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血清素能拮抗剂酮色林的特异性。

Specificity of the serotonergic antagonist ketanserin.

作者信息

Stott D J, Robertson J I, Ball S G

机构信息

MRC Blood Pressure Unit, Western Infirmary, Glasgow, UK.

出版信息

J Hypertens Suppl. 1985 Dec;3(3):S191-3.

PMID:2856702
Abstract

Ketanserin reduces blood pressure effectively, but without inducing tachycardia. Its precise mode of action is unclear but under some circumstances it attenuates the rise in blood pressure caused by infusion of the alpha 1-agonist phenylephrine, suggesting that it acts at least partly as an alpha 1-adrenoceptor antagonist. However, the specificity of this attenuation has been questioned. We have therefore examined the effects of ketanserin on the blood pressure and heart rate responses to angiotensin II (a vasoconstrictor agent largely devoid of alpha 1-agonist properties). The blood pressure response to infused angiotensin II, in contrast to that of phenylephrine, was not attenuated by ketanserin. Ketanserin appeared not to increase cardiac efferent parasympathetic activity. At a dose used in the treatment of hypertension, ketanserin produces alpha 1-antagonism in man, which may partly explain its antihypertensive effect.

摘要

酮色林能有效降低血压,但不会引起心动过速。其确切作用方式尚不清楚,但在某些情况下,它能减弱由输注α1-激动剂去氧肾上腺素引起的血压升高,这表明它至少部分作为一种α1-肾上腺素能受体拮抗剂起作用。然而,这种减弱作用的特异性受到了质疑。因此,我们研究了酮色林对血管紧张素II(一种基本不具有α1-激动剂特性的血管收缩剂)引起的血压和心率反应的影响。与去氧肾上腺素不同,酮色林不会减弱对输注血管紧张素II的血压反应。酮色林似乎不会增加心脏传出副交感神经活动。在用于治疗高血压的剂量下,酮色林在人体中产生α1-拮抗作用,这可能部分解释了其降压作用。

相似文献

1
Specificity of the serotonergic antagonist ketanserin.血清素能拮抗剂酮色林的特异性。
J Hypertens Suppl. 1985 Dec;3(3):S191-3.
2
Ketanserin: a possible tool for studying the role of serotonin in hypertension.酮色林:一种研究5-羟色胺在高血压中作用的可能工具。
J Cardiovasc Pharmacol. 1985;7 Suppl 7:S130-6.
3
Ketanserin: systemic and regional hemodynamic characterization of its serotonergic and alpha-adrenergic receptor blocking effects in the pithed SHR.酮色林:在脊髓横断的自发性高血压大鼠中其5-羟色胺能和α-肾上腺素能受体阻断作用的全身和局部血流动力学特征
J Cardiovasc Pharmacol. 1989 Jan;13(1):94-104.
4
Differences in vasodilating action between ketanserin, a 5-HT2-serotonergic receptor antagonist, and terazosin, an alpha 1-adrenoceptor antagonist, in anesthetized rabbits.5-羟色胺2(5-HT2)能受体拮抗剂酮色林与α1肾上腺素能受体拮抗剂特拉唑嗪在麻醉兔体内血管舒张作用的差异。
J Cardiovasc Pharmacol. 1987;10 Suppl 3:S69-72.
5
Differences in the acute and chronic antihypertensive mechanism of action of ketanserin in spontaneously hypertensive rats.
J Pharmacol Exp Ther. 1993 Jan;264(1):129-34.
6
Does acute serotonergic type-2 antagonism reduce blood pressure? Comparative effects of single doses of ritanserin and ketanserin in essential hypertension.急性5-羟色胺能2型拮抗作用是否能降低血压?单剂量利坦色林和酮色林对原发性高血压的比较效果。
J Cardiovasc Pharmacol. 1987;10 Suppl 3:S86-8.
7
Effects of ketanserin on peripheral vascular pressor mechanisms in essential hypertension.酮色林对原发性高血压患者外周血管升压机制的影响。
J Cardiovasc Pharmacol. 1988;11 Suppl 1:S62-6.
8
Ketanserin: haemodynamic effects and mechanism of action.酮色林:血流动力学效应及作用机制
J Hypertens Suppl. 1986 Apr;4(1):S7-12.
9
The alpha-adrenergic receptor blocking effect of ketanserin and the interaction between alpha-adrenergic and S2-serotonergic receptor blockade.酮色林的α-肾上腺素能受体阻断作用以及α-肾上腺素能与5-羟色胺2型(5-HT2)受体阻断之间的相互作用
J Cardiovasc Pharmacol. 1988;11 Suppl 1:S54-61.
10
Differences in the chronic hypotensive mechanism of action of ketanserin in spontaneously hypertensive and Wistar-Kyoto rats.酮色林对自发性高血压大鼠和Wistar-Kyoto大鼠慢性降压作用机制的差异。
J Hypertens. 1994 Jan;12(1):7-14.

引用本文的文献

1
The effects of the 5 HT2 antagonist ritanserin on blood pressure and serotonin-induced platelet aggregation in patients with untreated essential hypertension.5-羟色胺2拮抗剂利坦色林对未经治疗的原发性高血压患者血压及血清素诱导的血小板聚集的影响。
Eur J Clin Pharmacol. 1988;35(2):123-9. doi: 10.1007/BF00609240.