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Home , Antalarmin, Devazepide, EMPA (drug), Endothelin 2, Galnon, Glucagon receptor

Receptors Product Listing | Edition 1 | USD

Oriental Fire-bellied Toad Bombina orientalis A source of Products for: • Regulation • Regulation • Feeding and Appetite Regulation • Glucose Regulation • Other Peptide • Processing Tocris Product Listing Series Contents This listing contains over 200 products from Tocris that are used in the study of peptide hormone receptors, grouped by physiological activity; these include the regulation of the anterior , blood pressure, feeding, appetite and blood glucose levels. A product listing of nuclear compounds is also available from www.tocris.com.

Anterior Pituitary Regulation...... 4 (NMU) Receptors...... 12

Corticotropin-releasing Factor (CRF) Receptors...... 4 B/W (NPBW) Receptors...... 12

Gonadotropin-releasing Hormone (GnRH) Receptors.... 4 Receptor...... 13

Kisspeptin Receptor...... 5 (NPY) Receptors...... 13

Neurotensin (NT) Receptors...... 5 Opioid Receptors...... 14

...... (sst) Receptors 5 Receptors...... 14

Thyrotropin-releasing Hormone (TRH) Receptors...... 5 VIP and PACAP Receptors...... 14

Blood Pressure Regulation...... 6 Glucose Regulation...... 15 (AT) Receptors...... 6 Receptor...... 15 (APJ) Receptors...... 7 Gastric Inhibitory Polypeptide (GIP) Receptor...... 15 Receptors...... 7 Receptor...... 15 -related Peptide (CGRP) Receptor...... 7 Glucagon-like Peptide 1 (GLP-1) Receptor...... 15 (ET) Receptors...... 7 Glucagon-like Peptide 2 (GLP-2) Receptor...... 15 Receptors (NPR)...... 7 Receptor...... 15 Tachykinin (NK) Receptors...... 8 Insulin-like Growth Factor 1 Receptor (IGF1R)...... 15 Urotensin-II (UT) Receptor...... 9 Other Peptide Hormones...... 16 Receptors...... 9 ...... 16 Feeding and Appetite Regulation...... 10 Neuropeptide FF/AF (NPFF) Receptors...... 16 Bombesin (BB) Receptors...... 10 Receptor...... 16 CART...... 10 Receptors...... 16 (CCK) Receptors...... 10

Peptide Hormone Processing...... 17 (GAL) Receptors...... 11

...... & Ghrelin-related Receptors...... 11 Angiotensin-converting Enzyme (ACE) 17

GPR103 (QRFP Receptor)...... 12 Chymase...... 17

Leptin Receptors...... 12 Dipeptidyl Peptidase IV (DPP-IV)...... 17

Melanin-concentrating Hormone (MCH) Receptors..... 12 Endothelin-converting Enzyme (ECE)...... 17

Melanocortin (MC) Receptors...... 12 -degrading Enzymes...... 17

Motilin Receptors...... 12 Tripeptidyl Peptidase II...... 17

2 | Peptide Hormone Receptors Introduction Most hormones are endogenous mediators secreted by endocrine glands as part of . There are three types of hormone: peptide, steroid and amine hormones. Peptide hormones are generally hydrophilic molecules that do not freely diffuse across cell membranes; instead, most exert their effects by binding to cell-surface receptors in target tissues (Figure 1). Many peptide hormone receptors are coupled to heterotrimeric G (that is, they are GPCRs). One notable exception is the , which possesses tyrosine kinase activity. Peptide receptors belong to the A and B classes of GPCRs, constituting a large group of receptors that are activated by extracellular or peptide ligands. Endogenous peptide receptor ligands bind to the N-terminus and/or the three extracellular loops of the receptor. The peptide receptor-binding domains are large, conferring high affinity and specificity. Small molecule drugs, however, only bind to small discrete pockets or sites on these 7-transmembrane proteins. Peptide hormones and their downstream effects are incredibly diverse; interactions within and between endocrine signaling pathways regulate a variety of interlinked processes, such as appetite modulation and feeding. Studying their activity therefore sheds light on a variety of different disorders. Research into endocrine disorders is facilitated by the use of and antagonists active at peptide hormone receptors.

Figure 1 | Peptide receptors involved in physiological processes

Liver and Glucose Regulation Anterior Pituitary Regulation Amylin Receptor CRF Receptors GIP Receptor GnRH Receptors Glucagon-like Peptide 1 Receptor Receptor Glucagon-like Peptide 2 Receptor Neurotensin Receptors Insulin Receptor Insulin-like TRH Receptors

Stomach and Gut Appetite & Feeding Regulation Bombesin Receptors CART CCK Receptors Galanin Receptors Ghrelin & Ghrelin-related Receptors GPR103 (QRFP Receptor) Receptors , Arteries and Kidneys MCH Receptors Blood Pressure Regulation Receptors Angiotensin Receptors Receptor Apelin Receptors Neuromedin U Receptors Bradykinin Receptors Neuropeptide B/W Receptors CGRP Receptor Endothelin Receptors Neuropeptide Y Receptors Natriuretic Peptide Receptors Opioid Receptors Tachykinin Receptors Urotensin-II Receptor VIP and PACAP Receptors Vasopressin Receptors

Tocris has a broad range of products for peptide hormone receptors, including small molecules and . The information listed within is correct at the time of printing. For the latest information, and to request free scientific literature, please visitwww.tocris.com.

www.tocris.com | 3 Tocris Product Listing Series Anterior Pituitary Regulation The anterior pituitary gland is regulated by hypothalamic hormones such as somatostatin, -releasing hormone and thyrotropin-releasing hormone. Stimulation by the influences the release of hormones from the anterior pituitary, including , and adrenocorticotropic hormone (ACTH).

