Characterization of 5‐HT receptors mediating contraction of canine and primate basilar artery by use of GR43175, a selective 5‐HT1‐like receptor agonist
Characterization of 5‐HT receptors mediating contraction of canine and primate basilar artery by use of GR43175, a selective 5‐HT1‐like receptor agonist
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使用选择性 5-HT1 样受体激动剂 GR43175 表征 5-HT 受体介导犬和灵长类基底动脉收缩
DOI：
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发表时间：
1989
影响因子：
7.3
通讯作者：
P. Humphrey
中科院分区：
文献类型：
--
作者：
H. Connor;W. Feniuk;P. Humphrey
1本研究的目的是通过使用多种选择性5-羟色胺（5-HT）激动剂和拮抗剂来表征介导犬和灵长类动物离体基底动脉收缩的5-HT受体。2 5-HT、α-甲基5-HT和选择性5-HT 1样受体激动剂GR 43175和5-羧酰胺色胺（5-CT）均引起犬和灵长类动物基底动脉收缩，激动剂效力的顺序为5-CT ≥ 5-HT > GR 43175> α-甲基5-HT。5-HT 1样受体激动剂GR 43175和5-CT产生的最大效应小于5-HT或α-甲基5-HT产生的效应。3在犬基底动脉，酮色林（0.1-1 μm）对5-HT的最大效应有一定的抑制作用，但对浓度效应曲线的影响很小或没有影响。GR 43175的收缩作用不受酮色林（1 μm）、MDL 72222（1 μm）或氰基吲哚洛尔（1 μm）的影响。然而，5-HT和GR 43175的作用被甲硫替平（0.1 μm）特异性拮抗;平均激动剂浓度比分别为33和48。4在灵长类动物基底动脉中，酮色林（1 μm）再次引起5-HT最大反应的小幅降低，但对GR 43175诱导的收缩没有影响。相比之下，甲硫替平（0.1 μm）拮抗5-HT-和GR 43175诱导的收缩;两者的平均激动剂浓度比均为35。5这些结果表明，5-HT在犬和灵长类动物基底动脉中的大部分作用是通过刺激5-HT 1样受体产生的。这种受体的特征在于新型选择性激动剂GR 43175的高效力和对甲硫氨酸阻断的敏感性。然而，在这些前体中似乎也存在5-HT 2受体群体，其有助于5-HT的收缩作用。
1 The aim of this study was to characterize the 5‐hydroxytryptamine (5‐HT) receptor which mediates contraction of canine and primate isolated basilar artery by use of a variety of selective 5‐HT agonists and antagonists. 2 5‐HT, α‐methyl 5‐HT and the selective 5‐HT1‐like receptor agonists, GR43175 and 5‐carboxamidotryptamine (5‐CT), each caused contraction of canine and primate basilar artery with a rank order of agonist potency of 5‐CT ≥ 5‐HT > GR43175 > α‐methyl 5‐HT. The 5‐HT1‐like receptor agonists, GR43175 and 5‐CT, produced maximum effects which were less than that produced by 5‐HT or α‐methyl 5‐HT. 3 In canine basilar artery, ketanserin (0.1–1 μm) caused some depression of the maximum effect of 5‐HT but produced little or no shift of the concentration‐effect curve. The contractile effects of GR43175 were not modified by ketanserin (1 μm), MDL72222 (1 μm) or cyanopindolol (1 μm). However, the effects of 5‐HT and GR43175 were specifically antagonized by methiothepin (0.1 μm); the mean agonist concentration‐ratios were 33 and 48 respectively. 4 In primate basilar artery, ketanserin (1 μm) again caused a small depression of the 5‐HT maximum response but had no effect against GR43175‐induced contractions. In contrast, methiothepin (0.1 μm) antagonized both 5‐HT‐ and GR43175‐induced contractions; the mean agonist concentration‐ratios were 35 for both. 5 These results demonstrate that a large component of the effects of 5‐HT in canine and primate basilar artery is produced by stimulation of a 5‐HT1‐like receptor. This receptor can be characterized by the high potency of the novel, selective agonist, GR43175, and susceptibility to blockade by methiothepin. However, there also appears to be a population of 5‐HT2 receptors in these pre‐pAarations which contribute to the contractile effects of 5‐HT.
抗偏头痛药物与 5-羟色胺 1A 受体的相互作用。
影响因子：
11.2
作者：
Hiner,BC;Roth,HL;Peroutka,SJ
通讯作者：
Peroutka,SJ
5-羟色胺1A受体介导的犬基底动脉收缩。
DOI：
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发表时间：
1986
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Peroutka,SJ;Huang,S;Allen,GS
通讯作者：
Allen,GS