5-HT1D受体受体激动剂和人类冠状动脉反应体外:交叉比较5和舒马曲坦rizatriptan和l - 741519。

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朗莫J,面包师厘米比伊·德斯塔,希尔RG,斯科菲尔德WN,泰勒AA

5-HT1D受体受体激动剂和人类冠状动脉反应体外:交叉比较5和舒马曲坦rizatriptan和l - 741519。

Br中国新药杂志。1996年10月,42 (4):431 - 41。

PubMed ID

8904614 (在PubMed

]

文摘

1。Rizatriptan (mk - 462, (N, N-dimethyl-2 - [5 - (1、2、4-triazol-1-ylmethyl) 1 h-indol-3-yl]乙胺))及其相关结构模拟l - 741519 (N-methyl-4 - [5 - (1、2、4-triazol-4-yl) 1 h-indol-3-yl]哌啶)小说5-HT1D-receptor受体激动剂。Rizatriptan显示效果作为anti-migraine剂在临床试验中。舒马曲坦自血管造影的患者的研究表明(一种建立5-HT1D-receptor受体激动剂)可引起冠状动脉血管收缩,我们比较的影响rizatriptan和l - 741519与5 -和舒马曲坦endothelium-denuded人类冠状动脉体外的部分。2。冠状动脉移植获得心脏从接受心脏移植的患者(n = 16个可行的动脉来自13个男性,3个女性,年龄在38 - 68年)和动脉段(5 - 6毫米长度)被安装在器官浴等长张力记录。每段第一次接触到45毫米氯化钾,然后5 - (1 nm - 100 microM)。浓度效应曲线rizatriptan和舒马曲坦(研究1,n = 6或7动脉)或舒马曲坦和l - 741519(研究2 n = 8动脉)被连续和随机的方式进行。得到的响应重复应用5 -在不同的段。3所示。 One artery showed severe atheroma and was not included in the analysis. ANOVA showed that 5-HT responsiveness varied significantly between arteries from different patients; but not between arterial segments from the same patient. Desensitization was seen consistently across all agonists but did not significantly affect inter-agonist comparisons. 4. There was graded effectiveness in the ability of the agonists to cause contraction with the rank order of Emax values being 5-HT >> sumatriptan > L-741,519 > rizatriptan. In terms of EC50 values, L-741,519 was significantly more potent than sumatriptan. 5. The present study (using a 'cross-over' experimental protocol) confirms our previous observation that rizatriptan is less effective than sumatriptan in causing contraction of human isolated coronary artery. Furthermore, it shows that the lower maximum contractile response to rizatriptan, compared with that of sumatriptan, is not merely the consequence of variability in response to 5-HT1D-receptor agonists between patients or between segments from the same artery.

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药物靶点

药物	目标	类	生物	药理作用	行动
Rizatriptan	5 -羟色胺受体1 d	蛋白质	人类	是的	受体激动剂	细节