Category Cat. No. Product Name Description Unit Size USD Corticotropin-releasing Factor (CRF) Receptors Agonists 1151 CRF (human, rat) Stimulates ACTH release 200 µg 155

1608 Stressin I CRF1 500 µg 365 1604 (human) Endogenous CRF agonist 1 mg 415 1605 Urocortin (rat) Endogenous CRF agonist 1 mg 415

Antagonists 2778 CRF1 antagonist 10 mg 195 50 mg 819

2071 Antisauvagine-30 Potent, selective and competitive CRF2 antagonist 1 mg 389 1606 Astressin Potent CRF 500 µg 315

2391 Astressin 2B Selective CRF2 antagonist 500 µg 385

2779 CP 154526 Selective, non-peptide CRF1 antagonist 10 mg 195 50 mg 819

3212 CP 376395 Potent and selective CRF1 antagonist 10 mg 185 50 mg 779 1184 α-helical CRF 9-41 CRF receptor antagonist 500 µg 255

2070 K 41498 Highly selective and potent CRF2 antagonist 1 mg 389

1591 NBI 27914 Selective non-peptide CRF1 antagonist 10 mg 149 50 mg 629

3100 NBI 35965 Potent and selective CRF1 antagonist 10 mg 199 50 mg 839

3294 SN 003 Potent and selective CRF1 antagonist 10 mg 189 Other 1607 CRF (6-33) CRF binding protein inhibitor 1 mg 335 Gonadotropin-releasing Hormone (GnRH) Receptors Agonists 3592 Goserelin acetate GnRH receptor agonist 10 mg 155 2873 Leuprolide GnRH receptor agonist 1 mg 75 2544 Nafarelin GnRH receptor agonist 1 mg 129 Antagonists 2730 AG 045572 Selective GnRH receptor antagonist 1 mg 105 10 mg 219 3536 Cetrorelix acetate Potent GnRH antagonist 1 mg 195 2519 T 98475 GnRH receptor antagonist 1 mg 219

Highly Potent Antagonist Selective, Non-peptide CRF1 Antagonist SR 142948 Cat. No. 2309 CP 154526 Cat. No. 2779

O CO2H NH N N N N N OMe N N

N MeO O CP 154526 is a selective, non-peptide CRF1 receptor antagonist (K values are 2.7 and >10000 nM for CRF and CRF receptors SR 142948 is a potent non-peptide neurotensin (NT) receptor i 1 2 respectively). The compound blocks CRF-induced adenylate antagonist that binds with high affinity (IC = 0.32 – 3.96 nM; 50 cyclase activation (K = 3.7 nM) and attenuates activation of the K < 10 nM). The compound attenuates amphetamine-induced i i HPA axis by CRF. CP 154526 displays -like activity in hyperactivity and is orally active in vivo. the rat elevated plus-maze test, and is brain penetrant.

(Sold for research purposes under agreement from Pfizer Inc.)

4 | Peptide Hormone Receptors Anterior Pituitary Regulation – continued

Category Cat. No. Product Name Description Unit Size USD Kisspeptin Receptor Agonists 2570 Kisspeptin 10 (human) Endogenous ligand for KISS1 receptor 1 mg 279 4243 Kisspeptin 10 (rat) Endogenous ligand for KISS1 receptor 1 mg 159 Antagonists 3881 Kisspeptin 234 KISS1/GPR54 antagonist; kisspeptin 10 (Cat. No. 2570) analog 1 mg 129 Neurotensin (NT) Receptors Agonists 1998 JMV 449 Potent neurotensin receptor agonist 1 mg 105 1909 Neurotensin Endogenous and endocrine modulator 1 mg 75 Antagonists 2309 SR 142948 Highly potent neurotensin receptor antagonist 1 mg 125 10 mg 265

3721 SR 48692 Selective non-peptide NTS1 antagonist 10 mg 249 50 mg 1049 Somatostatin (sst) Receptors

Agonists 2842 BIM 23052 sst5 agonist 1 mg 195

2454 CH 275 Potent and selective sst1 receptor agonist 1 mg 249

2444 (1R,1ʹS,3ʹR/1R,1ʹR,3ʹS)-L-054,264 Potent and selective sst2 agonist 1 mg 115 10 mg 239

1979 L-803,087 Potent and selective sst4 agonist 10 mg 275

1980 L-817,818 Potent and selective sst5 agonist 10 mg 275

2440 NNC 26-9100 Selective sst4 agonist 10 mg 219

1818 Octreotide sst2, sst3 and sst5 agonist 1 mg 255 1157 Somatostatin Endogenous sst agonist; influences growth hormone release 1 mg 105 1165 Somatostatin 1-28 sst receptor agonist 500 µg 285

4639 TT 232 sst1/sst4 receptor agonist 1 mg 195 Antagonists 3493 Cyclosomatostatin Non-selective sst receptor antagonist 1 mg 169

1843 CYN 154806 Selective sst2 antagonist 1 mg 235 Ligands 1844 BIM 23056 Somatostatin receptor ligand 1 mg 219

Other 3374 Cortistatin 14 Endogenous neuropeptide; binds sst1 - sst5 and GHS-R1a 1 mg 205 Thyrotropin-releasing Hormone (TRH) Receptors Agonists 2672 Synthetic thyrotropin-releasing hormone analog 1 mg 105 10 mg 219

Key Products for Anterior Pituitary Regulation H N

N O H O N N N H D-Phe-His-Leu-Leu-Arg-Lys-Met-Ile-Glu-Ile- N O NH Glu-Lys-Gln-Glu-Lys-Glu-Lys-Gln-Gln-Ala- O 2 D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-ol Ala-Asn-Asn-Arg-Leu-Leu-Leu-Asp-Thr-Ile-NH2 O

Octreotide (1818) Taltirelin (2672) Antisauvagine-30 (2071)

sst2, sst3 and sst5 agonist Synthetic TRH analog Potent, selective and competitive CRF2 antagonist

www.tocris.com | 5 Tocris Product Listing Series Blood Pressure Regulation Blood pressure may vary in response to factors such as diet, exercise and . Key hormones that regulate this response include angiotensin, endothelin and vasopressin. Feedback of the -angiotensin system to the prompts the release of vasopressin, increasing blood pressure.

