Vasoactive intestinal polypeptide receptor 1 and vasoactive intestinal polypeptide receptor 2 (VPAC1 and VPAC2)

Vasoactive intestinal polypeptide receptor 1 (VPAC1) and vasoactive intestinal polypeptide receptor 2 (VPAC2) are members of the class B1 family of G protein-coupled receptors, primarily activated by the endogenous neuropeptides VIP and PACAP. These receptors are widely expressed in the central and peripheral nervous systems and various peripheral tissues, where they mediate numerous physiological functions including regulation of hormone and exocrine secretion, control of circadian rhythm, immune regulation, vascular tone, growth, and development. Both play roles in diseases such as inflammatory and neurodegenerative conditions, autoimmune diseases, and some cancers. Their broad physiological relevance and potential for pharmacologic modulation make them attractive, though complex, therapeutic targets.

Other names

VPAC1 (VIP receptor 1, VIPR1)VPAC2 (VIP receptor 2, VIPR2)Vasoactive intestinal peptide receptor 1Vasoactive intestinal peptide receptor 2VIP receptor 1VIP receptor 2

Agonists (e.g., VIP, PACAP) activate adenylyl cyclase via Gs protein, increasing cAMP and protein kinase A (PKA) activity, leading to downstream gene expression and physiological effects. Antagonists block peptide binding, inhibiting receptor signaling.