PA-8 (PAC1 antagonist PA-8) is a potent, specific small molecule antagonist of PACAP type I (PAC1) receptor.
PA-8 (1 nM) significantly and dose dependently attenuated PACAP (1 nM)-induced CREB phosphorylation in the CHO cells expressing PAC1, but not CHO cells expressing VPAC1, or VPAC2 receptors.
PA-8 also dose dependently inhibited PACAP-induced cAMP elevation with an IC50 of 2 nM.
PA-8 blocked PACAP-induced aversive responses and mechanical allodynia in mice.