Category Cat. No. Product Name Description Unit Size USD Angiotensin (AT) Receptors Agonists 1562 Angiotensin (1-7) Vasorelaxant peptide 1 mg 65 1563 Angiotensin I (human, mouse, rat) Endogenous precursor to angiotensin II (Cat. No. 1158) 1 mg 75 1158 Angiotensin II Potent vasoconstrictor peptide 5 mg 115

Antagonists 4553 Azilsartan Potent AT1 receptor inverse agonist; antihypertensive 10 mg 165 50 mg 695

4792 Candesartan cilexetil Prodrug of candesartan (Cat. No. 4791), an AT1 receptor 10 mg 69 antagonist 50 mg 295

1849 EMD 66684 Potent, selective non-peptide AT1 antagonist 10 mg 195 50 mg 819

4696 Eprosartan Potent and selective AT1 receptor antagonist 10 mg 59 50 mg 249

3798 Losartan Selective, non-peptide AT1 antagonist 50 mg 105

4616 Olmesartan Potent AT1 antagonist 50 mg 105

1361 PD 123319 Potent, selective non-peptide AT2 antagonist 10 mg 195 50 mg 819

4216 Valsartan High affinity, selective AT1 antagonist 10 mg 189 50 mg 795

1211 ZD 7155 Selective non-peptide AT1 antagonist 10 mg 169 50 mg 715

Ligands 2569 CGP 42112 Selective, high affinity AT2 ligand 1 mg 169

Key Products for Angiotensin and Apelin Receptors

O

N Ph2HC N N NH N HO2C Et N O N N

NMe2 N

Me Et

PD 123319 (1361) ZD 7155 (1211) N Potent, selective non-peptide AT2 antagonist Selective non-peptide AT1 antagonist

S N O O

O O pGlu-Arg-Pro-Arg-Leu-Ser-His-Lys-Gly-Pro- O2N Met-Pro-Phe

ML 221 (4748) [Pyr1]-Apelin-13 (2420) antagonist Potent peptide agonist for apelin receptor

6 | Peptide Hormone Receptors Blood Pressure Regulation – continued

Category Cat. No. Product Name Description Unit Size USD Apelin (APJ) Receptors Agonists 2420 [Pyr1]-Apelin-13 Potent peptide agonist for APJ receptor 1 mg 169 3007 Apelin-17 (human, bovine) Endogenous APJ receptor agonist 1 mg 235 2426 Apelin-36 (human) Endogenous APJ receptor agonist 1 mg 415 2427 Apelin-36 (rat, mouse) Endogenous APJ receptor agonist 1 mg 415 Antagonists 4748 ML 221 APJ receptor antagonist 10 mg 185 50 mg 779 Bradykinin Receptors

Agonists 3004 Bradykinin Endogenous agonist at bradykinin receptors (B2 > B1) 5 mg 79 9 3005 [Des-Arg ]-Bradykinin agonist (B1 > B2) 5 mg 59 8 9 3229 [Phe Ψ(CH-NH)Arg ]-Bradykinin Selective B2 agonist 1 mg 205

3227 Lys-Bradykinin Potent bradykinin receptor agonist (B2 > B1) 1 mg 75 9 3225 Lys-[Des-Arg ]Bradykinin Selective B1 agonist 1 mg 75 8 9 3230 Sar-[D-Phe ]-des-Arg -Bradykinin Potent and selective B1 agonist 1 mg 195

Antagonists 3014 HOE 140 Potent and selective B2 antagonist 500 µg 195

3978 MEN 11270 Selective B2 antagonist; analog of HOE 140 (Cat. No. 3014) 500 µg 325 1697 Noscapine Bradykinin antagonist. Also tubulin inhibitor 100 mg 95

3407 R 715 Potent and selective B1 antagonist 1 mg 205

3226 R 892 Potent and selective B1 antagonist 1 mg 205

1057 WIN 64338 Bradykinin B2 antagonist 10 mg 185 50 mg 779 Other 2370 Bombinakinin-GAP Bioactive, bradykinin-related peptide 1 mg 205 Calcitonin Gene-related Peptide (CGRP) Receptor Agonists 3012 α-CGRP (human) CGRP receptor agonist 1 mg 405 Antagonists 4561 BIBN 4096 Potent and selective CGRP receptor antagonist 10 mg 285

1181 CGRP 8-37 (human) CGRP1 receptor antagonist 500 µg 285

1169 CGRP 8-37 (rat) CGRP1 receptor antagonist 500 µg 295

4314 SB 268262 Selective non-peptide CGRP1 antagonist 10 mg 219 50 mg 925 Endothelin (ET) Receptors

Agonists 1189 BQ-3020 Selective ETB agonist 500 µg 219 1160 (human, porcine) Potent vasoconstrictor peptide 100 µg 179

1164 (human) ETA/ETB agonist 100 µg 179 1162 (human, rat) Potent vasoconstrictor 100 µg 179

1175 S6c Selective ETB agonist 100 µg 179

Antagonists 1441 BMS 182874 Highly selective, orally active non-peptide ETA antagonist 10 mg 195 50 mg 819

1188 BQ-123 Selective ETA antagonist 500 µg 169

1500 BQ 788 Selective ETB antagonist 1 mg 305

1210 FR 139317 Highly potent, selective ETA antagonist 10 mg 215 50 mg 905

1838 IRL-2500 Potent ETB antagonist 10 mg 245 Natriuretic Peptide Receptors (NPR) Agonists 1906 Atrial natriuretic factor (1-28) Endogenous peptide regulating blood pressure 1 mg 315 (human, porcine) 1912 Atrial natriuretic factor (1-28) (rat) Endogenous peptide regulating blood pressure 1 mg 295 3522 Brain natriuretic peptide (1-32) Endogenous peptide agonist at ANP receptor A (NPR1) 1 mg 375 (human) 3520 C-type natriuretic peptide (1-22) Endogenous peptide agonist at NPR2 500 µg 185 (human, rat, swine)

www.tocris.com | 7 Tocris Product Listing Series

Category Cat. No. Product Name Description Unit Size USD Tachykinin (NK) Receptors

Agonists 1668 GR 64349 Potent, selective NK2 agonist 1 mg 345

1669 GR 73632 Potent, selective NK1 agonist 1 mg 315

1535 Hemokinin 1 (mouse) Endogenous, high affinity, selective NK1 agonist 1 mg 205 8 1640 [bAla ]-(4-10) NK2 agonist 1 mg 205 1152 Neurokinin A (porcine) Endogenous tachykinin peptide 1 mg 145 1582 (human, porcine) Endogenous tachykinin peptide 1 mg 169 5 9 10 3228 [Lys ,MeLeu ,Nle ]-NKA(4-10) Selective NK2 agonist 1 mg 195

1068 Senktide Tachykinin NK3 agonist 500 µg 115 9 11 1178 [Sar ,Met(O2) ]- Potent, selective NK1 agonist 1 mg 145 1156 Substance P Sensory neuropeptide, inflammatory mediator 5 mg 139 Antagonists 1954 Antagonist G Broad spectrum antagonist 1 mg 169

