Candoxatril,口服有效中性肽链内切酶抑制剂,提高血浆心房利钠因子和利钠在原发性高血压。

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奥康奈尔我,怡和AG,戴维森G,康奈尔JM

Candoxatril,口服有效中性肽链内切酶抑制剂,提高血浆心房利钠因子和利钠在原发性高血压。

J Hypertens。1992年3月,10 (3):271 - 7。

PubMed ID

1315825 (在PubMed

]

文摘

目的:Candoxatril (UK79,300)是一种口服可用中性肽链内切酶的抑制剂(E.C.3.4.24.11)降低心房利钠因子(曾帮工)。本研究旨在建立初步的安全性和有效性数据这部小说在原发性高血压类药物。设计:一个前瞻性,双盲,安慰剂对照,交叉的方式单剂与安慰剂比较candoxatril。三个剂量的candoxatril(10、50和200毫克),有四个科目在每一个剂量水平。设置:医学研究理事会血压单位,西方医院,英国格必威国际app拉斯哥(医院临床研究单位)。病人:十二未经治疗的原发性高血压患者。舒张压是大于95毫米汞柱在进入研究前三次。干预:Candoxatril或匹配的安慰剂的口服药物在空腹状态。连续测量尿量和电解质排泄(每小时尿量换成了一个相同体积的水嘴)。血压和心率都记录了12 h后药物管理局和系列血样测量等离子体曾帮工和神经激素浓度。 MAIN OUTCOME MEASURES: Urine volume and electrolyte concentration; blood pressure; heart rate; plasma atrial natriuretic factor. RESULTS: Plasma ANF concentrations rose significantly in all patients within 2 h of candoxatril administration compared with placebo although peak and integrated ANF levels were similar at all three doses. A significant natriuresis was only seen after 200 mg candoxatril, with a greater cumulative urine sodium excretion over 12 h compared with placebo; this was associated with a greater diuresis over 12 h compared with placebo. After a single oral dose of candoxatril, blood pressure and heart rate remained unchanged. CONCLUSIONS: Candoxatril in a single dose caused no adverse effects in essential hypertension. The drug caused a rise in basal ANF levels at all doses, but natriuresis was only seen with the highest dose used. No change in blood pressure was recorded after acute dosing, and the results of chronic studies with this compound are awaited. Oral inhibitors of ANF degradation may have therapeutic potential in cardiovascular disorders.

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药物靶点

药物	目标	类	生物	药理作用	行动
Candoxatril	Neprilysin	蛋白质	人类	是的	抑制剂	细节