中文同义词:
[(2S,6R)-6-[[(S)-1-(乙氧羰基)-3-苯基丙基]氨基]-5-氧代-2-(2-噻吩基)-1,4-硫氮杂卓-4-基]乙酸盐酸盐;盐酸替莫普利;替莫普利盐酸盐;TEMOCAPRIL HYDROCHLORIDE盐;盐酸替莫普利及中间体
英文名称:
Temocapril hydrochloride
英文同义词:
TEMOCAPRIL HYDROCHLORIDE;Temocapril HCl and intermediates;Acecol;CS-622;1,4-Thiazepine-4(5H)-acetic acid, 6-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]tetrahydro-5-oxo-2-(2-thienyl)-, monohydrochloride, (2S,6R)- (9CI);1,4-Thiazepine-4(5H)-acetic acid, 6-[[1-(ethoxycarbonyl)-3-phenylpropyl]amino]tetrahydro-5-oxo-2-(2-thienyl)-, monohydrochloride, [2S-[2a,6b(R*)]]-;Temocapril Hcl;TemocarpileHCL
相关类别:
小分子抑制剂,天然产物;中间体;药物分子;原料;Intermediates Fine Chemicals;Pharmaceuticals;Inhibitors
比旋光度
25D +47.7° (c = 1 in DMF)
CAS 数据库
110221-44-8(CAS DataBase Reference)
生物活性
Temocapril HCl (CS-622)是Temocapril的盐酸盐形式,是一种长效的血管紧张素转换酶(ACE)抑制剂,用于治疗高血压。
体外研究
Temocapril hydrochloride is a prodrug of the ACE inhibitor, Temocaprilat. Temocapril hydrochloride can be readily uptaken via the human small intestine, and then be converted to its active metabolite (temocaprilat) by CES1 in the liver.
体内研究
Temocapril hydrochloride (30 mg/kg; p.o.; daily; for 4 weeks) suppresses Angiotensin I-induced hypertension, plasma and renal ACE activity, but fails to reduce the level of Ang II in the kidney.
Animal Model: Male Sprague Dawley rats
Dosage: 30 mg/kg
Administration: Oral administration, daily, for 4 weeks
Result: Suppressed the blood pressure elevation induced by Ang I.
Animal Model:
Male Sprague Dawley rats
Administration:
Oral administration, daily, for 4 weeks
Result:
Suppressed the blood pressure elevation induced by Ang I.
毒性
LD50 in mice, rats, dogs (mg/kg): >5000, >5000, >800 orally (Koike)