VICTOR3, VICTOR3 V and ViewLux are trademarks and DELFIA, FlashPlate, MicroBeta, SignalScreen, TopCount, TriCarb and UniFilter are registered trademarks of PerkinElmer, Inc. or its subsidiaries, in the United States and other countries. AcroPrep and AcroWell are trademarks of Pall Corporation. Alexa Fluor is a trademark of Molecular Probes, Inc. Barex is a registered trademark of BP Chemicals, Inc. All other trademarks not owned by PerkinElmer, Inc. or its subsidiaries that are depicted herein are the property of their respective owners. PerkinElmer reserves the right to change this document at any time without notice and disclaims liability for editorial, pictorial or typographical errors.

007154_01 Printed in USA