Peptide Hormone Receptors Product Listing | Edition 2
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Peptide Hormone Receptors Product Listing | Edition 2 Oriental Fire-bellied Toad Bombina orientalis A source of Bombesin Products for: • Anterior Pituitary Regulation • Cardiovascular Regulation • Feeding and Appetite Regulation • Glucose Regulation • Other Peptide Hormones • Peptide Hormone 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 pituitary gland, blood pressure, feeding, appetite and blood glucose levels. A product listing of nuclear receptor compounds is also available from www.tocris.com. Anterior Pituitary Regulation ................................................4 Neuromedin U (NMU) Receptors .................................. 13 Corticotropin-releasing Factor (CRF) Receptors ............ 4 Neuropeptide B/W (NPBW) Receptors ......................... 13 Gonadotropin-releasing Hormone (GnRH) Receptors ... 4 Neuropeptide S Receptors ............................................. 13 Kisspeptin Receptors ........................................................ 5 Neuropeptide Y (NPY) Receptors .................................. 13 Neurotensin (NT) Receptors ............................................ 5 Orexin Receptors ............................................................. 14 Somatostatin (sst) Receptors ........................................... 5 Glucose Regulation ............................................................. 15 Thyrotropin-releasing Hormone (TRH) Receptors ......... 5 Amylin Receptors ............................................................. 15 Gastric Inhibitory Polypeptide (GIP) Receptors ........... 15 Cardiovascular Regulation .....................................................6 Glucagon Receptors ........................................................ 15 Angiotensin (AT) Receptors .............................................. 6 Glucagon-like Peptide 1 (GLP-1) Receptor .................. 15 Apelin (APJ) Receptors ..................................................... 6 Glucagon-like Peptide 2 (GLP-2) Receptor .................. 15 Bradykinin Receptors ........................................................ 7 Insulin and Insulin-like Receptors ................................. 15 Calcitonin and Related Receptors ................................... 7 Other Peptide Receptors .................................................... 16 Endothelin (ET) Receptors ............................................... 7 Calcitonin Receptors ....................................................... 16 Natriuretic Peptide Receptors (NPR) .............................. 8 Mas-Related G Protein-Coupled Receptors ................. 16 Tachykinin (NK) Receptors ............................................... 8 Neuropeptide FF/AF Receptors ...................................... 16 Urotensin-II (UT) Receptors ............................................. 9 Opioid Receptors ............................................................. 17 Vasopressin Receptors .................................................... 10 Oxytocin Receptors ......................................................... 17 Feeding and Appetite Regulation ..................................... 10 PACAP Receptors ............................................................ 18 Bombesin (BB) Receptors .............................................. 10 Parathyroid Hormone Receptors ................................... 18 CART ................................................................................. 10 VIP Receptors .................................................................. 18 Cholecystokinin (CCK) Receptors .................................. 10 Peptide Hormone Processing ............................................ 19 Galanin (GAL) Receptors ................................................ 11 Aminopeptidases ............................................................. 19 Ghrelin Receptors ............................................................ 11 Angiotensin-converting Enzymes (ACE) ....................... 19 GPR103 (QRFP Receptor) .............................................. 11 Chymase ........................................................................... 19 GPR171 ............................................................................ 12 Dipeptidyl Peptidase IV (DPP IV) .................................. 19 GPR83 .............................................................................. 12 Endothelin-converting Enzyme (ECE) ........................... 19 Leptin Receptors ............................................................. 12 Insulin-degrading Enzyme (ICE) .................................... 19 Melanin-concentrating Hormone (MCH) Receptors .... 12 Neurotensin-degrading Enzymes ................................... 19 Melanocortin (MC) Receptors ........................................ 12 Renin ................................................................................. 19 Motilin Receptors............................................................. 13 Tripeptidyl Peptidase II ................................................... 19 2 | PEPTIDE HORMONE RECEPTORS Introduction Most hormones are endogenous mediators secreted by endocrine glands as part of homeostasis. 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 proteins (that is, they are GPCRs). One notable exception is the insulin receptor, 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 protein 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 ligand 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 agonists and antagonists active at peptide hormone receptors. Figure 1 | Peptide receptors involved in physiological processes Liver and Pancreas Brain Glucose Regulation Anterior Pituitary Regulation Amylin Receptor CRF Receptors GIP Receptor GnRH Receptors Glucagon Receptor Kisspeptin Receptor Glucagon-like Peptide 1 Receptor Neurotensin Receptors Glucagon-like Peptide 2 Receptor Somatostatin Receptors Insulin and Insulin-like Receptors TRH Receptors Stomach and Gut Appetite & Feeding Regulation Bombesin Receptors CART CCK Receptors Galanin Receptors Ghrelin & Ghrelin-related Receptors GPR103 (QRFP Receptor) GPR171 Heart, Arteries and Kidneys GPR83 Cardiovascular Regulation Leptin Receptors Angiotensin Receptors MCH Receptors Apelin Receptors Melanocortin Receptors Bradykinin Receptors Motilin Receptors CGRP Receptor Neuromedin U Receptors Endothelin Receptors Neuropeptide B/W Receptors Natriuretic Peptide Receptors Neuropeptide S Receptor Tachykinin Receptors Neuropeptide Y Receptors Urotensin-II Receptor Orexin Receptors Vasopressin Receptors Tocris has a broad range of products for peptide hormone receptors, including small molecules and peptides. The information listed within is correct at the time of printing. For the latest information, and to request free scientific literature, please visit www.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, gonadotropin-releasing hormone and thyrotropin-releasing hormone. Stimulation by the hypothalamus influences the release of hormones from the anterior pituitary, including growth hormone, prolactin and adrenocorticotropic hormone (ACTH). Category Cat. No. Product Name Description Unit Size Corticotropin-releasing Factor Receptors Agonists 6450 Cortagine Potent and selective CRF1 agonist 100 µg 1151 CRF (human, rat) Stimulates ACTH release 200 µg 1609 Sauvagine CRF agonist 500 µg 1608 Stressin I CRF1 agonist 500 µg 1604 Urocortin (human) Endogenous CRF agonist 1 mg 1605 Urocortin (rat) Endogenous CRF agonist 1 mg Antagonists 2778 Antalarmin CRF1 antagonist 10 mg 50 mg 2071 Antisauvagine-30 Potent, selective and competitive CRF2 antagonist 1 mg 1606 Astressin Potent CRF antagonist 500 µg 2391 Astressin 2B Selective CRF2 antagonist 500 µg 2779 CP 154526 Selective, non-peptide CRF1 antagonist 10 mg 50 mg 3212 CP 376395 Potent and selective CRF1 antagonist 10 mg 50 mg 1184 α-helical CRF 9-41 CRF antagonist 500 µg 2070 K 41498 Highly selective and potent CRF2 antagonist 1 mg 1591 NBI 27914 Selective non-peptide CRF1 antagonist 10 mg 50 mg 3100 NBI 35965 Potent and selective CRF1 antagonist 10 mg 50 mg 6451 Pexacerfont Potent and selective CRF1 antagonist; anxiolytic 10 mg 50 mg 6530 R 121919 High affinity CRF1 antagonist; orally bioavailable 10 mg 50 mg 3294 SN 003 Potent and selective CRF1