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一种新型血管紧张素转换酶抑制剂——地拉普利的特性

Characteristics of a new angiotensin converting enzyme inhibitor: delapril.

作者信息

Saruta T, Nishikawa K

机构信息

Department of Internal Medicine, Keio University School of Medicine, Tokyo, Japan.

出版信息

Am J Hypertens. 1991 Jan;4(1 Pt 2):23S-28S. doi: 10.1093/ajh/4.1.23s.

Abstract

Delapril, a nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor, which has an indanylglycine moiety differing from the proline moiety of captopril or enalapril, is an esterified prodrug that is converted in vivo to its active metabolites. Delapril effectively inhibits rabbit lung ACE activity and lowers blood pressure in spontaneously hypertensive rats. Delapril has several characteristics that differ from captopril and enalapril, including high lipophilicity and weak bradykinin potentiating action. Delapril is a more potent inhibitor of vascular wall ACE activity than enalapril or captopril. It also shows a weaker potentiating action on the citric acid-induced cough in the guinea pig model compared with captopril and enalapril. In 12 out of 150 patients with essential hypertension who complained of cough during treatment with enalapril, changing to delapril resulted in resolution of the cough in 6 out of 12 of these patients: the percentage of patients in the total population with cough decreased from 8% to 4%.

摘要

地拉普利是一种非巯基血管紧张素转换酶(ACE)抑制剂,其茚满甘氨酸部分与卡托普利或依那普利的脯氨酸部分不同,它是一种酯化前药,在体内可转化为活性代谢产物。地拉普利能有效抑制兔肺ACE活性,并降低自发性高血压大鼠的血压。地拉普利具有一些与卡托普利和依那普利不同的特性,包括高亲脂性和较弱的缓激肽增强作用。与依那普利或卡托普利相比,地拉普利是血管壁ACE活性更强的抑制剂。与卡托普利和依那普利相比,它对豚鼠模型中柠檬酸诱导的咳嗽的增强作用也较弱。在150例原发性高血压患者中,有12例在接受依那普利治疗期间出现咳嗽,改用 地拉普利后,其中12例患者中有6例咳嗽症状消失:总体人群中咳嗽患者的比例从8%降至4%。

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