ACPT-I

ACPT-I is an agonist of the group III metabotropic glutamate receptors (mGluRs) mGluR4a and mGluR8 (EC50s = 7.2 and 8.2 µM, respectively) that has no effect on mGluR1a or mGluR2.{5944} It has diverse biological activity, including neuroprotective, anticonvulsant, and anxiolytic-like effects.{38572,38571,38570,38573} ACPT-I (1-200 µM) reduces cell death following oxygen-glucose deprivation in primary neuronal cultures and in a rat model of middle cerebral artery occlusion when used at a dose of 30 mg/kg.{38572} It is neuroprotective against excitotoxicity induced by kainite in vitro and in vivo and reduces the incidence of clonic seizures in various seizure models in mice and rats (ED50s = 0.08-49.3 nM, i.c.v.).{38571,38570} ACPT-I also has anxiolytic-like effects in mice and rats, however, these effects can be blocked by WAY-100635 (Item No. 14599) and flumazenil (Item No. 14252), indicating the involvement of the serotonin (5-HT) receptor subtype 5-HT1A and GABAA receptor.{38573}