Vasoactive Intestinal Peptide GPCR Family Subtypes and Products

What Are Vasoactive Intestinal Peptide Receptors?

Vasoactive intestinal peptide (VIP) receptors are a family of G protein-coupled receptors (GPCRs) comprised of three receptor subtypes: PAC1, VPAC1, and VPAC2. VIP receptors are found all throughout peripheral tissues and the brain, and are involved in a variety of biological functions, such as circadian rhythms, insulin secretion, immune response, inflammatory response, and neurodevelopment. VIP receptor agonists have shown a potential therapeutic application in the treatment of type 2 diabetes, while antagonists have potential pharmacological uses in treating autoimmune diseases and inflammatory diseases. The VPAC2 receptor has also been implicated in certain psychotic disorders, and has become a potential drug target.

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Vasoactive Intestinal Peptide Receptor Information

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PAC1

VPAC1/VPAC2

The pituitary adenylate cyclase-activating polypeptide (PACAP)- selective PAC1 receptor (PAC1R, ADCYAP1R1) is a member of the vasoactive intestinal peptide (VIP) family of G protein-coupled receptors (GPCRs). PAC1R has been shown to play crucial roles in the central and peripheral nervous systems. Inadequate PACAP/PAC1R signaling has been implicated in a number of disorders, including stress-related psychopathologies (i.e., depression, posttraumatic stress disorder, and related abnormalities), chronic pain and migraine, and metabolic diseases. Repealing PAC1R signaling under these pathological conditions represent opportunities for therapeutic intervention.

VIPR1 (Vasoactive intestinal polypeptide receptor 1) is also known as PACAP type II receptor (pituitary adenylate cyclase activating polypeptide type II receptor). It is a receptor for both vasoactive intestinal polypeptide and pituitary adenylate cyclase activating polypeptide, and therefore more popularly known as VPAC1. VIP is a neuromodulator and growth regulator in the developing nervous system. Both VIPR1 and VIPR2 are highly expressed in central primitive neuroectodermal tumors and mediate the growth modulation of VIP in these tumors. VIPR1 gene is mapped to human 3p22-p21 where loss-of-heterozygosity is observed in small-cell lung carcinoma (SCLC) cell lines and primary tumors.

Vasoactive Intestinal Peptide Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
Vasoactive Intestinal PeptidePAC1humanHEK293TC1415DC1415MC1415
VPAC1humanCHO-K1C1292-1DC1292-1MC1292-1
VPAC2humanHEK293TH1293DH1293MH1293

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