205701-85-5
205701-85-5 結(jié)構(gòu)式
基本信息
中文別名
化合物 T16811 英文別名
RWJ-51204Pyrido[1,2-a]benzimidazole-4-carboxamide, 5-(ethoxymethyl)-7-fluoro-N-(2-fluorophenyl)-1,2,3,5-tetrahydro-3-oxo-
物理化學(xué)性質(zhì)
沸點(diǎn)533.0±50.0 °C(Predicted)
密度1.41±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)10.81±0.70(Predicted)
常見問題列表
生物活性
RWJ-51204 是 GABA(A) receptor 的部分激動(dòng)劑，Ki 值為 0.2-2 nM。靶點(diǎn)
Ki: 0.2-2 nM (GABA(A))
體外研究
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.
體內(nèi)研究
RWJ-51204 is orally active in anxiolytic efficacy tests. WJ 51204 dose-relatedly antagonizes PTZ-induced clonic convulsions when administered orally (ED 50 = 0.04 mg/kg). RWJ-51204 is effective in the conflict test in monkeys (ED 50 of approximately 0.5 mg/kg p.o.). RWJ-51204 potently impairs rotarod performance in rats (ED 50 = 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.