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牛肺血管中的色胺能受体:酮色林的作用

Tryptaminergic receptors in the bovine pulmonary vasculature: effects of ketanserin.

作者信息

Ogunbiyi P O, Eyre P

出版信息

Res Commun Chem Pathol Pharmacol. 1984 Apr;44(1):31-55.

PMID:6328601
Abstract

The vasoconstrictor actions of 5-hydroxytryptamine (5-HT) were investigated in the isolated helical strips of the pulmonary artery and vein of the adult bovine and calf. Agonist-antagonist interactions were studied by pretreating the vessels with methysergide, ketanserin and phentolamine and then establishing the dose-response curves to 5-HT or noradrenaline (NA). Methysergide significantly (p less than 0.05) inhibited 5-HT-induced contractions in the vessels. Ketanserin antagonized the vasoconstrictor actions of 5-HT but inhibition was not dose-related. NA-induced contractions of the vessels from the adult bovine were non-competitively inhibited by ketanserin. Phentolamine (PH) competitively antagonized contractions induced by 5-HT and NE in the tissues. The results suggest that 1. ketanserin is a potent, competitive antagonist of 5-HT but a weak antagonist of NE and 2. 5-HT-induced contractions in the bovine pulmonary vessels are mediated via specific tryptamine receptors (5-HT2) and alpha-adrenergic receptors.

摘要

在成年牛和小牛的离体肺动脉和肺静脉螺旋条上研究了5-羟色胺(5-HT)的血管收缩作用。通过用麦角新碱、酮色林和酚妥拉明预处理血管,然后建立对5-HT或去甲肾上腺素(NA)的剂量反应曲线,研究了激动剂-拮抗剂相互作用。麦角新碱显著(p<0.05)抑制5-HT诱导的血管收缩。酮色林拮抗5-HT的血管收缩作用,但抑制作用与剂量无关。酮色林对成年牛血管由NA诱导的收缩产生非竞争性抑制。酚妥拉明(PH)竞争性拮抗5-HT和NE在组织中诱导的收缩。结果表明:1. 酮色林是5-HT的强效竞争性拮抗剂,但对NE是弱拮抗剂;2. 5-HT诱导的牛肺血管收缩是通过特异性色胺受体(5-HT2)和α-肾上腺素能受体介导的。

相似文献

1
Tryptaminergic receptors in the bovine pulmonary vasculature: effects of ketanserin.牛肺血管中的色胺能受体:酮色林的作用
Res Commun Chem Pathol Pharmacol. 1984 Apr;44(1):31-55.
2
A two-state model for the 5-HT2 receptor: effects of alpha-adrenoceptor ligands.5-羟色胺2型受体的双态模型:α-肾上腺素能受体配体的作用
J Cardiovasc Pharmacol. 1988;11 Suppl 1:S88-92.
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The subtype of serotonin (5-HT) receptors in the rat pulmonary artery.大鼠肺动脉中血清素(5-羟色胺,5-HT)受体的亚型。
Arch Int Pharmacodyn Ther. 1987 Aug;288(2):248-55.
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10
A paradox: the 5-HT2-receptor antagonist ketanserin restores the 5-HT-induced contraction depressed by methysergide in large coronary arteries of calf. Allosteric regulation of 5-HT2-receptors.一个悖论:5-羟色胺2(5-HT2)受体拮抗剂酮色林可恢复被麦角新碱抑制的5-羟色胺在小牛大冠状动脉中所诱导的收缩。5-HT2受体的变构调节。
Naunyn Schmiedebergs Arch Pharmacol. 1985 Jan;328(3):295-300. doi: 10.1007/BF00515556.