PA-8

Description: PA-8 is a small molecule receptor antagonist for PACAP Type I (PAC1) that is selective, effective, and orally active. PA-8 inhibits PacAP-induced CREB phosphorylation at PAC1- receptors, but does not inhibit VPAC1- or vpac2 receptors. PA-8 also inhibited PacAP-induced elevation of cAMP levels in vitro (IC50 = 2 nM) and PacAP-induced aversive response and mechanical atopic pain after intrathecal injection in vivo. Target: PACAP. Smiles: COc1cc(ccc1OCC=C)C1CC(=O)Nc2nc(N)[nH]c(=O)c12. References: Ichiro Takasaki, et al. In Silico Screening Identified Novel Small-molecule Antagonists of PAC1 Receptor. J Pharmacol Exp Ther. 2018 Apr,365(1):1-8.