A PACAP receptor antagonist
Pituitary adenylate cyclase-activating peptide (PACAP) (6-38) is a PACAP receptor antagonist with IC50 values of 30, 600, and 40 nM, respectively for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors in rat brain membrane (IC50 = 39.14 nM) and to SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 2.9, 129, and 227 nM, respectively). In vivo, in newborn pigs, PACAP (6-38) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-38) , the full-length peptide. It also inhibits decreased food intake and reduced body weight in rats induced by cocaine- and amphetamine-regulated transcript peptides (CARTp) following intracerebroventricular administration of 0.3-3 mol per animal doses.
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