RWJ-51204是GABA(A)receptor的部分激动剂，Ki值为0.2-2nM。
CAS：205701-85-5
分子式：C21H19F2N3O3
分子量：399.39
纯度：98%
存储：Store at -20°C

Background:

RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

RWJ-51204 binds to receptors in the cerebral cortex, cerebellum, or medulla-spinal cord with Ki ranging from 0.2 to 0.6 nM.

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.

[1]. Dubinsky B, et al. 5-ethoxymethyl-7-fluoro-3-oxo-1,2,3,5-tetrahydrobenzo[4,5]imidazo[1,2a]pyridine-4-N-(2-fluorophenyl)carboxamide (RWJ-51204), a new nonbenzodiazepine anxiolytic. J Pharmacol Exp Ther. 2002 Nov;303(2):777-90.