常用名 | 氢溴酸达非那新 | CAS号 | 133099-07-7 |
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价格 | 纯度 | 98.0% | |
备货期 | 10天 | 库存 | 现货 |
产品详情(用途,包装等)
用途: Darifenacin HBr(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.IC50 value: 8.9 (pKi) [1]Target: M3 receptorin vitro: Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced concentration-dependent contraction of the isolated bladder of rat [1]. Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6?μM. Darifenacin (100 nM) shows a significantly greater permeability for darifenacin in the basolateral to apical direction resulting in an efflux ratio in BBMEC monolayers of approximately 2.6 [2].in vivo: Darifenacin produces dose-dependent inhibition of amplitude of volume-induced bladder contractions(VIBCAMP), producing 35% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50–55% [1]. Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers [3]. 作用: 【剂型及规格】 缓释片,7.5mg、15mg 【适应症】 用于治疗伴有急迫性尿失禁、尿急、尿频症状的膀胱过动症(OAB)患者。 【用法用量】 该药为缓释片,初始剂量通常为7.5mg/d,可在用药开始后2周内将剂量增加至15mg/d。每日一次用水服用,可与食物同服。 物理化学性质: CAS号:133099-07-7 常用中文名:氢溴酸达非那新 常用英文名:Darifenacin HBr 分子式:C28H31BrN2O2 分子量:507.46 密度:N/A 沸点:614.3ºC at 760 mmHg 熔点:228-230ºC 闪点:325.3ºC 储存条件:-20°C Freezer |