210421-74-2
中文名称
西他生坦钠
英文名称
Sitaxentan sodium
CAS
210421-74-2
分子式
C18H14ClN2NaO6S2
分子量
476.89
MOL 文件
210421-74-2.mol
更新日期
2024/04/30 10:32:10
210421-74-2 结构式
基本信息
中文别名
西他生坦钠司他生坦钠
西他塞坦钠
心脑血管类原料药
西他塞坦钠/司他生坦钠
(4-氯-3-甲基-1,2-恶唑-5-基)-[2-[2-(6-甲基-1,3-苯并二氧戊环-5-基)乙酰基]噻吩-3-基]磺酰亚胺钠盐
(4-氯-3-甲基异恶唑-5-基)((2-(2-(6-甲基苯并[D][1,3]二氧杂戊环-5-基)乙酰基)噻吩-3-基)磺酰基)胺钠盐
英文别名
CS-777CS-338
Thelin
TBC-11249
TBC-11250
TBC-11251 sodium
sitaxentan sodiuM
SITAXSENTAN SODIUM
TBC11251 sodiuM salt
Sitaxentan sodium salt
所属类别
生物化工：Endothelin Receptor 拮抗剂常见问题列表
简介
西他生坦钠为一种小分子化合物，主要通过抑制内皮素(Endothelin) 的作用而产生治疗作用（内皮素能调节血管收缩及血管平滑肌的生长）。其对内皮素A受体的作用是对B型内皮素受体作用的6500倍，高选择性的内皮素A受体拮抗剂能增加血流与反转血管收缩。生物活性
Sitaxentan sodium是一种选择性的endothelin A receptor (ETA)(内皮素受体A）拮抗剂，IC50和Ki分别为1.4 nM和0.43 nM，比作用于ETB选择性高7000倍。Phase 3。体外研究
Sitaxentan sodium inhibits ET-1-induced stimulation of phosphoinositide turnover with a Ki of 0.69 nM and a pA2 of 8.0.体内研究
Sitaxentan sodium has a serum half-life in the rat and the dog of 6 hours - 7 hours and 60−100% oral bioavailability. Orally administered Sitaxentan sodium is rapidly absorbed in both the rat and the dog with a t1/2(abs) of 0.7 hours and 0.3 hours, respectively. Peak plasma concentrations occurred between 2 hours and 3 hours postdosing in the rat and between 45 minutes and 90 minutes in the dog. The pulmonary vasoconstrictor response to acute hypoxia (10% O2 for 90 minutes) is prevented with Sitaxentan sodium (5 mg/kg infused i.v. 10 minutes prior to the onset of hypoxia). Sitaxentan sodium delivered i.v. 50 minutes after the onset of hypoxia reverses the established pulmonary vasoconstriction. Sitaxsentan blocks increased plasma endothelin levels. Sitaxsentan dose dependently (10 mg/kg and 50 mg/kg per day in the drinking water) attenuates right ventricular systolic pressure, right heart hypertrophy, and pulmonary vascular remodeling observed 3 weeks after a single subcutaneous injection of monocrotaline. Systemic administration of the ETA receptor antagonist Sitaxentan sodium significantly attenuates cerebral vasospasm after subarachnoid hemorrhage (SAH). Sitaxentan sodium reduces the development of hypoxic pulmonary vasoconstriction (HPV) in the pig. In addition, bolus injection of Sitaxentan sodium reverses already established HPV.不良反应
西他生坦钠常见的不良反应为头痛、外周水肿。