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沙拉新的临床前药理学

Preclinical pharmacology of saralasin.

作者信息

Castellion A W, Fulton R W

出版信息

Kidney Int Suppl. 1979 Mar(9):S11-9.

PMID:113608
Abstract

Saralasin is a highly soluble and stable AII antagonist with a relatively short half-life; therefore, its effects are rapidly reversible when administered i.v. Acute and subacute studies have shown only transient toxicosis with no significant pathology or teratology. Saralasin's angiotensin receptor affinity has been correlated with its biologic acitivity. Observations from the pharmacodynamic investigations have shown that saralasin is a specific competitive antagonist of the vascular, renal, adrenal, cardiac, and central nervous system actions of AII. In addition, these studies further support the utility of saralasin as a diagnostic and therapeutic agent for patients whose hypertension is due directly to AII.

摘要

沙拉新是一种高度可溶且稳定的血管紧张素II拮抗剂,半衰期相对较短;因此,静脉给药时其作用可迅速逆转。急性和亚急性研究仅显示有短暂的中毒现象,无明显病理改变或致畸作用。沙拉新的血管紧张素受体亲和力与其生物活性相关。药效学研究观察表明,沙拉新是血管紧张素II在血管、肾脏、肾上腺、心脏及中枢神经系统作用的特异性竞争性拮抗剂。此外,这些研究进一步支持了沙拉新作为直接由血管紧张素II引起高血压患者的诊断和治疗药物的效用。

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