124750-92-1
124750-92-1 結(jié)構(gòu)式
基本信息
氯沙坦羧酸
5-羧酸洛沙坦
洛沙坦-5-羧酸
EXP 317
exp3174
l-158641
AKOS 91941
Losartan acid
LOSARTAN CARBOXY ACID
Losartan Carboxylic Acid
’-biphenyl)-4-yl)methyl)-
EXP 3174 (LOSARTAN CARBOXYLIC ACID)
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
常見(jiàn)問(wèn)題列表
藥理作用：氟沙坦能特異性的拮抗血管緊張素ⅡAT1受體，阻斷了循環(huán)和局部組織中血管緊張素Ⅱ(AGⅡ) 所致的動(dòng)脈血管收縮、交感神經(jīng)興奮和壓力感受器敏感性增加等效應(yīng)，強(qiáng)力和持續(xù)性降低血壓，使收縮壓和舒張壓下降。尚可減輕左心室肥厚，抑制心肌細(xì)胞增生，延遲或逆轉(zhuǎn)心肌重構(gòu)，改善左室功能。對(duì)血糖、血脂代謝無(wú)不利影響。其還具有改善腎血流動(dòng)力學(xué)作用，減輕腎血管阻力，選擇性擴(kuò)張出球小動(dòng)脈，降低腎小球內(nèi)壓力，降低蛋白尿，增加腎血流量和腎小球?yàn)V過(guò)率，保護(hù)腎臟而延緩慢性腎功能不全的過(guò)程，特別對(duì)糖尿病腎病的惡化有逆轉(zhuǎn)作用。
用途：用于原發(fā)性高血壓和充血性心力衰竭。
圖1為氟沙坦的合成路線
有關(guān)氟沙坦的抗高血壓藥、合成路線、注意事項(xiàng)、不良反應(yīng)、藥代動(dòng)力學(xué)是由Chemicalbook的燦燦編輯整理。（2016-02-03）
Angiotensin II receptor type 1
The specific binding of [125I]-angiotensin II to VSMC is inhibited by Losartan Carboxylic Acid (E-3174) with an IC 50 of 1.1 nM. Losartan Carboxylic Acid abolishes the angiotensin II-induced formation of inositolphosphates in VSMC. Losartan Carboxylic Acid inhibits the angiotensin II-induced elevation of intracellular cytosolic Ca2+ concentration with an IC 50 of 5 nM. Losartan Carboxylic Acid is more effective than losartan in blocking the angiotensin II-induced increase in Egr-1 mRNA. Losartan Carboxylic Acid inhibits the angiotensin II-induced cell protein synthesis with an IC 50 of 3 nM.
Losartan Carboxylic Acid (E-3174) (0.1 mg/kg; i.v. followed by 0.02 mg/kg/h for 5.5 h) induces a similar level of inhibition (87±4%) of the pressor responses to angiotensin I.
Intravenous Losartan Carboxylic Acid (0.1 mg/kg+0.01 mg/kg/min) is infused in anesthetized dogs with recent (8.1±0.4 days) anterior myocardial infarction. Electrolytic injury of the left circumflex coronary artery to induce thrombotic occlusion and posterolateral ischemia is initiated 1 h after the start of treatment.
| Animal Model: | Mongrel dogs of either sex, weighing 15-25 kg |
| Dosage: | 0.1 mg/kg (followed by 0.02 mg/kg/h) |
| Administration: | i.v. for 5.5 hours |
| Result: | The pressor response was reduced by 87±4%. |