PACAP (1-27) (the N-terminal fragment of PACAP-38) is a novel neuropeptides originally isolated from bovine hypothalamus, also found in humans and rats.
PACAP (6-38), human, ovine, rat, is a potent and selective antagonist of PACAP 38, outperforming PACAP (6-27) in inhibiting PACAP-27-stimulated pituitary adenylate cyclase.
Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.
PACAP (1-38), a novel neuropeptide isolated from the bovine hypothalamus is more active than vasoactive intestinal peptide (VIP) in stimulating adenylate cyclase (EC50=7 nM). PACAP 1-38 (10-9 M) increased substance P (SP), gastrin releasing peptide (GRP),
PACAP (1-27), human, ovine, rat TFA (PACAP 1-27 TFA), an N-terminal fragment of PACAP-38, is an effective PACAP receptor antagonist with IC50 values of 3 nM for rat PAC1, 2 nM for rat VPAC1, and 5 nM for human VPAC2.
PACAP (6-38), human, ovine, rat TFA is a potent PACAP receptor antagonist with IC50 values of 30 nM, 600 nM, and 40 nM for the PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2, respectively.