Vasoactive intestinal polypeptide receptors are class B G protein-coupled receptors (GPCRs) and are receptors for the vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating polypeptide (PACAP). VIPs and PACAPs are members of a superfamily of structurally related peptide hormones that mediate diverse and important physiological and biological functions. VIPs and PACAPs act via three different receptors: VIPR1, VIPR2, and PAC1. PAC1 receptors are selective for PACAP, whereas VIPR1 and VIPR2 respond to both VIP and PACAP with high affinity. These receptors have been identified in various tissues, including brain, lung, kidney, gastrointestinal tract, tongue, and also on immunocompetent cells. In the CNS, these receptors function in the control of circadian rhythms, learning and memory, anxiety and responses to stress and brain injury. In the periphery, they are involved in the control of immunity and inflammation, the control of pancreatic insulin secretion, the release of catecholamines from the adrenal medulla, and as co-transmitters in autonomic and sensory neurons.
Here, we give a separate introduction and a brief summary of part of the vasoactive intestinal polypeptide receptors focusing on our current understanding of their structure, pharmacology and functions, and their likely physiological roles in health and disease.
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