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TABLE 1 Studies of Antagonist Activity in Constitutively Active
TABLE 1 Studies of antagonist activity in constitutively active receptors systems shown to demonstrate inverse agonism for at least one ligand Targets are natural Gs and constitutively active mutants (CAM) of GPCRs. Of 380 antagonists, 85% of the ligands demonstrate inverse agonism. Receptor Neutral Antagonist Inverse Agonist Reference Human β2-adrenergic Dichloroisoproterenol, pindolol, labetolol, timolol, Chidiac et al., 1996; Azzi et alprenolol, propranolol, ICI 118,551, cyanopindolol al., 2001 Turkey erythrocyte β-adrenergic Propranolol, pindolol Gotze et al., 1994 Human β2-adrenergic (CAM) Propranolol Betaxolol, ICI 118,551, sotalol, timolol Samama et al., 1994; Stevens and Milligan, 1998 Human/guinea pig β1-adrenergic Atenolol, propranolol Mewes et al., 1993 Human β1-adrenergic Carvedilol CGP20712A, metoprolol, bisoprolol Engelhardt et al., 2001 Rat α2D-adrenergic Rauwolscine, yohimbine, WB 4101, idazoxan, Tian et al., 1994 phentolamine, Human α2A-adrenergic Napthazoline, Rauwolscine, idazoxan, altipamezole, levomedetomidine, Jansson et al., 1998; Pauwels MPV-2088 (–)RX811059, RX 831003 et al., 2002 Human α2C-adrenergic RX821002, yohimbine Cayla et al., 1999 Human α2D-adrenergic Prazosin McCune et al., 2000 Rat α2-adrenoceptor MK912 RX821002 Murrin et al., 2000 Porcine α2A adrenoceptor (CAM- Idazoxan Rauwolscine, yohimbine, RX821002, MK912, Wade et al., 2001 T373K) phentolamine Human α2A-adrenoceptor (CAM) Dexefaroxan, (+)RX811059, (–)RX811059, RS15385, yohimbine, Pauwels et al., 2000 atipamezole fluparoxan, WB 4101 Hamster α1B-adrenergic -
Zebrafish Behavioral Profiling Links Drugs to Biological Targets and Rest/Wake Regulation
www.sciencemag.org/cgi/content/full/327/5963/348/DC1 Supporting Online Material for Zebrafish Behavioral Profiling Links Drugs to Biological Targets and Rest/Wake Regulation Jason Rihel,* David A. Prober, Anthony Arvanites, Kelvin Lam, Steven Zimmerman, Sumin Jang, Stephen J. Haggarty, David Kokel, Lee L. Rubin, Randall T. Peterson, Alexander F. Schier* *To whom correspondence should be addressed. E-mail: [email protected] (A.F.S.); [email protected] (J.R.) Published 15 January 2010, Science 327, 348 (2010) DOI: 10.1126/science.1183090 This PDF file includes: Materials and Methods SOM Text Figs. S1 to S18 Table S1 References Supporting Online Material Table of Contents Materials and Methods, pages 2-4 Supplemental Text 1-7, pages 5-10 Text 1. Psychotropic Drug Discovery, page 5 Text 2. Dose, pages 5-6 Text 3. Therapeutic Classes of Drugs Induce Correlated Behaviors, page 6 Text 4. Polypharmacology, pages 6-7 Text 5. Pharmacological Conservation, pages 7-9 Text 6. Non-overlapping Regulation of Rest/Wake States, page 9 Text 7. High Throughput Behavioral Screening in Practice, page 10 Supplemental Figure Legends, pages 11-14 Figure S1. Expanded hierarchical clustering analysis, pages 15-18 Figure S2. Hierarchical and k-means clustering yield similar cluster architectures, page 19 Figure S3. Expanded k-means clustergram, pages 20-23 Figure S4. Behavioral fingerprints are stable across a range of doses, page 24 Figure S5. Compounds that share biological targets have highly correlated behavioral fingerprints, page 25 Figure S6. Examples of compounds that share biological targets and/or structural similarity that give similar behavioral profiles, page 26 Figure S7. -
)&F1y3x PHARMACEUTICAL APPENDIX to THE
)&f1y3X PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE )&f1y3X PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 3 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. Product CAS No. Product CAS No. ABAMECTIN 65195-55-3 ACTODIGIN 36983-69-4 ABANOQUIL 90402-40-7 ADAFENOXATE 82168-26-1 ABCIXIMAB 143653-53-6 ADAMEXINE 54785-02-3 ABECARNIL 111841-85-1 ADAPALENE 106685-40-9 ABITESARTAN 137882-98-5 ADAPROLOL 101479-70-3 ABLUKAST 96566-25-5 ADATANSERIN 127266-56-2 ABUNIDAZOLE 91017-58-2 ADEFOVIR 106941-25-7 ACADESINE 2627-69-2 ADELMIDROL 1675-66-7 ACAMPROSATE 77337-76-9 ADEMETIONINE 17176-17-9 ACAPRAZINE 55485-20-6 ADENOSINE PHOSPHATE 61-19-8 ACARBOSE 56180-94-0 ADIBENDAN 100510-33-6 ACEBROCHOL 514-50-1 ADICILLIN 525-94-0 ACEBURIC ACID 26976-72-7 ADIMOLOL 78459-19-5 ACEBUTOLOL 37517-30-9 ADINAZOLAM 37115-32-5 ACECAINIDE 32795-44-1 ADIPHENINE 64-95-9 ACECARBROMAL 77-66-7 ADIPIODONE 606-17-7 ACECLIDINE 827-61-2 ADITEREN 56066-19-4 ACECLOFENAC 89796-99-6 ADITOPRIM 56066-63-8 ACEDAPSONE 77-46-3 ADOSOPINE 88124-26-9 ACEDIASULFONE SODIUM 127-60-6 ADOZELESIN 110314-48-2 ACEDOBEN 556-08-1 ADRAFINIL 63547-13-7 ACEFLURANOL 80595-73-9 ADRENALONE -
