Chemical Name: 2-Amino-5,8-dihydro-5-[3-methoxy-4-(2-propen-1-yloxy)phenyl]pyrido[2,3-d]pyrimidine-4,7(3H,6H)-dione
Biological ActivityPAC1 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
In silico screening identified novel small-molecule antagonists of PAC1 receptor.
Takasaki et al.
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