Antimigraine drug interactions with 5-hydroxytryptamine1A receptors.
Antimigraine drug interactions with 5-hydroxytryptamine1A receptors.
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抗偏头痛药物与 5-羟色胺 1A 受体的相互作用。
DOI：
10.1002/ana.410190518
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发表时间：
1986
影响因子：
11.2
通讯作者：
Peroutka,SJ
中科院分区：
文献类型：
--
作者：
Hiner,BC;Roth,HL;Peroutka,SJ
研究了四种抗偏头痛药物与大鼠脑膜5 -羟色胺受体和β -肾上腺素能受体的相互作用。甲基塞吉特、环肝苷、（−）普萘洛尔和吡唑替芬对由[3H]8 -羟基- N、N -二丙基- 2 -氨基四氢alin标记的5 -羟色胺受体表现出相似的亲和力（ic50值，83 ~ 280 nM）。赛庚啶、匹唑替芬和甲塞吉特在[3H]双氢丙烯诺尔标记的β -肾上腺素能受体上基本无活性（ic50值，8,700至87,000 nM）。相比之下，（−）心得安是一种非常有效的β -肾上腺素能药物（IC50, 3 nM）。这些数据表明，5‐羟色胺受体是（−）心得安和其他抗偏头痛药物的共同作用位点。
The interactions of four antimigraine drugs with 5‐hydroxytryptamine1Aand beta‐adrenergic receptors were analyzed in rat brain membranes. Methysergide, cyprohepatadine, (−)propranolol, and pizotifen display similar affinities (IC50values, 83 to 280 nM) for 5‐hydroxytryptamine1Areceptors labeled by [3H]8‐hydroxy‐N,N‐dipropyl‐2‐aminotetralin. Cyproheptadine, pizotifen, and methysergide are essentially inactive at beta‐adrenergic receptors labeled by [3H]dihydroal‐prenolol (IC50values, 8,700 to 87,000 nM). By contrast, (−)propranolol is an extremely potent beta‐adrenergic agent (IC50, 3 nM). These data indicate that the 5‐hydroxytryptamine1Areceptor is a common site of action for (−)propranolol and other antimigraine agents.