Effects of Dopamine Receptor Antagonism and Amphetamine Sensitization on Sign- and Goal-Tracking After Extended Training
bioRxiv preprint doi: https://doi.org/10.1101/848150; this version posted November 20, 2019. The copyright holder for this preprint (which was not certified by peer review) is the author/funder, who has granted bioRxiv a license to display the preprint in perpetuity. It is made available under aCC-BY 4.0 International license. BioRxiv Chaudhri Lab Concordia University RESEARCH ARTICLE PREPRINT Effects of dopamine receptor antagonism and amphetamine sensitization on sign- and goal-tracking after extended training Shaun Yon-Seng Khoo1,2, Alexandra Uhrig1 and Nadia Chaudhri1,* 1Center for Studies in Behavioral Neurobiology, Department of Psychology, Concordia University, Montreal, Quebec, Canada. and 2Department of Pharmacology and Physiology, Faculty of Medicine, Université de Montréal, Montreal, QC, Canada. *[email protected] Abstract Rationale. The dopamine system is thought to be important in incentive salience attribution, where motivational value is assigned to a cue that predicts an appetitive reinforcer (sign-tracking), however, dopamine’s role may change with extended training. Objectives. We tested the effects of selective dopamine D1-like and D2-like receptor antagonism on the expression of Pavlovian conditioned approach after extended Pavlovian conditioned approach (PCA) training. We also tested the hypothesis that locomotor sensitization would accelerate the phenotypic shift to sign-tracking. Methods. 24 male Long-Evans rats were subjected to 20 PCA sessions in which one lever (CS+, 10 s) predicted 0.2 mL sucrose delivery and the other lever (CS–) did not. SCH-23390 or eticlopride were administered prior to behavioral tests at doses of 0, 0.01, and 0.1 mg/kg (s.c.). -
Reproducibility of Behavioral Phenotypes in Mouse Models - a Short History with Critical and Practical Notes
Reproducibility of behavioral phenotypes in mouse models - a short history with critical and practical notes Vootele Voikar Neuroscience Center and Laboratory Animal Center, Helsinki Institute of Life Science Correspondence: Mustialankatu 1 G Helsinki, Finland [email protected] Progress in pre-clinical research is built on endorsed by more than 1000 journals so far, reproducible findings, yet reproducibility has awareness of researchers and the quality of different dimensions and even meanings. Indeed, publications have not been sufficiently improved the terms reproducibility, repeatability, and (13-15). In order to facilitate and enhance replicability are often used interchangeably, implementation of the ARRIVE guidelines, a although each has a distinct definition. Moreover, revised version with exhaustive explanation and reproducibility can be discussed at the level of elaborative documentation was recently published methods, analysis, results, or conclusions (1, 2). (16, 17). Despite these differences in definitions and Paradigm shift. Mice and rats are the most dimensions, the main aim for an individual widely used model animals in basic biomedicine. research group is the ability to develop new However, there has been a drastic change in the studies and hypotheses based on firm and reliable relative use of these two rodent species over time findings from previous experiments. In practice (Figure 1). Historically, the rat was the model of this wish is often difficult to accomplish. In this choice for behavioral studies but from the review, issues affecting reproducibility in the field beginning of 1990s a sharp shift from rats to mice of mouse behavioral phenotyping are discussed. took place. Obviously, this was due to rapid Crisis in reproducibility. -
