2-(2-氨基乙基)-喹啉(D-1997):一种与偏头痛治疗相关的脑血管5-HT1受体的新型激动剂

J. Terron
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引用次数: 1

摘要

对一组喹啉衍生物的功能药理学性质进行了筛选,以确定其对介导血管收缩的5- ht1样受体的激动剂活性。在预测抗偏头痛活性的实验模型中,2-(2-氨基乙基)喹啉盐酸盐(D-1997)对血管收缩剂5- ht1样受体表现出比喹帕嗪更高的效力和疗效。D-1997还被发现在颈动脉循环中激活一种新的血管收缩机制。这表明D-1997可能是寻找更好的急性抗偏头痛治疗方法的有用线索。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
2-(2-aminoethyl)-quinoline (D-1997): A Novel Agonist at Craniovascular 5-HT1 Receptors Relevant to Migraine Therapy
The functional pharmacological properties of a group of quinoline-derivatives were screened for agonist activity at 5-HT1-like receptors mediating vasoconstriction. In experimental models predictive of antimigraine activity, 2-(2-aminoethyl) quinoline hydrochloride (D-1997) exhibited higher potency and efficacy at vasoconstrictor 5-HT1-like receptors than quipazine. D-1997 was also found to activate a novel vasoconstrictor mechanism in the carotid circulation. It is suggested D-1997 may represent a useful lead in the search for better acute antimigraine therapies.
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