PACAP Receptor Agonists

Pituitary adenylate cyclase-activating polypeptide (PACAP) receptors are G_s-protein-coupled receptors referred to as PAC₁. The endogenous ligand, PACAP, also activates the VIP receptors, VPAC₁ and VPAC₂.

PAC₁ receptors are predominantly expressed in the central nervous system, particularly in the olfactory bulb, thalamus, hypothalamus, dentate gyrus and granule cells of the cerebellum. They are also found in the adrenal medulla and pancreas. PAC₁ receptors are involved in daytime regulation of the biological clock, emotional control of behavior, anxiolysis and control of adrenal medulla catecholamine release. The human PAC₁ receptor gene has been localized to chromosome 7p14.