吲哚胺拮抗剂：作为色胺和5-羟色氨酸诱发反应抑制剂的相对效力。
Indoleamine antagonists: relative potencies as inhibitors of tryptamine- and 5-hydroxytryptophan-evoked responses.
作者信息
Clineschmidt B V, Lotti V J
出版信息
Br J Pharmacol. 1974 Feb;50(2):311-3. doi: 10.1111/j.1476-5381.1974.tb08577.x.
Abstract
Four indoleamine antagonists were evaluated for relative potencies as inhibitors of tryptamine-induced forepaw clonus and 5-hydroxytryptophan-evoked head twitches. Methergoline was approximately three times more potent against the forepaw clonus than the head twitch response, whereas methysergide exhibited nearly equal activity in both tests. Cyproheptadine and cinanserin showed a profile opposite to methergoline and a greater degree of selectivity, being 25 to 40 times more potent as inhibitors of the 5-hydroxytryptophan- than of the tryptamine-induced response. These findings clearly demonstrate that the rank order of potency of indoleamine antagonists varies greatly depending upon the test procedure employed.
摘要
对四种吲哚胺拮抗剂作为色胺诱导的前爪阵挛和5-羟色氨酸诱发的头部抽搐的抑制剂的相对效力进行了评估。麦角新碱对前爪阵挛的效力比对头部抽搐反应的效力大约高三倍，而麦角酰二乙胺在两项测试中表现出几乎相等的活性。赛庚啶和辛那色林表现出与麦角新碱相反的情况，且具有更高的选择性，作为5-羟色氨酸诱导反应的抑制剂，其效力比色胺诱导反应的抑制剂高25至40倍。这些发现清楚地表明，吲哚胺拮抗剂的效力顺序根据所采用的测试程序有很大差异。
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A NEW, POTENT AND SPECIFIC SEROTONIN INHIBITOR, (SQ 10,643) 2'-(3-DIMETHYLAMINOPROPYLTHIO) CINNAMANILIDE HYDROCHLORIDE: ANTISEROTONIN ACTIVITY ON UTERUS AND ON GASTROINTESTINAL, VASCULAR, AND RESPIRATORY SYSTEMS OF ANIMALS.一种新型、强效且特异性的血清素抑制剂，（SQ 10,643）2'-（3-二甲基氨基丙硫基）肉桂酰苯胺盐酸盐：对动物子宫及胃肠、血管和呼吸系统的抗血清素活性。
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The effects of tryptamine on the central nervous system, including a pharmacological procedure for the evaluation of iproniazidlike drugs.色胺对中枢神经系统的作用，包括一种评价异烟肼样药物的药理学方法。
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