当前位置： SCI文献检索 > BRITISH JOURNAL OF CLINICAL PHARMACOLOGY期刊下所有文献 > Attenuation by ACE inhibitor drugs of alpha-adrenoceptor sensitivity in human vessels: possible differences related to drug lipophilicity.

Attenuation by ACE inhibitor drugs of alpha-adrenoceptor sensitivity in human vessels: possible differences related to drug lipophilicity.

Abstract：

AIMS:We investigated the effect of angiotensin converting enzyme inhibitors (ACEIs) on postsynaptic adrenoceptor sensitivity and compared the effect of the lipophilic ACEI, quinapril, and that of hydrophilic agent, enalapril in human vessels. METHODS:Alpha-adrenoceptor sensitivity was evaluated using the dorsal hand vein compliance technique. The dose-response curves of vasoconstriction to phenylephrine and prostaglandin F2alpha were obtained in healthy male volunteers. RESULTS:The ACEIs shifted the dose-response curve of phenylephrine to the right and raised the median effective dose (ED50; 189.3 (57.6 ng min(-1)) of phenylephrine. Following quinapril administration, ED50 increased to 481.1 (101.8 ngmin(-1) compared with 266.8 (55.8 ngmin(-1) after enalapril (95% CI for differences; 31.1-397.5 ng min(-1)). Quinapril administration had no effect on the dose-response curve of PGF2alpha. CONCLUSIONS:ACE inhibition attenuates alpha-adrenoceptor sensitivity in human vessels. The effect of quinapril, a lipophilic ACEI, was greater than that of enalapril, a hydrophilic ACEI. Lipophilic ACEIs may be more potent in vasodilating effect than hydrophilic ACEIs. Angiotensin II concentration in tissue rather than that in plasma may contribute to the alpha-adrenoceptor sensitivity of the vessels.

journal_name

Br J Clin Pharmacol

journal_title

British journal of clinical pharmacology

authors

Kimura M,Umemura K,Kosuge K,Nishimoto M,Ohashi K,Nakashima M

doi

10.1046/j.1365-2125.1998.00834.x

subject

Has Abstract

pub_date

1998-12-01 00:00:00

pages

599-603

issue

6

eissn

0306-5251

issn

1365-2125

journal_volume

46

pub_type

临床试验,杂志文章,随机对照试验

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