PAC1 receptor antagonist. Inhibits PACAP-induced CREB phosphorylation in PAC1, but not VPAC1 or VPAC2, expressing cells. Also inhibits PACAP-induced increases in cAMP levels in vitro (IC50 = 2 nM) and PACAP-induced aversive responses and mechanical allodynia following intrathecal injection in vivo.
Takasaki et al (2018) In silico screening identified novel small-molecule antagonists of PAC1 receptor. J.Pharmacol.Exp.Ther. 365 1 PMID:29363578
