Download Product Insert (PDF)
PRODUCT INFORMATION Eticlopride (hydrochloride) Item No. 29112 CAS Registry No.: 97612-24-3 Formal Name: 3-chloro-5-ethyl-N-[[(2S)-1-ethyl-2- pyrrolidinyl]methyl]-6-hydroxy-2-methoxy- OH benzamide, monohydrochloride O Synonyms: S-(−)-Eticlopride, (−)-Eticlopride N MF: C17H25ClN2O3 • HCl FW: 377.3 H N Purity: ≥98% O • HCl UV/Vis.: λmax: 213 nm Cl Supplied as: A crystalline solid Storage: -20°C Stability: ≥2 years Information represents the product specifications. Batch specific analytical results are provided on each certificate of analysis. Laboratory Procedures Eticlopride (hydrochloride) is supplied as a crystalline solid. A stock solution may be made by dissolving the eticlopride (hydrochloride) in the solvent of choice, which should be purged with an inert gas. Eticlopride (hydrochloride) is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF). The solubility of eticlopride (hydrochloride) in ethanol is approximately 30 mg/ml and approximately 25 mg/ml in DMSO and DMF. Description Eticlopride is a dopamine D2 and D3 receptor antagonist (Kis = 0.029 and 0.46 nM in MN9D mouse 1 neuronal cells expressing rat D2 and human D3 receptors, respectively). It is selective for dopamine D2 and D3 receptors (IC50s = 1 and 113 nM, respectively) over dopamine D1, α2-adrenergic, and β-adrenergic, histamine H1, and muscarinic receptors (IC50s = 700->100,000 nM), as well as the serotonin (5-HT) receptor subtypes 5-HT1 and 5-HT2 (IC50s = 6,200 and 830, respectively), but does bind α1-adrenergic receptors 2 (α1-ARs; IC50 = 110 nM) in radioligand binding assays. Eticlopride (10 μg/kg) inhibits stereotyped behavior in rats induced by 7-hydroxy-N,N-di-n-propyl-2-aminotetralin (7-OH-DPAT).3 It also inhibits ketamine- and cocaine-induced hypermotility in rats when administered at doses of 20 and 50 μg/kg, respectively. -
Director's Report
DIRECTOR’S REPORT to the National Advisory Council on Drug Abuse May 2020 Nora D. Volkow, M.D. Director National Institute on Drug Abuse TABLE OF CONTENTS RESEARCH HIGHLIGHTS ............................................................................................................ 1 GRANTEE HONORS AND AWARDS ......................................................................................... 21 STAFF HONORS AND AWARDS ................................................................................................ 22 STAFF CHANGES .......................................................................................................................... 23 IN MEMORIAM .............................................................................................................................. 25 RESEARCH HIGHLIGHTS BASIC AND BEHAVIORAL RESEARCH Local And Global Consequences Of Reward-Evoked Striatal Dopamine Release Li N, Jasanoff A. Nature. 2020 Apr 1. [Epub ahead of print]. The neurotransmitter dopamine is required for the reinforcement of actions by rewarding stimuli. Neuroscientists have tried to define the functions of dopamine in concise conceptual terms, but the practical implications of dopamine release depend on its diverse brain-wide consequences. Although molecular and cellular effects of dopaminergic signaling have been extensively studied, the effects of dopamine on larger-scale neural activity profiles are less well-understood. Here we combine dynamic dopamine-sensitive molecular imaging and functional magnetic resonance -
56Th Annual Teratology Society Meeting
