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血管紧张素转换酶抑制剂2-[N-[(S)-1-乙氧羰基-3-苯基丙基]-L-丙氨酰]-(1S,3S,5S)-2-氮杂双环[3.3.0]辛烷-3-羧酸(Hoe 498)在健康志愿者中的耐受性和药效学

Tolerance and pharmacodynamics of the angiotensin converting enzyme inhibitor 2-[N-[(S)-1-ethoxycarbonyl-3-phenylpropyl]-L-alanyl]-(1S,3S,5S)-2- azabicyclo[3.3.0]octane-3-carboxylic acid (Hoe 498) in healthy volunteers.

作者信息

Witte P U, Metzger H, Eckert H G, Irmisch R

出版信息

Arzneimittelforschung. 1984;34(10B):1448-51.

PMID:6097272
Abstract

In healthy volunteers a single oral dose of 5 mg 2-[N-[(S)-1-Ethoxycarbonyl-3-phenylpropyl]-L-alanyl]-(1S,3S, 5S)-2-azabicyclo[3.3.0]octane-3-carboxylic acid (Hoe 498) was well tolerated. Following 5 mg Hoe 498 plasma angiotensin converting enzyme (ACE) activity was inhibited by almost 100% up to 8 h. A marked effect on plasma ACE was observed for more than 8 days. Plasma renin activity increased whereas aldosterone plasma levels decreased only slightly. Sodium and potassium excretion was not influenced by the compound. Systolic and diastolic blood pressure was slightly lowered by Hoe 498, whereas no relevant changes in pulse rate were observed.

摘要

在健康志愿者中,单次口服5毫克2-[N-[(S)-1-乙氧羰基-3-苯基丙基]-L-丙氨酰基]-(1S,3S,5S)-2-氮杂双环[3.3.0]辛烷-3-羧酸(Hoe 498)耐受性良好。服用5毫克Hoe 498后,血浆血管紧张素转换酶(ACE)活性在长达8小时内几乎被抑制100%。在超过8天的时间里观察到对血浆ACE有显著影响。血浆肾素活性增加,而醛固酮血浆水平仅略有下降。该化合物对钠和钾排泄没有影响。Hoe 498使收缩压和舒张压略有降低,而脉搏率未观察到相关变化。

相似文献

1
Tolerance and pharmacodynamics of the angiotensin converting enzyme inhibitor 2-[N-[(S)-1-ethoxycarbonyl-3-phenylpropyl]-L-alanyl]-(1S,3S,5S)-2- azabicyclo[3.3.0]octane-3-carboxylic acid (Hoe 498) in healthy volunteers.血管紧张素转换酶抑制剂2-[N-[(S)-1-乙氧羰基-3-苯基丙基]-L-丙氨酰]-(1S,3S,5S)-2-氮杂双环[3.3.0]辛烷-3-羧酸(Hoe 498)在健康志愿者中的耐受性和药效学
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2-[N-[(S)-1-ethoxycarbonyl-3-phenylpropyl]-L-alanyl]-(1S,3S,5S) -2-azabicyclo[3.3.0]octane-3-carboxylic acid (Hoe 498)--a new and highly effective angiotensin I converting enzyme inhibitor.2-[N-[(S)-1-乙氧羰基-3-苯基丙基]-L-丙氨酰]-(1S,3S,5S)-2-氮杂双环[3.3.0]辛烷-3-羧酸(Hoe 498)——一种新型高效的血管紧张素I转换酶抑制剂。
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引用本文的文献

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Pharmacokinetics and pharmacodynamics of a novel orally active angiotensin converting enzyme inhibitor (HOE 498) in healthy subjects.一种新型口服活性血管紧张素转换酶抑制剂(HOE 498)在健康受试者中的药代动力学和药效学。
Eur J Clin Pharmacol. 1984;27(5):577-81. doi: 10.1007/BF00556895.
2
The effect of an angiotensin converting enzyme inhibitor, ramipril, on bronchial responses to inhaled histamine and bradykinin in asthmatic subjects.血管紧张素转换酶抑制剂雷米普利对哮喘患者支气管对吸入组胺和缓激肽反应的影响。
Br J Clin Pharmacol. 1987 Jan;23(1):91-3. doi: 10.1111/j.1365-2125.1987.tb03015.x.
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Studies on the antihypertensive effect of single doses of the angiotensin converting enzyme inhibitor ramipril (HOE 498) in man.
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Eur J Clin Pharmacol. 1986;30(5):541-7. doi: 10.1007/BF00542412.
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Effects of the new angiotensin-converting enzyme inhibitor, ramipril, in patients with essential hypertension.新型血管紧张素转换酶抑制剂雷米普利对原发性高血压患者的疗效
Klin Wochenschr. 1986 Jun 16;64(12):558-62. doi: 10.1007/BF01735319.
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Frusemide, ACE inhibition, renal dopamine and prostaglandins: acute interactions in normal man.速尿、血管紧张素转换酶抑制剂、肾多巴胺与前列腺素:正常人的急性相互作用
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