Molecular pharmacology and structure of VPAC receptors for VIP and PACAP

VIP and PACAP are two prominent neuropeptides which share two common G protein-coupled receptors VPAC1 and VPAC2 while PACAP has an additional specific receptor PAC1. This paper reviews the present knowledge regarding three aspects of VPAC receptors including: (i) receptor specificity towards natural VIP-related peptides and pharmacology of synthetic agonists or antagonists; (ii) receptor signaling; (iii) molecular basis of ligand-receptor interaction as determined by site-directed mutagenesis, construction of receptor chimeras and structural modeling. (C) 2002 Elsevier Science B.V. All rights reserved.