54th Annual Meeting Birth Defects Research (Part A) 106:309–347 (2016) This event has been accredited by the McGill Center for Continuing Health Professional Education. 29th Annual Meeting for Organization of the Teratology Information Specialists (OTIS) June 25–28, 2016 40th Annual Meeting of the Developmental Neurotoxicology Society (DNTS) June 26–29, 2016 All text and graphics are © 2016 by the Teratology Society unless noted. River Walk photo courtesy of Staurt Dee/SACVB. Birth Defects Research (Part A) Clinical and Molecular Teratology 106:309–347 (2016) 310 TERATOLOGY SOCIETY PROGRAM Birth Defects Research (Part A) 106:309–347 (2016) TERATOLOGY SOCIETY PROGRAM 311 Program & Abstracts New Horizons in Birth Defects Research All text and graphics are © 2016 by the Teratology Society unless noted. River Walk photo courtesy of Staurt Dee/SACVB. Birth Defects Research (Part A) 106:309–347 (2016) 312 TERATOLOGY SOCIETY PROGRAM Program Overview FRIDAY, JUNE 24, 2016 12:00 Noon–1:30 PM 12:00 Noon–1:30 PM WEDNESDAY, JUNE 29, 2016 3:00 PM–6:00 PM Student and Postdoctoral Fellow Past Presidents’ and Honorees’ 6:30 AM–7:30 AM Council 1A Meeting Lunch Workshop Luncheon (By Invitation Only) Teratology Society 35th Annual Advancing Your Career in Birth Defects 3:00 PM–6:00 PM 1:30 PM–5:30 PM Volleyball Game Research and Prevention March of Dimes Symposium Registration Open (Advance Registration Required) 7:00 AM–2:30 PM New Approaches to the Treatment of Registration Open 3:00 PM–6:00 PM 1:30 PM–2:00 PM Birth Defects Speaker Ready Room Open 7:00 AM–2:30 PM F. -
Non-Pharmacological Factors That Determine Drug Use and Addiction Aldo Badiani, Klaus Miczek, Christian Müller, Serge Ahmed H
Non-pharmacological factors that determine drug use and addiction Aldo Badiani, Klaus Miczek, Christian Müller, Serge Ahmed H. To cite this version: Aldo Badiani, Klaus Miczek, Christian Müller, Serge Ahmed H.. Non-pharmacological factors that determine drug use and addiction. Neuroscience & Biobehavioral Reviews, Oxford: Elsevier Ltd., 2020, 110, pp.3-27. 10.1016/j.neubiorev.2018.08.015. hal-03005497 HAL Id: hal-03005497 https://hal.archives-ouvertes.fr/hal-03005497 Submitted on 25 Nov 2020 HAL is a multi-disciplinary open access L’archive ouverte pluridisciplinaire HAL, est archive for the deposit and dissemination of sci- destinée au dépôt et à la diffusion de documents entific research documents, whether they are pub- scientifiques de niveau recherche, publiés ou non, lished or not. The documents may come from émanant des établissements d’enseignement et de teaching and research institutions in France or recherche français ou étrangers, des laboratoires abroad, or from public or private research centers. publics ou privés. Special Issue – IBNS Non-pharmacological factors that determine drug use and addiction Serge Ahmed 1*, Aldo Badiani 2,3*, Klaus A. Miczek 4,5*, Christian P. Müller 6* 1 Université de Bordeaux, Institut des Maladies Neurodégénératives, UMR 5293, 146 rue Léo-Saignat, F-33000 Bordeaux, France; CNRS, Institut des Maladies Neurodégénératives, UMR 5293, 146 rue Léo-Saignat, F-33000 Bordeaux, France. 2 Department of Physiology and Pharmacology, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy. 3 Sussex Addiction Research and Intervention Centre (SARIC), School of Psychology, University of Sussex, BN1 9RH, Brighton, UK. 4 Psychology Department, Tufts University, Bacon Hall, 530 Boston Avenue, Medford, MA, 02155, USA. -
Effects of the 5-HT2C/2B Antagonist SB 206553 on Hyperactivity Induced by Cocaine Andrew C
Effects of the 5-HT2C/2B Antagonist SB 206553 on Hyperactivity Induced by Cocaine Andrew C. McCreary, Ph.D., and Kathryn A. Cunningham, Ph.D. Serotonin (5-HT) appears to play a modulatory role in the However, the 4-mg/kg dose of SB 206553 significantly behavioral effects of cocaine, although the impact of 5-HT2C enhanced the effects of cocaine on peripheral activity. Based receptors in this control has not been fully established. The upon the present observations and an interpretation of aim of the present study was to establish whether acute previous research to implicate 5-HT2C receptor control of pretreatment with the selective 5-HT2C/2B antagonist SB the dopamine (DA) mesoaccumbens pathways in behavior, 206553 (1, 2, and 4 mg/kg IP) altered hyperactivity induced a thorough and systematic analysis of the role of 5-HT2C by cocaine (15 mg/kg, IP) using an open field activity (and 5-HT2B) receptors in psychostimulant-induced system which recorded central, peripheral, and