2893 CP 96345 Potent and selective NK1 antagonist 10 mg 199 50 mg 839

2400 FK 888 High affinity NK1 receptor antagonist 10 mg 275

1274 GR 159897 Non-peptide, potent NK2 antagonist 10 mg 195 50 mg 819

1667 GR 94800 Potent, selective NK2 antagonist 1 mg 399

0868 L-732,138 Potent, selective NK1 antagonist 10 mg 89 50 mg 339

1145 L-733,060 Potent NK1 antagonist 10 mg 195 50 mg 819

4013 L 760735 High affinity NK1 receptor antagonist 10 mg 219 50 mg 925

1635 RP 67580 Potent and selective NK1 antagonist 10 mg 195 50 mg 819

1376 SB 218795 Potent, selective non-peptide NK3 antagonist 10 mg 195 50 mg 819

1393 SB 222200 Potent, selective non-peptide NK3 antagonist. Brain penetrant 10 mg 185 50 mg 779

4012 SR 140333 Potent NK1 receptor antagonist 10 mg 249 50 mg 1049 1946 [D-Arg1,D-Phe5,D-Trp7,9,Leu11]- Substance P analog and broad spectrum neuropeptide receptor 1 mg 139 Substance P antagonist/inverse agonist

Potent and Selective CGRP Receptor Antagonist Potent and Selective B2 Antagonist BIBN 4096 Cat. No. 4561 HOE 140 Cat. No. 3014

HN D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg N O

NH2 HOE 140 is a potent and selective bradykinin B2 receptor N antagonist (pA2 = 9.04). The compound also inhibits O aminopeptidase N (Ki = 9.1 µM). Br HN HN N N N HO O O

Br

BIBN 4096 is a potent and selective CGRP receptor antagonist

(IC50 values are 0.03 and 6.4 nM for human and rat CGRP receptors respectively). The compound displays high affinity for

human CGRP receptors (Ki = 14.4 pM) but exhibits no significant affinity against a panel of 75 other receptors.

8 | Peptide Hormone Receptors Blood Pressure Regulation – continued

Key Products for Endothelin and Natriuretic Peptide Receptors

O NaO2C MeO

N O NH Me O Cys-Ser-Cys-Ser-Ser-Leu-Met-Asp-Lys-Glu- H N N N Cys-Val-Tyr-Phe-Cys-His-Leu-Asp-lle-Ile-Trp H O Me Me3C

Endothelin 1 (human, porcine) (1160) BQ 788 (1500)

Potent vasoconstrictor peptide Selective ETB antagonist

Ser-Pro-Lys-Met-Val-Gln-Gly-Ser-Gly-Cys- Ser-Leu-Arg-Arg-Ser-Ser-Cys-Phe-Gly-Gly- Phe-Gly-Arg-Lys-Met-Asp-Arg-Ile-Ser-Ser- Arg-Met-Asp-Arg-Ile-Gly-Ala-Gln-Ser-Gly- Leu-Gly-Cys-Asn-Ser-Phe-Arg-Tyr Ser-Ser-Gly-Lys-Gly-Cys-Lys-Val-Leu-Arg- Arg-His

Atrial natriuretic factor (1-28) (human, porcine) (1906) Brain natriuretic peptide (1-32) (human) (3522) Endogenous peptide regulating blood pressure Endogenous peptide agonist at ANP receptor A (NPR1)

Category Cat. No. Product Name Description Unit Size USD Urotensin-II (UT) Receptor Agonists 1642 Urotensin-II (human) Endogenous vasoactive agonist for the urotensin-II receptor 1 mg 255 Antagonists 4670 SB 611812 Urotensin-II receptor antagonist; attenuates cardiac dysfunction 10 mg 185 50 mg 779 3571 SB 657510 Selective urotensin-II receptor antagonist 10 mg 189 50 mg 795 2529 UFP 803 Urotensin-II receptor antagonist 1 mg 205 3162 [Orn5]-URP Urotensin-II receptor antagonist 1 mg 185 Vasopressin Receptors

Agonists 3396 Desmopressin Synthetic vasopressin analog; V1B and V2 agonist 1 mg 105 2935 [Arg8]-Vasopressin Antidiuretic hormone 1 mg 75 4 8 3127 d[Leu ,Lys ]-VP Selective V1B agonist 1 mg 285

Antagonists 3924 OPC 21268 Orally active vasopressin V1 antagonist 10 mg 219 50 mg 925

2310 SR 49059 Selective, orally active vasopressin V1A receptor antagonist 10 mg 315 1 2 8 3377 (d(CH2)5 ,Tyr(Me) ,Arg )- Selective vasopressin V1A antagonist 1 mg 129 Vasopressin

Key Products for Tachykinin and Vasopressin Receptors

Arg-Pro-Lys-Pro-Gln-Gln-Phe Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Arg-Gly-NH -Phe-Gly-Leu-Met-NH2 2

Substance P (1156) [Arg8]-Vasopressin (2935) O NH2 Cl O Sensory neuropeptide, inflammatory mediator Antidiuretic hormone OH Cl N CF3 O N S O O CF3

N OMe H OMe

SR 49059 (2310) L-733,060 (1145) Selective, orally active vasopressin

Potent NK1 antagonist V1A receptor antagonist

www.tocris.com | 9 Tocris Product Listing Series Feeding and Appetite Regulation Feeding and appetite modulation are key targets in antiobesity research. In particular, leptin, ghrelin and orexin sense and regulate energy levels in the body. Other appetite-regulating peptides include opioids, which stimulate feeding. Gastrointestinal hormones such as cholecystokinin influence following food intake.

Category Cat. No. Product Name Description Unit Size USD Bombesin (BB) Receptors Agonists 2716 BIM 187 Bombesin/GRP receptor agonist 1 mg 185 1149 Bombesin agonist; involved in 1 mg 105 function 1789 GRP (human) Endogenous GRP receptor agonist 1 mg 255 1788 GRP (porcine) Endogenous GRP receptor agonist 1 mg 219 1908 (porcine) Mammalian bombesin-like peptide 1 mg 129 Antagonists 2717 BIM 189 Bombesin receptor antagonist 1 mg 185

3237 BIM 23042 Selective BB1 receptor antagonist 1 mg 129

2602 PD 176252 BB2 and BB1 receptor antagonist 10 mg 265 CART Other 3339 CART (62-76) (rat, human) Neuromodulating neuropeptide fragment; inhibits food intake 1 mg 195 in vivo 3338 CART (55-102) (human) Neuromodulatory neuropeptide fragment; satiety factor 100 µg 229 3337 CART (55-102) (rat) Neuromodulatory neuropeptide fragment; satiety factor 100 µg 259 Cholecystokinin (CCK) Receptors

