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虽然对肾素-血管紧张素系统在高血压发病机理中的作用尚有争论,但日益认识用药物抑制其作用可引起降压。β-阻断剂心得安对正肾素、高肾素型有降压作用,对低肾素型则无效,甚至可引起血压升高。血管紧张素Ⅱ桔抗剂肌丙抗增压素(Sarala-Sin)有部份激动作用,只限于对血管紧张素浓度高的高血压病人有效。血管紧张素转化酶抑制剂SQ20881能抑止血管紧张素Ⅱ的产生,制止血管收缩,并可能抑止缓激肽的灭能,从而促使血管扩张,降低血压。然而,SQ20881仅能由静脉给药。为此,设计合成了口服的转化酶抑制剂巯甲丙脯氨酸(SQ14225,Captopril)。初步结果提示其降压范围甚至
Although the role of the renin-angiotensin system in the pathogenesis of hypertension remains controversial, it is increasingly recognized that the use of drugs to suppress its effects can lead to hypotension. Beta-blockers are safe and correct renin, high renin-type antihypertensive effect on the low renin-type is invalid, and even can cause high blood pressure. Angiotensin II antagonist muscle anti-triad of anti-hypertensive (Sarala-Sin) is part of the inflammatory effect, limited to high concentrations of angiotensin in patients with hypertension effective. Angiotensin converting enzyme inhibitor SQ20881 can inhibit the production of angiotensin Ⅱ to stop the vasoconstriction, and may inhibit the bradykinin inactivation, thereby contributing to vasodilation and lower blood pressure. However, SQ20881 can only be administered intravenously. To this end, we designed and synthesized oral transcontase inhibitor captopril (SQ14225, Captopril). Preliminary results suggest that its buck range even