各种AT1-receptor阻滞剂孤立船舶机械的差异不同的起源。

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莫尔斯P,阿德勒克Brandt-Eliasson U,卡普L, Ohlson K, Renberg L, Sjoquist PO, Abrahamsson T

各种AT1-receptor阻滞剂孤立船舶机械的差异不同的起源。

高血压。1999年6月,33(6):1406 - 13所示。

PubMed ID

10373224 (在PubMed

]

文摘

的功能抑制特征血管紧张素ⅱ1型受体拮抗剂(ARB)坎地沙坦;irbesartan;和洛沙坦及其活性代谢物EXP 3174 (EXP)研究了兔主动脉条和体外大鼠门静脉准备。此外,血浆蛋白质绑定决心,绑定是高(> 98。所有arb的5%)。这些价值观需要与arb的浓度用体外非蛋白绑定浓度在临床使用。在这两种血管准备,坎地沙坦显著降低最大收缩引起的血管紧张素ⅱ(Ang II)的响应量效曲线。洛沙坦、经验和irbesartan引起了向右平行转移没有任何重大影响最大反应和二世。坎地沙坦的抑制效应发展缓慢(最大效应> 30分钟后)和持续> 2小时尽管反复洗涤的血管。irbesartan洛沙坦的影响,实验有一个更快的开始,而且大部分的抑制作用洗后消失。 The duration of the inhibitory effects of the ARBs were not related to lipophilicity of the compounds. Cooling of the rat portal vein preparations to 4 degrees C before administration of candesartan prevented the persistent inhibition of Ang II response seen at 37 degrees C. For the other ARBs studied, the magnitude of inhibition and the speed of recovery of the Ang II response were independent of the incubation temperature before washing. In addition, when candesartan was given to conscious rats, the inhibitory effect on Ang II-induced blood pressure responses persisted during the 24-hour period despite nondetectable plasma concentrations of candesartan at 24 hours. It is concluded that functional inhibitory characteristics of candesartan differ from those of the other ARBs tested. At clinically relevant concentrations, candesartan is an insurmountable and long-lasting antagonist of the vascular contractile responses to Ang II.

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药物靶点

药物	目标	类	生物	药理作用	行动
Irbesartan	1型血管紧张素ⅱ受体	蛋白质	人类	是的	拮抗剂	细节