5-Hydroxytryptamine (5-HT)-induced endothelium-dependent relaxation of pig coronary arteries is mediated by 5-HT receptors similar to the 5-HT1D receptor subtype.
5-Hydroxytryptamine (5-HT)-induced endothelium-dependent relaxation of pig coronary arteries is mediated by 5-HT receptors similar to the 5-HT1D receptor subtype.
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5-羟色胺 (5-HT) 诱导的猪冠状动脉内皮依赖性舒张是由类似于 5-HT1D 受体亚型的 5-HT 受体介导的。
DOI：
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发表时间：
1990
影响因子：
3.5
通讯作者：
D. Hoyer
中科院分区：
文献类型：
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作者：
P. Schoeffter;D. Hoyer
用5-羟色胺（5-HT）受体激动剂和拮抗剂研究了5-HT受体介导的猪冠状动脉内皮依赖性舒张反应。在酮色林存在下，前列腺素F2 α预收缩的未摩擦（保留内皮）环以内皮依赖性方式对5-HT、5-羧酰胺色胺和5-甲氧基色胺松弛，效力和疗效大致相等。相比之下，蟾毒替宁，3-（二甲基氨基）乙基-N-甲基-1H-吲哚-5-甲磺酰胺，（-）-α-甲基-5-HT，N，N-二丙基-5-甲酰胺色胺和5-甲氧基-3-（1，2，3，6-四氢-4-吡啶基）-1H吲哚是半有效的，而其它药物[特别是5-HT 1A受体激动剂8-羟基-2-（二正丙基氨基）四氢萘]在0.1 mM以下无活性，15种药物明显竞争性拮抗5-羧酰胺色胺的作用。在最有效的拮抗剂中，（平均pKB值）为非选择性5-HT受体拮抗剂，（7.30）和甲麦角林（6.86），5-HT 1A/5-HT 1D受体配体，1-[2-（4-氨基-苯基）乙基]-4-（3-三氟甲基苯基）-哌嗪（7.02）、5-HT 1A/5-HT 1B/5-HT 1D受体配体7-三氟甲基-4-（4-甲基-1-哌嗪基）-吡咯并[1，2，-a]喹喔啉1（6.73）和育亨宾（6.37）。5-HT 1A受体的选择性配体要么无活性[8-羟基-2-（二正丙基氨基）四氢萘氢溴酸盐]，要么活性差（螺哌隆，4.44）。对5-HT 1A和5-HT 1B受体具有亲和力的β-肾上腺素受体拮抗剂可微弱拮抗5-羧酰胺色胺的作用（pKB值小于或等于5.32），5-HT 1c/5-HT 2受体拮抗剂美舒麦角碱（5.30）和育亨宾异构体柯宁碱（4.85）也是如此。甲基麦角酰胺显然是一种非竞争性拮抗剂。（250字处删节）
The 5-hydroxytryptamine (5-HT) receptor mediating endothelium-dependent relaxation of pig coronary arteries was characterized using a variety of 5-HT receptor agonists and antagonists. Unrubbed (with endothelium preserved) rings precontracted by prostaglandin F2 alpha in the presence of ketanserin relaxed in an endothelium-dependent manner to 5-HT, 5-carboxamidotryptamine and 5-methoxytryptamine with about equal potency and efficacy. By comparison, bufotenine, 3-(dimethylamino)ethyl-N-methyl-1H-indole-5-methane sulfonamide, (-)-alpha-methyl-5-HT,N,N-dipropyl-5-carboxamidotryptamine and 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H indole were half-efficient and other drugs [in particular the 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin] were inactive as agonists up to 0.1 mM. The effect of 5-carboxamidotryptamine was antagonized in an apparently competitive manner by 15 drugs. Among the most potent antagonists (mean pKB value) were the nonselective 5-HT receptor antagonists, methiothepin (7.30) and metergoline (6.86), the 5-HT1A/5-HT1D receptor ligand, 1-[2-(4-amino-phenyl)ethyl]-4-(3-trifluoromethylphenyl)-piperazine (7.02), the 5-HT1A/5-HT1B/5-HT1D receptor ligand, 7-trifluoromethyl-4-(4-methyl-1-piperazinyl)-pyrrolo[1,2,-a]quinoxaline 1 (6.73) and yohimbine (6.37). Selective ligands for 5-HT1A receptors were either inactive [8-hydroxy-2-(di-n-propylamino)tetralin hydrobromide] or poorly active (spiperone, 4.44). Beta-adrenoceptor antagonists with affinity for 5-HT1A and 5-HT1B receptors weakly antagonized the effect of 5-carboxamidotryptamine (pKB values less than or equal to 5.32), as did the 5-HT1c/5-HT2 receptor antagonist, mesulergine (5.30) and the yohimbine isomer, corynanthine (4.85). Methysergide was clearly a noncompetitive antagonist.(ABSTRACT TRUNCATED AT 250 WORDS)