rearing behaviors is warranted. [Neuropsychopharmacology activity. Pretreatment with 1 and 2 mg/kg of SB 206553 20:556–564, 1999] © 1999 American College of attenuated cocaine-induced central and peripheral activity, Neuropsychopharmacology. Published by Elsevier respectively; rearing was also attenuated by the latter dose. Science Inc. KEY WORDS: Cocaine; Hyperactivity; SB 206553; Serotonin; vated DA neurotransmission, particularly within the 5-HT2C; 5-HT2B mesoaccumbens pathway originating from DA soma in the ventral tegmental area (VTA) and terminating in the The behavioral effects of cocaine in rodents include the nucleus accumbens (NAc), is especially important in stimulation of locomotor activity and stereotypy as well mediating the locomotor, discriminative stimulus and as convulsions at higher doses (Scheel-Kruger et al. -
The Developmental Neurobiology of Autism Spectrum Disorder
The Journal of Neuroscience, June 28, 2006 • 26(26):6897–6906 • 6897 Mini-Review Editor’s Note: Two reviews in this week’s issue examine the rapidly expanding interest in autism research in the neuroscience community. Moldin et al. provide a brief prospective on the overall state of research in autism. DiCicco-Bloom and colleagues summarize their presentations at the Neurobiology of Disease workshop at the 2005 Annual Meeting of the Society for Neuroscience. The Developmental Neurobiology of Autism Spectrum Disorder Emanuel DiCicco-Bloom,1 Catherine Lord,2 Lonnie Zwaigenbaum,3 Eric Courchesne,4,5 Stephen R. Dager,6 Christoph Schmitz,7 Robert T. Schultz,8 Jacqueline Crawley,9 and Larry J. Young10 1Departments of Neuroscience and Cell Biology and Pediatrics (Neurology), Robert Wood Johnson Medical School, University of Medicine and Dentistry of New Jersey, Piscataway, New Jersey 08854, 2University of Michigan Autism and Communication Disorders Center, Departments of Psychology and Psychiatry, University of Michigan, Ann Arbor, MI 48109-2054, 3Department of Pediatrics, McMaster University, Hamilton, Ontario, L8N 3Z5, Canada, 4Department of Neurosciences, University of California, San Diego, La Jolla, California 92093, 5Center for Autism Research, Children’s Hospital Research Center, San Diego, California 92123, 6Departments of Radiology, Psychiatry, and Bioengineering, University of Washington School of Medicine, Seattle, Washington 98105, 7Department of Psychiatry and Neuropsychology, Division of Cellular Neuroscience, Maastricht University, -
Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DIX to the HTSUS—Continued
20558 Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DEPARMENT OF THE TREASURY Services, U.S. Customs Service, 1301 TABLE 1.ÐPHARMACEUTICAL APPEN- Constitution Avenue NW, Washington, DIX TO THE HTSUSÐContinued Customs Service D.C. 20229 at (202) 927±1060. CAS No. Pharmaceutical [T.D. 95±33] Dated: April 14, 1995. 52±78±8 ..................... NORETHANDROLONE. A. W. Tennant, 52±86±8 ..................... HALOPERIDOL. Pharmaceutical Tables 1 and 3 of the Director, Office of Laboratories and Scientific 52±88±0 ..................... ATROPINE METHONITRATE. HTSUS 52±90±4 ..................... CYSTEINE. Services. 53±03±2 ..................... PREDNISONE. 53±06±5 ..................... CORTISONE. AGENCY: Customs Service, Department TABLE 1.ÐPHARMACEUTICAL 53±10±1 ..................... HYDROXYDIONE SODIUM SUCCI- of the Treasury. NATE. APPENDIX TO THE HTSUS 53±16±7 ..................... ESTRONE. ACTION: Listing of the products found in 53±18±9 ..................... BIETASERPINE. Table 1 and Table 3 of the CAS No. Pharmaceutical 53±19±0 ..................... MITOTANE. 53±31±6 ..................... MEDIBAZINE. Pharmaceutical Appendix to the N/A ............................. ACTAGARDIN. 53±33±8 ..................... PARAMETHASONE. Harmonized Tariff Schedule of the N/A ............................. ARDACIN. 53±34±9 ..................... FLUPREDNISOLONE. N/A ............................. BICIROMAB. 53±39±4 ..................... OXANDROLONE. United States of America in Chemical N/A ............................. CELUCLORAL. 53±43±0