Vasoactive intestinal peptide receptor (specifically VPAC1 and VPAC2) (VPAC1, VPAC2)

VIP receptors (VPAC1 and VPAC2) are cell-surface G protein-coupled receptors for the 28-amino acid neuropeptide VIP. These receptors are present throughout the central and peripheral nervous systems, gastrointestinal tract, pancreas, cardiovascular system, and immune cells[1][2][3][4][5][6]. Activation of these receptors by VIP induces diverse physiological responses, including vasodilation, modulation of smooth muscle relaxation, stimulation of pancreatic and gastrointestinal secretions, immune regulation, cell proliferation, and neuroprotection. Dysregulation of VIP signaling is implicated in several disease processes such as chronic inflammation, neurodegenerative conditions, cardiovascular dysfunction, and gastrointestinal disorders. The VPAC receptors are considered viable therapeutic targets, but no approved drugs directly target them as of 2024, although several experimental compounds are available for research. Therapeutic modulation of the VIP pathway is challenged by its extensive physiologic functions and widespread tissue expression, which complicate selective targeting without side effects[1][2][3][4][6].

Other names

VPAC receptorVIP receptorVIP1 receptor (VPAC1)VIP2 receptor (VPAC2)

Agonists activate the receptor, increasing cAMP and regulating downstream signaling. Antagonists block VIP binding, inhibiting the physiological effects of VIP.