Agonists 2411 A-71623 Potent and selective CCK1 agonist. Suppresses feeding 1 mg 259 1150 CCK octapeptide, non-sulfated Non-sulfated form of CCK octapeptide (Cat. No. 1166) 1 mg 129 1166 CCK octapeptide, sulfated C-terminal octapeptide of CCK 1 mg 255

3006 I (human) Selective CCK2 agonist 1 mg 285

Antagonists 2607 CI 988 Potent and selective CCK2 antagonist 10 mg 265 50 mg 1115

2304 Selective, orally active CCK1 receptor antagonist 10 mg 229 50 mg 965

2767 L-365,260 Selective CCK2 antagonist 10 mg 219 50 mg 925

1524 LY 288513 Selective CCK2 antagonist 10 mg 275 50 mg 1155

Key Products for CCK, Galanin and Ghrelin Receptors

O Me H t-Bu N HN O O NH O H N N NH H N N O N H O NH Me O Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu- O Leu-Gly-Pro-His-Ala-Ile-Asp-Asn-His-Arg- HO2C N NH2 Ser-Phe-Ser-Asp-Lys-His-Gly-Leu-Thr-NH2 O

Devazepide (2304) A-71623 (2411) Galanin (1-29) (rat, mouse) (2696)

Selective, orally active CCK1 antagonist Potent and selective CCK1 agonist; Non-selective agonist suppresses feeding

F N nOctanoyl

N N Gly-Ser-Ser-Phe-Leu-Ser-Pro-Glu-His-Gln- O Lys-Ala-Gln-Gln-Arg-Lys-Glu-Ser-Lys-Lys- His-D-Trp-D-Lys-Trp-D-Phe-Lys-NH2 Pro-Pro-Ala-Lys-Leu-Gln-Pro-Arg O

[D-Lys3]-GHRP-6 (1922) YIL 781 (3959) Ghrelin (rat) (1465) Ghrelin receptor antagonist Ghrelin receptor antagonist Endogenous ghrelin receptor agonist

10 | Peptide Hormone Receptors Feeding and Appetite Regulation – continued

Category Cat. No. Product Name Description Unit Size USD

Antagonists 2608 PD 135158 Potent and selective CCK2 antagonist 10 mg 249 50 mg 1049 1478 Non-selective CCK antagonist; orally active 50 mg 59

2190 SR 27897 Potent and selective CCK1 antagonist 10 mg 195 50 mg 819

1408 YM 022 Highly potent, selective non-peptide CCK2 antagonist 10 mg 185 50 mg 779 Galanin (GAL) Receptors

Agonists 2699 AR-M 1896 GAL2 agonist 1 mg 249 2696 Galanin (1-29) (rat, mouse) Non-selective galanin receptor agonist 1 mg 205 1179 Galanin (1-30) (human) Endogenous galanin receptor agonist 200 µg 185

1451 Galanin (2-29) (rat) Selective GAL2 peptide agonist 1 mg 399 2085 Non-selective galanin receptor agonist 10 mg 129

3629 M 1145 Potent and selective GAL2 agonist 500 µg 295

2697 M617 Selective GAL1 agonist 1 mg 285 Antagonists 3425 M40 Potent, non-selective galanin receptor antagonist 1 mg 195

2698 M871 Selective GAL2 antagonist 1 mg 285 Ghrelin & Ghrelin-related Receptors Agonists 1463 Ghrelin (human) Endogenous ghrelin receptor agonist 1 mg 389 1465 Ghrelin (rat) Endogenous ghrelin receptor agonist 1 mg 425 2261 L-692,585 Potent, non-peptide ghrelin receptor agonist 10 mg 265 2308 Tabimorelin Potent, orally active ghrelin receptor agonist 10 mg 315 Antagonists 3033 Cortistatin-8 Ghrelin receptor antagonist 1 mg 195 1922 [D-Lys3]-GHRP-6 Ghrelin receptor antagonist 5 mg 129 1946 [D-Arg1,D-Phe5,D-Trp7,9,Leu11]- Potent ghrelin receptor full inverse agonist. Also antagonist at 1 mg 139 Substance P other neuropeptide receptors 3959 YIL 781 Ghrelin receptor antagonist 10 mg 205 50 mg 865

Other 3374 Cortistatin 14 Endogenous neuropeptide; binds ghrelin receptor and sst1 - sst5 1 mg 205 2260 [Des-octanoyl]-Ghrelin (human) Major circulating form of ghrelin; devoid of activity at ghrelin 1 mg 219 receptor but is active in vivo 2951 [Des-octanoyl]-Ghrelin (rat) Major circulating form of ghrelin; devoid of activity at ghrelin 1 mg 255 receptor 2445 (rat) Endogenous anorexigenic peptide 1mg 75

Standard k Selective Antagonist Highly Potent and Selective OX2 Antagonist nor-Binaltorphimine Cat. No. 0347 EMPA Cat. No. 4558

OMe

N N

N N O OH HO N N S O O

O N O HO OH H EMPA is a highly potent, selective OX2 receptor antagonist (IC50 values are 2.3 and 1900 nM for OX2 and OX1 respectively). The nor-Binaltorphimine is a selective k antagonist compound displays negligible or no inhibition of a panel of 80 that reduces food intake induced by food deprivation and receptors. EMPA blocks orexin-B and orexin-A-invoked opioid receptor agonists. The compound reduces meal size and mobilization in hOX2-expressing CHO cells (IC50 values are 7.9 frequency, increases energy expenditure and improves satiation in and 8.8 nM respectively); it also reverses orexin-B-induced obese Zucker rats. hyperlocomotion in mice. EMPA is brain penetrant.

