Substance P (SP) |
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Amino acids: 11
Discovered: 1931
Localization: Sensory nerves
Related mammalian neuropeptides:
Neurokinin A, neurokinin B
Related non-neural peptides:
Hemokinins, endokinins |
Receptors: NK1, NK2, NK3
Antagonists: range of nonpeptide antagonists available for each receptor
Therapeutic use: NK1 antagonist in emesis
Positive results in clinical trials: NK1 antagonist in depression |
Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2
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α-Calcitonin gene related peptide (CGRP)
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Amino acids: 37
Discovered: 1983
Related mammalian neuropeptides:
βCGRP, intermedin
Related non-neural peptides:
Adrenomedullin,
amylin |
Receptors: CGRP1, CGRP2(?), AM2 (?)
Antagonists: CGRP8–37 (peptide) BIBN4096BS (nonpeptide)
Positive results in clinical trials: BIBN4096BS in migraine |
Ala-Cys-Asp-Thr-Ala-Thr-Cys-Val-Thr-His-Arg-Leu-Ala-Gly-Leu-Leu-Ser-Arg-Ser-Gly-Gly-Val-Val-Lys-Asn-Asn-Phe-Val-Pro-Thr-Asn-Val-Gly-Ser-Lys-Ala-Phe-NH2
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Neuropeptide Y (NPY) |
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Amino acids: 36
Discovered: 1982
Localization: Sympathetic, cholinergic, sensory, enteric and central neurons
Related nonmammalian neuropeptides: PY in bony fish; NPF in D. melanogaster
Related non-neural peptides: Peptide YY (PYY), PYY(3–36) and pancreatic polypeptide (PP) |
Receptors: Y1, Y2, Y4, Y5
Antagonists: Y1 BIBO3304;
Y2 BIIE0246; Y5 L-152,804
Positive results in clinical trials: none to date; Y1 and Y5 antagonists were ineffective against obesity; PYY(3–36) is in development as an anti-obesity agent |
Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu-Asp-Ala-Pro-Ala-Glu-Asp-Met-Ala-Arg-Tyr-Tyr-Ser-Ala-Leu-Arg-His-Tyr-Ile-Asn-Leu-Ile-Thr-Arg-Gln-Arg-Tyr-NH2
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