VIP and PACAP receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

  • Jan Fahrenkrug University of Copenhagen
  • Edward J. Goetzl University of California San Francisco
  • Illana Gozes Tel Aviv University
  • Anthony Harmar University of Edinburgh
  • Marc Laburthe INSERM
  • Victor May University of Vermont College of Medicine
  • Joseph R. Pisegna University of California Los Angeles
  • Sami I. Said State University of New York at Stony Brook
  • David Vaudry Normandy University
  • Hubert Vaudry Normandy University
  • James A. Waschek University of California Los Angeles https://orcid.org/0000-0003-2727-9876

Abstract


Vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating peptide (PACAP) receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Vasoactive Intestinal Peptide Receptors [64, 65]) are activated by the endogenous peptides VIP, PACAP-38, PACAP-27, peptide histidine isoleucineamide (PHI), peptide histidine methionineamide (PHM) and peptide histidine valine (PHV). VPAC1 and VPAC2 receptors display comparable affinity for the PACAP peptides, PACAP-27 and PACAP-38, and VIP, whereas PACAP-27 and PACAP-38 are >100 fold more potent than VIP 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, PACAP-27 and VIP with comparable affinity [29]. PG 99-465 [115] 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 [35]. The selective PAC1 receptor agonist maxadilan, was extracted from the salivary glands of sand flies (Lutzomyia longipalpis) and has no sequence homology to VIP or the PACAP peptides [116]. Two deletion variants of maxadilan, M65 [180] and Max.d.4 [117] have been reported to be PAC1 receptor antagonists, but these peptides have not been extensively characterised.
Published
16-Sep-2019
How to Cite
Fahrenkrug, J., Goetzl, E. J., Gozes, I., Harmar, A., Laburthe, M., May, V., Pisegna, J. R., Said, S. I., Vaudry, D., Vaudry, H. and Waschek, J. A. (2019) “VIP and PACAP receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database”, IUPHAR/BPS Guide to Pharmacology CITE, 2019(4). doi: 10.2218/gtopdb/F67/2019.4.
Section
Summaries