(Sold with the permission of the University of Minnesota)

www.tocris.com | 11 Tocris Product Listing Series

Category Cat. No. Product Name Description Unit Size USD GPR103 (QRFP Receptor) Ligands 4402 26RFa Ligand of GPR103; orexigenic neuropeptide 1 mg 195 Leptin Receptors Other 2985 LEP (116-130) (mouse) Synthetic leptin peptide fragment 1 mg 205 Melanin-concentrating Hormone (MCH) Receptors Agonists 3434 [Ala17]-MCH Potent, MCH receptor agonist 1 mg 219 3806 MCH (human, mouse, rat) Potent endogenous MCH agonist 100 µg 79

Antagonists 3359 ATC 0065 Potent and selective MCH1 antagonist 10 mg 199 50 mg 839

3346 ATC 0175 MCH1 antagonist; also 5-HT2B antagonist and 5-HT1A partial 10 mg 199 agonist 50 mg 839

4242 GW 803430 MCH1 antagonist 10 mg 219 50 mg 925

3347 SNAP 94847 Potent and selective MCH1 antagonist 10 mg 195 50 mg 819

4365 TC-MCH 7c Selective MCH1 antagonist 10 mg 249 Melanocortin (MC) Receptors

Agonists 3492 ACTH (1-39) Potent endogenous MC2 agonist 1 mg 335

4053 BMS 470539 Potent, selective MC1 receptor agonist 10 mg 229 50 mg 965 2566 Melanotan II High affinity agonist 1 mg 139 2584 α-MSH Endogenous melanocortin receptor agonist 1 mg 75 3013 [Nle4,D-Phe7]-α-MSH Melanocortin receptor agonist 1 mg 159 8 4272 [D-Trp ]-γ-MSH Selective MC3 receptor agonist 1 mg 159

3032 THIQ Potent and selective MC4 receptor agonist 1 mg 219

Antagonists 1831 HS 014 Selective MC4 receptor antagonist 1 mg 305

1832 HS 024 Highly potent MC4 receptor antagonist 1 mg 305

3438 MCL 0020 Selective MC4 receptor antagonist 1 mg 205

Other 3420 SHU 9119 MC3 and MC4 antagonist, MC5 partial agonist 1 mg 129 Motilin Receptors Other 2264 Motilin (human, porcine) Endogenous peptide regulator of gastrointestinal motility 1 mg 285 Neuromedin U (NMU) Receptors

Agonists 3648 (rat) Potent, endogenous NMU1 and NMU2 agonist 500 µg 295 1917 Neuromedin U (rat) Endogenous modulator of blood pressure and flow, gut ion 1 mg 205 transport, feeding and body temperature Neuropeptide B/W (NPBW) Receptors Agonists 3009 Neuropeptide W-23 (human) Endogenous NPBW1 and NPBW2 receptor agonist 1mg 255

Key Products for Melanocortin and Orexin Receptors

Tyr-Val-Met-Gly-His-Phe-Arg-D-Trp-Asp-Arg- Ac-Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys-Pro- Phe-Gly Pro-Lys-Asp-NH2

[D-Trp8]-γ-MSH (4272) HS 014 (1831)

Selective MC3 receptor agonist Selective MC4 receptor antagonist

OMe pGlu-Pro-Leu-Pro-Asp-Cys-Cys-Arg-Gln-Lys-

N Thr-Cys-Ser-Cys-Arg-Leu-Tyr-Glu-Leu-Leu- N OMe H His-Gly-Ala-Gly-Asn-His-Ala-Ala-Gly-Ile- N O Leu-Thr-Leu-NH2

TCS OX2 29 (3371) Orexin A (human, rat, mouse) (1455)

Potent and selective OX2 antagonist Endogenous agonist at OX1 and OX2

12 | Peptide Hormone Receptors Feeding and Appetite Regulation – continued

Category Cat. No. Product Name Description Unit Size USD Neuropeptide S Receptor Antagonists 4510 SHA 68 Selective neuropeptide S receptor antagonist 10 mg 185 50 mg 779 Neuropeptide Y (NPY) Receptors

Agonists 2035 BWX 46 Highly selective NPY Y5 agonist 1 mg 219

1177 Neuropeptide Y 13-36 (porcine) NPY Y2 receptor agonist 500 µg 195 31 34 1176 [Leu ,Pro ]-Neuropeptide Y NPY Y1 receptor agonist 200 µg 139 (human, rat) 1153 Neuropeptide Y (human, rat) Influences feeding and sexual behavior 200 µg 139 31 34 1168 [Leu ,Pro ]-Neuropeptide Y NPY Y1 receptor agonist 200 µg 169 (porcine) 1173 Neuropeptide Y (porcine) Influences feeding and sexual behavior 200 µg 185

1154 (human) NPY Y4 agonist; involved in gastrointestinal tract function 200 µg 169 1-7 19-23 31 32 34 1365 [cPP ,NPY ,Ala ,Aib ,Gln ]- Potent, selective NPY Y5 agonist 1 mg 435 hPancreatic Polypeptide

1618 Peptide YY (3-36) Selective NPY Y2 receptor agonist 500 µg 185

Antagonists 2412 BIBO 3304 Highly selective NPY Y1 receptor antagonist 10 mg 289 50 mg 1215

2707 BIBP 3226 Mixed NPY Y1 and NPFF receptor antagonist 1 mg 129 10 mg 275

1700 BIIE 0246 Potent, selective non-peptide NPY Y2 receptor antagonist 1 mg 145 10 mg 305

3242 BMS 193885 Potent, competitive NPY Y1 receptor antagonist 10 mg 229 50 mg 965

2199 CGP 71683 Highly selective and potent non-peptide NPY Y5 receptor 10 mg 195 antagonist 50 mg 819

4606 CYM 9484 Potent NPY Y2 receptor antagonist 10 mg 185 50 mg 779

4018 JNJ 5207787 Selective NPY Y2 receptor antagonist 10 mg 245 50 mg 1029

1382 L-152,804 Potent, selective non-peptide NPY Y5 receptor antagonist 10 mg 195 50 mg 819

3562 LU AA33810 Potent NPY Y5 receptor antagonist 10 mg 155 50 mg 655

3677 NPY 5RA972 Potent and selective NPY Y5 antagonist 10 mg 185 50 mg 779

2200 PD 160170 Selective non-peptide NPY Y1 receptor antagonist 10 mg 165 50 mg 695

3898 SF 11 NPY Y2 receptor antagonist 10 mg 195 50 mg 819

Key Products for Neuropeptide Y Receptors H2N NH

HN

O O O NH O N N N H N NH2 H H N HN HN O O Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu- HN HN NH N 2 Asp-Ala-Pro-Ala-Glu-Asp-Met-Ala-Arg-Tyr- N Tyr-Ser-Ala-Leu-Arg-His-Tyr-Ile-Asn-Leu- O N O O Leu-Thr-Arg-Pro-Arg-Tyr-NH2

BIBO 3304 (2412) [Leu31,Pro34]-Neuropeptide Y BIIE 0246 (1700)

