Description
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.1 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).2,3 In vivo, in newborn pigs, PACAP (6-38) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-38) (Item No. 24770), the full-length peptide.4 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.5WARNING This product is not for human or veterinary use.
References
[1] PHILIPPE GOURLET. Fragments of pituitary adenylate cyclase activating polypeptide discriminate between type I and II recombinant receptors[J]. European journal of pharmacology, 1995, 287 1: Pages 7-11. DOI:
10.1016/0014-2999(95)00467-5[2] O MORO. Functional characterization of structural alterations in the sequence of the vasodilatory peptide maxadilan yields a pituitary adenylate cyclase-activating peptide type 1 receptor-specific antagonist.[J]. The Journal of Biological Chemistry, 1999, 274 33: 23103-23110. DOI:
10.1074/jbc.274.33.23103[3] M. EGGENBERGER . Maxadilan interacts with receptors for pituitary adenylyl cyclase activating peptide in human SH-SY5Y and SK-N-MC neuroblastoma cells[J]. Neuropeptides, 1999, 33 2: Pages 107-114. DOI:
10.1054/npep.1999.0004[4] LAURA LENTI . Pituitary adenylate cyclase-activating polypeptide induces pial arteriolar vasodilation through cyclooxygenase-dependent and independent mechanisms in newborn pigs[J]. Brain Research, 2007, 1165: Pages 81-88. DOI:
10.1016/j.brainres.2007.06.032[5] JONATHAN R BURGOS Ulrika S Britt Marie Iresjö. Pituitary adenylate cyclase-activating polypeptide 6-38 blocks cocaine- and amphetamine-regulated transcript Peptide-induced hypophagia in rats.[J]. PLoS ONE, 2013: e72347. DOI:
10.1371/journal.pone.0072347
