RWJ-51204

RWJ-51204 is a partial agonist of GABA(A) receptor, with K_i of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors. IC50 & Target: Ki: 0.2-2 nM (GABA(A))^[1] In Vitro: RWJ-51204 binds to receptors in the cerebral cortex, cerebellum, or medulla-spinal cord with K_i ranging from 0.2 to 0.6 nM. In Vivo: RWJ-51204 is orally active in anxiolytic efficacy tests. WJ 51204 dose-relatedly antagonizes PTZ-induced clonic convulsions when administered orally (ED₅₀ = 0.04 mg/kg). RWJ-51204 is effective in the conflict test in monkeys (ED₅₀ of approximately 0.5 mg/kg p.o.). RWJ-51204 potently impairs rotarod performance in rats (ED₅₀ = 0.12 mg/kg), and all rats given RWJ-51204 orally at 30 mg/kg exhibit sedation, reduced skeletal muscle tone, and impairment of rotarod performance.