Highly selective NPY Y1 (human, rat) (1176) Potent, selective non-peptide

receptor antagonist NPY Y1 receptor agonist NPY Y2 receptor antagonist

www.tocris.com | 13 Tocris Product Listing Series Feeding and Appetite Regulation – continued

Category Cat. No. Product Name Description Unit Size USD Opioid Receptors Agonists 4335 AR-M 1000390 Low-internalizing δ opioid receptor agonist 10 mg 165 50 mg 695 3790 DADLE Prototypical δ agonist 5 mg 95 1171 DAMGO Selective m agonist 1 mg 75 4591 Deltorphin 1 Potent δ agonist 1 mg 95 1431 DPDPE Selective δ agonist 1 mg 115 3195 A Endogenous k agonist 1 mg 205 3196 Endogenous k agonist 1 mg 205 1055 -1 Potent and selective m agonist 5 mg 115 0910 Endogenous NOP agonist 1 mg 139 3240 SCH 221510 Potent and selective NOP agonist 10 mg 195 50 mg 819 0764 SNC 80 Highly selective, non-peptide δ agonist 10 mg 195 50 mg 819 Antagonists 0347 nor-Binaltorphimine Standard k-selective antagonist 10 mg 155 50 mg 655 0740 Naltrindole δ-selective non-peptide antagonist 10 mg 135 50 mg 559 Orexin Receptors

Agonists 1455 Orexin A (human, rat, mouse) Endogenous agonist at OX1 and OX2 500 µg 465

1456 Orexin B (human) Endogenous agonist at OX1 and OX2 500 µg 275 11 15 2142 [Ala ,D-Leu ]-Orexin B Potent, selective OX2 receptor agonist 1 mg 315

Antagonists 4558 EMPA Highly potent and selective OX2 antagonist; brain penetrant 10 mg 209 50 mg 879

4317 JNJ 10397049 Selective OX2 receptor antagonist 10 mg 195 50 mg 819

1960 SB 334867 Selective non-peptide OX1 antagonist 1 mg 95 10 mg 195 50 mg 819

1963 SB 408124 Selective non-peptide OX1 antagonist 10 mg 239

3818 TCS 1102 Potent antagonist of OX1 and OX2 10 mg 155 50 mg 655

3371 TCS OX2 29 Potent and selective OX2 antagonist 10 mg 195 50 mg 819 VIP and PACAP Receptors

Agonists 2711 Bay 55-9837 Potent and selective VPAC2 agonist 1 mg 325 1183 PACAP 1-27 Potent stimulator of 100 µg 139 1186 PACAP 1-38 Potent stimulator of adenylyl cyclase 100 µg 179 2080 PHM 27 (human) Endogenous peptide product of human prepro-VIP 1 mg 205 11,22,28 1386 [Ala ]VIP Potent, highly selective VPAC1 agonist 1 mg 399 1911 VIP (human, rat, mouse, rabbit, Involved in neurotransmission, relaxation 1 mg 169 canine, porcine) Antagonists 1172 [Ac-Tyr1,D-Phe2]GRF 1-29, VIP antagonist 500 µg 185 (human)

3236 PACAP 6-38 Potent PAC1 receptor antagonist 100 µg 145 3054 [D-p-Cl-Phe6,Leu17]-VIP Selective VIP receptor antagonist 1 mg 259 1905 VIP (6-28) (human, rat, porcine, VIP antagonist 1 mg 255 bovine)

14 | Peptide Hormone Receptors Glucose Regulation Glucose homeostasis is vital for maintaining a sufficient level of glucose in the body, whilst preventing the serious clinical outcomes associated with hyperglycemia, as observed in . Regulatory peptides involved in glucose homeostasis, such as insulin and glucagon-like peptide 1 (GLP-1), and their receptors are key therapeutic targets in diabetes research.

Category Cat. No. Product Name Description Unit Size USD Amylin Receptor Agonists 3418 Amylin Endogenous peptide agonist for amylin, calcitonin, CGRP and 500 µg 235 receptors Antagonists 3419 AC 187 Potent and selective amylin receptor antagonist 500 µg 295 Gastric Inhibitory Polypeptide (GIP) Receptor Agonists 2257 GIP (1-39) Highly potent insulinotropic peptide 1 mg 339 2084 GIP (human) Potent insulinotropic gut hormone 1 mg 389 Antagonists 2216 des-His1-[Glu9]-Glucagon (1-29) Glucagon receptor antagonist 1 mg 285 amide 2311 L-168,049 Potent, orally active human glucagon receptor antagonist 10 mg 155 50 mg 655 Glucagon-like Peptide 1 (GLP-1) Receptor Agonists 1933 Exendin-4 Potent GLP-1 receptor agonist 1 mg 339 1851 Glucagon-like peptide 1 (1-37) Endogenous pancreatic peptide 1 mg 389 (human, rat) 2082 Glucagon-like peptide 1 (7-36) Potent insulinotropic peptide 1 mg 389 amide (human, rat) Antagonists 2081 Exendin-3 (9-39) amide Potent GLP-1 receptor antagonist 1 mg 389 3266 GLP-1 (9-36) amide Metabolite of GLP-1-(7-36) (Cat. No. 2082) 1 mg 295 Other 2094 Endogenous gut peptide; modulates feeding and 1 mg 315 Glucagon-like Peptide 2 (GLP-2) Receptor Other 2258 GLP-2 (human) Endogenous hormone; displays intestinotropic activity 1 mg 265 2259 GLP-2 (rat) Endogenous hormone; displays intestinotropic activity 1 mg 265 Insulin Receptor Activators 1819 Demethylasterriquinone B1 Selective insulin RTK activator 5 mg 219 Agonists 3435 Insulin (human) recombinant, Endogenous insulin receptor peptide agonist 10 mg 75 expressed in yeast Insulin-like Growth Factor 1 Receptor (IGF1R) Inhibitors 2956 Picropodophyllotoxin Selective IGF1R inhibitor 10 mg 195 2768 PQ 401 IGF1R inhibitor 10 mg 145 50 mg 609

Key Products for Glucagon and Related Receptors

His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu- Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu- Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg- Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu- Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly- Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala- Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2 Pro-Pro-Pro-Ser-NH2 OH H Exendin-4 (1933) Exendin-3 (9-39) amide (2081) O Potent GLP-1 receptor agonist Potent GLP-1 receptor antagonist O O H O

His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val- Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys- MeO OMe Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-NH2 OMe

Glucagon-like peptide 1 (7-36) amide (human, rat) (2082) Picropodophyllotoxin (2956) Potent insulinotropic peptide Selective IGF1R inhibitor

www.tocris.com | 15 Tocris Product Listing Series Other Peptide Hormones Numerous processes are influenced by peptide hormones, including calcium regulation (calcitonin and parathyroid hormone), uterine contraction (oxytocin) and nociception (neuropeptide FF). Regulation of calcium homeostasis is of particular importance in .

