VIP and PACAP receptors

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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Vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating peptide (PACAP) receptors (nomenclature recommended by the NC-IUPHAR Subcommittee on Vasoactive Intestinal Peptide Receptors, [5]) are activated by the endogenous peptides VIP (VIP, P01282), PACAP-38 (ADCYAP1, P18509), PACAP-27 (ADCYAP1, P18509), peptide histidine isoleucineamide (PHI), peptide histidine methionineamide (PHM (VIP, P01282)) and peptide histidine valine (PHV (VIP, P01282)). “PACAP type II receptors” (VPAC1 and VPAC2 receptors) display comparable affinity for PACAP and VIP (VIP, P01282), whereas PACAP-27 (ADCYAP1, P18509) and PACAP-38 (ADCYAP1, P18509) are >100 fold more potent than VIP (VIP, P01282) as agonists of most isoforms of the PAC1 receptor. However, one splice variant of the human PAC1 receptor has been reported to respond to PACAP-38 (ADCYAP1, P18509), PACAP-27 (ADCYAP1, P18509) and VIP (VIP, P01282) with comparable affinity [1]. PG 99-465 [8] has been used as a selective VPAC2 receptor antagonist in a number of physiological studies, but has been reported to have significant activity at VPAC1 and PAC1 receptors [2]. The selective PAC1 receptor agonist maxadilan, was extracted from the salivary glands of sand flies (Lutzomyia longipalpis) and has no sequence homology to VIP (VIP, P01282) or PACAP [9]. Two deletion variants of maxadilan, M65 [14] and Max.d.4 [10] have been reported to be PAC1 receptor antagonists, but these peptides have not been extensively characterised.

Receptors

PAC1 receptor Show summary » More detailed page

VPAC1 receptor Show summary » More detailed page

VPAC2 receptor Show summary » More detailed page

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation:

VIP and PACAP receptors. Accessed on 18/12/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=67.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Spedding M, Peters JA and Harmar AJ, CGTP Collaborators. (2013) The Concise Guide to PHARMACOLOGY 2013/14: G Protein-Coupled Receptors. Br J Pharmacol. 170: 1459–1581.