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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

The alpha-adrenergic receptor blocking effect of ketanserin and the interaction between alpha-adrenergic and S2-serotonergic receptor blockade.

作者信息

van der Starre P J, Reneman R S

机构信息

Department of Anesthesiology, Medical Center De Klokkenberg, Breda, The Netherlands.

出版信息

J Cardiovasc Pharmacol. 1988;11 Suppl 1:S54-61.

PMID:2459516
Abstract

The alpha 1-adrenergic receptor blocking effect of ketanserin, the blocking properties of this compound for nonspecific stimulation with angiotensin II, and the alpha-adrenergic receptor blocking properties and the blood pressure lowering effect of phentolamine, ritanserin, and the combination of both compounds were studied in patients on cardiopulmonary bypass (constant flow rate, mild hypothermia) undergoing coronary artery bypass grafting. Phenylephrine was used as alpha 1-adrenergic agonist. Ketanserin reduces the alpha 1-agonistic effect of phenylephrine on blood pressure in a dose-dependent manner up to a dose of 10 mg. Ketanserin did not block the nonspecific vasoconstriction, as induced by angiotensin II. The moderate blood pressure lowering effect of phentolamine was substantially potentiated by ritanserin, which in itself did not affect blood pressure. The findings in this study indicate that the blood pressure lowering activity of ketanserin results from a combined blockade of alpha 1-adrenergic and S2-serotonergic receptors.

摘要

在接受冠状动脉搭桥术的体外循环(恒流率,轻度低温)患者中,研究了酮色林的α1-肾上腺素能受体阻断作用、该化合物对血管紧张素II非特异性刺激的阻断特性,以及酚妥拉明、利坦色林及其两者组合的α-肾上腺素能受体阻断特性和降压作用。去氧肾上腺素用作α1-肾上腺素能激动剂。酮色林以剂量依赖性方式降低去氧肾上腺素对血压的α1-激动作用,最大剂量达10 mg。酮色林未阻断血管紧张素II诱导的非特异性血管收缩。利坦色林显著增强了酚妥拉明的中度降压作用,而利坦色林本身不影响血压。本研究结果表明,酮色林的降压活性源于α1-肾上腺素能受体和S2-血清素能受体的联合阻断。

相似文献

1
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.
2
5-HT2-receptor antagonists: alpha 1- vs. 5-HT2-receptor blocking properties in blood vessels.5-羟色胺2受体拮抗剂:血管中α1与5-羟色胺2受体阻断特性
J Cardiovasc Pharmacol. 1988;11 Suppl 1:S25-9.
3
Antihypertensive effects of ketanserin and ritanserin in the spontaneously hypertensive rat.酮色林和利坦色林对自发性高血压大鼠的降压作用。
J Cardiovasc Pharmacol. 1988;11 Suppl 1:S22-4.
4
Are there interactions between S2-serotonergic and alpha 1-adrenergic receptors in isolated canine arteries?在离体犬动脉中,S2 - 5羟色胺能受体与α1 - 肾上腺素能受体之间是否存在相互作用?
J Cardiovasc Pharmacol. 1988;11 Suppl 1:S16-21.
5
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.
6
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.
7
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.
8
Alpha-adrenergic and serotonergic mechanisms in the human digit.人类手指中的α-肾上腺素能和5-羟色胺能机制。
J Cardiovasc Pharmacol. 1988;11 Suppl 1:S49-53.
9
Antihypertensive properties of ketanserin (R 41 468).酮色林(R 41 468)的降压特性。
Fed Proc. 1983 Feb;42(2):182-5.
10
Comparison between ketanserin and LY 53857 on vascular and cardiac 5-HT2 and alpha 1-adrenergic receptors in the pithed rat.酮色林与LY 53857对脊髓麻醉大鼠血管及心脏5-羟色胺2型和α1-肾上腺素能受体作用的比较
Arch Int Pharmacodyn Ther. 1990 Jul-Aug;306:57-64.

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Serotonin-induced platelet aggregation predicts the antihypertensive response to serotonin receptor antagonists.血清素诱导的血小板聚集可预测对血清素受体拮抗剂的降压反应。
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Cardiovasc Drugs Ther. 1990 Jan;4 Suppl 1:59-61. doi: 10.1007/BF00053428.
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