Category Cat. No. Product Name Description Unit Size USD Calcitonin Receptor Agonists 1161 CGRP (rat) Potent vasodilator 100 µg 135 2550 SUN-B 8155 Non-peptide calcitonin receptor agonist 10 mg 155 50 mg 655 Neuropeptide FF/AF (NPFF) Receptors

Agonists 3137 Neuropeptide FF Endogenous NPFF1 and NPFF2 agonist 1 mg 135

4683 RFRP 3 (human) NPFF1 agonist; GnIH homolog 1 mg 135

Antagonists 2707 BIBP 3226 Mixed NPFF and NPY Y1 receptor antagonist 1 mg 129 10 mg 275

3672 RF 9 Selective NPFF1 and NPFF2 antagonist 1 mg 105

Ligands 1486 GR 231118 NPFF receptor ligand. Also NPY Y1 antagonist/NPY Y4 agonist 500 µg 339 Agonists 4852 Carbetocin Oxytocin analog 10 mg 149 1910 Oxytocin Involved in uterine contraction and lactation 1 mg 75 3933 WAY 267464 Potent, non-peptide oxytocin receptor agonist 10 mg 239 Antagonists 2641 L-368,899 Potent, non-peptide oxytocin receptor antagonist 1 mg 135 10 mg 289 2410 L-371,257 Potent and selective oxytocin receptor antagonist 10 mg 219 Parathyroid Hormone Receptors Agonists 3011 Parathyroid hormone (1-34) (human) Parathyroid agonist 1 mg 305

Key Products for Oxytocin Receptors

O S O N

N HN HO S NH2 O O O N N L-368,899 (2641) N Potent, non-peptide oxytocin receptor antagonist HO NH N NH N O Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH2 O

Oxytocin (1910) WAY 267464 (3933) Involved in uterine contraction and lactation Potent, non-peptide oxytocin receptor agonist

16 | Peptide Hormone Receptors Peptide Hormone Processing Peptide hormone signaling is modulated by various proteases that metabolize peptide hormones. Examples include: dipeptidyl peptidase IV, which degrades glucagon-like peptide 1 thereby curbing insulin secretion; and angiotensin- converting enzyme, which catalyzes the conversion of angiotensin I to angiotensin II.

Category Cat. No. Product Name Description Unit Size USD Angiotensin-converting Enzyme (ACE) Inhibitors 2578 Benazepril ACE inhibitor 50 mg 129

4455 Captopril ACE inhibitor; also inhibits LTA4 hydrolase 50 mg 59 2691 Moexipril ACE inhibitor 10 mg 139 50 mg 585 4302 Perindopril ACE inhibitor 50 mg 115 2931 -degrading and ACE inhibitor 1 mg 129 Substrates 1563 Angiotensin I (human, mouse, rat) Endogenous peptide substrate of ACE 1 mg 75 1764 (rat) Bioactive substrate for endopeptidase 24.15, neurolysin and ACE 1 mg 325 Chymase Substrates 3841 RETF-4NA Selective chymase substrate 1 mg 155 Dipeptidyl Peptidase IV (DPP-IV) Inhibitors 2783 DPPI 1c Dipeptidyl peptidase IV inhibitor 1 mg 105 10 mg 219 2790 K 579 Dipeptidyl peptidase IV inhibitor 10 mg 219 50 mg 925 3506 NVP DPP 728 Potent, orally active dipeptidyl peptidase IV inhibitor 10 mg 195 50 mg 819 4145 PK 44 Potent and selective dipeptidyl peptidase IV inhibitor 10 mg 285 Endothelin-converting Enzyme (ECE) Inhibitors 2512 CGS 35066 Endothelin-converting 10 mg 249 Neurotensin-degrading Enzymes Inhibitors 2575 JMV 390-1 Inhibits multiple neurotensin and degrading 1 mg 115 enzymes Tripeptidyl Peptidase II Inhibitors 1323 Butabindide Potent, competitive inhibitor of CCK-inactivating serine protease 10 mg 185 (tripeptidyl peptidase II) 50 mg 779

Prices are correct for 2016. For a full product listing please visit www.tocris.com

www.tocris.com | 17 Tocris Product Listing Series

Related literature from Tocris that you may be interested in:

Gut Hormones and the Regulation of Appetite V. Taylor, P. Jethwa, C. Small and S. Bloom, Imperial College London The gastrointestinal tract is the largest in the human body, secreting hormones that affect digestion, appetite and energy expenditure. Neuropeptide modulators and gut hormones that influence appetite are reviewed in this poster.

Peptides Involved in Appetite Modulation S. Tucci, L. Koblis and T. Kirkham, University of Liverpool A synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis. This review outlines the putative roles of most of the known peptides, and lists compounds available from Tocris.

Nuclear Receptors Product Listing Over 150 products for Nuclear Receptors Our new product listing contains products for key nuclear receptors including: • Androgen Receptors • Receptors • Retinoic Acid Receptors • Retinoid X Receptors • Receptors

Cardiovascular Research Product Guide Over 250 products for Cardiovascular Research Our new guide contains products with supporting information and figures to illustrate the relevance of each target within the areas of: • • Thrombosis and Hemostasis • Atherosclerosis • Myocardial Infarction and Ischemia/Reperfusion Injury • Arrhythmias • Heart Failure

Seven-Transmembrane Receptor Signaling T. Kenakin, GlaxoSmithKline Research and Development R. Lefkowitz and J. Violin, Duke University Medical Center Michael Bouvier and Geneviève Oligny-Longpré, Université de Montréal Seven-transmembrane (7-TM)-receptors are now recognized as complex processors of information that can bind to molecules and cytosolic interactants on the cell membrane. The 7-TM poster highlights the multiple behaviours of 7-TMs including G-protein-dependent and -independent signaling as well as the concept of collateral efficacy.

To download or request copies, please visit www.tocris.com/requestliterature

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