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对双氢麦角环肽和双氢麦角胺的静脉收缩反应:5-羟色胺1样受体参与的证据。

Venoconstrictor responses to dihydroergocristine and dihydroergotamine: evidence for the involvement of 5-HT1 like receptors.

作者信息

Müller-Schweinitzer E

机构信息

Sandoz Pharma AG, Basel, Switzerland.

出版信息

Cardiovasc Drugs Ther. 1990 Dec;4(6):1455-60. doi: 10.1007/BF02026491.

DOI:10.1007/BF02026491
PMID:2127899
Abstract

Dihydroergocristine (DHEC) and dihydroergotamine (DHE) were investigated on canine saphenous veins in vivo and on canine saphenous veins and basilar arteries in vitro. Following local i.v. infusion in vivo, the venoconstrictor response to DHEC was about 30% weaker than that produced by DHE. When administered orally, however, both ergot alkaloids elicited similar venoconstrictor effects. In vitro maximal contractile responses to DHEC and DHE of basilar arteries were only 20-30% of those produced by 5-HT, whereas in saphenous veins both DHEC and DHE elicited similar maximal effects as those observed with 5-HT. In saphenous veins, methiothepin antagonized venoconstrictor responses to 5-HT, DHEC, and DHE within the same concentration range, being significantly less potent when tested against noradrenaline. The reverse was true for yohimbine, which was significantly more potent against noradrenaline than against 5-HT, DHEC, and DHE. It is suggested that the venoconstrictor responses to both DHEC and DHE are mediated through 5-HT1-like receptors.

摘要

在体研究了双氢麦角隐亭(DHEC)和双氢麦角胺(DHE)对犬隐静脉的作用,并在体外研究了它们对犬隐静脉和基底动脉的作用。在体局部静脉内输注后,DHEC引起的静脉收缩反应比DHE产生的反应弱约30%。然而,口服给药时,两种麦角生物碱引起的静脉收缩作用相似。在体外,基底动脉对DHEC和DHE的最大收缩反应仅为5-羟色胺(5-HT)产生反应的20%-30%,而在隐静脉中,DHEC和DHE引起的最大效应与5-HT观察到的相似。在隐静脉中,甲硫噻平在相同浓度范围内拮抗对5-HT、DHEC和DHE的静脉收缩反应,与去甲肾上腺素相比其效力明显较低。育亨宾的情况则相反,它对去甲肾上腺素的效力明显比对5-HT、DHEC和DHE的效力更强。提示对DHEC和DHE的静脉收缩反应均通过5-HT1样受体介导。

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本文引用的文献

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In vitro studies on the duration of action of dihydroergotamine.
Int J Clin Pharmacol Ther Toxicol. 1980;18(2):88-91.
2
The specific activity of retained and released norepinephrine in dog saphenous vein prelabeled with radiolabeled norepinephrine.用放射性标记去甲肾上腺素预先标记的犬隐静脉中留存和释放的去甲肾上腺素的比活性。
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Actions of co-dergocrine mesylate and its components at vascular smooth muscle.甲磺酸双氢麦角隐亭及其成分对血管平滑肌的作用。
Naunyn Schmiedebergs Arch Pharmacol. 1982 Feb;318(3):225-33. doi: 10.1007/BF00500484.
5
[Hypertension therapy with Briserin: what role do dihydroergocristine components play?].[使用溴麦角环肽进行高血压治疗:二氢麦角隐亭成分起什么作用?]
Med Klin. 1981 Dec 18;76(26):746-52.
6
Evidence for mediation by 5-HT2 receptors of 5-hydroxytryptamine-induced contraction of canine basilar artery.5-羟色胺诱导犬基底动脉收缩通过5-HT2受体介导的证据。
Naunyn Schmiedebergs Arch Pharmacol. 1983 Dec;324(4):287-92. doi: 10.1007/BF00502625.
7
The recording of venous compliance in the conscious dog: a method for the assessment of venoconstrictor agents.清醒犬静脉顺应性的记录:一种评估静脉收缩剂的方法。
J Pharmacol Methods. 1984 Aug;12(1):53-8. doi: 10.1016/0160-5402(84)90006-8.
8
Pharmacological actions of the main metabolites of dihydroergotamine.
Eur J Clin Pharmacol. 1984;26(6):699-705. doi: 10.1007/BF00541928.
9
Alpha-adrenoceptors, 5-hydroxytryptamine receptors and the action of dihydroergotamine in human venous preparations obtained during saphenectomy procedures for varicose veins.α-肾上腺素能受体、5-羟色胺受体以及双氢麦角胺在大隐静脉切除术治疗静脉曲张过程中获取的人体静脉制剂中的作用。
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10
Studies on the peripheral mode of action of dihydroergotamine in human and canine veins.双氢麦角胺在人及犬类静脉中的外周作用模式研究。
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