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Rizatriptan

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Chemical Structure| 144034-80-0 同义名 : -
CAS号 : 144034-80-0
货号 : A138654
分子式 : C15H19N5
纯度 : 98%
分子量 : 269.345
MDL号 : MFCD03840591
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Rizatriptan, a quick and consistent 5-HT1B/1D agonist, is mainly used for the treatment of migraine[3]. In vitro studies, rizatriptan, with the lower maximum contractile response, would be less effective than sumatriptan in causing contraction of human isolated coronary artery[4]. Besides this, it was found that rizatriptan could not only cause about 10-fold effect of vasoconstriction in human isolated middle meningeal artery than in human coronary artery, but also more effectively promote the expression of 5-HT1B-receptors in middle meningeal artery than in coronary artery[5]. In vivo studies, rizatriptan could inhibit the expression of calcitonin gene-related peptide (CGRP) and cholecystokinin (CCK) in the rat migraine model induced by nitroglycerin, contributing to the mitigation of migraine[6]. In addition, rizatriptan, combined with inflammatory soup, has the ability of inducing nociception-related behaviours in Sprague-Dawley rats, as well as increasing Fos expression in the cortex and trigeminal pathway[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00360282 - Completed - -
NCT01332500 - Completed - -
NCT01381523 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.71mL

0.74mL

0.37mL

18.56mL

3.71mL

1.86mL

37.13mL

7.43mL

3.71mL

参考文献

[1]Perez M, Fourrier C, et al. Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors. J Med Chem. 1995 Sep 1;38(18):3602-7.

[2]Street LJ, Baker R, et al. Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl] ethylamine and analogues: potent agonists for 5-HT1D receptors. J Med Chem. 1995 May 12;38(10):1799-810.

[3]Pascual J. A review of rizatriptan, a quick and consistent 5-HT1B/1D agonist for the acute treatment of migraine. Expert Opin Pharmacother. 2004 Mar;5(3):669-77. doi: 10.1517/14656566.5.3.669. PMID: 15013934.

[4]Longmore J, Boulanger CM, Desta B, Hill RG, Schofield WN, Taylor AA. 5-HT1D receptor agonists and human coronary artery reactivity in vitro: crossover comparisons of 5-HT and sumatriptan with rizatriptan and L-741,519. Br J Clin Pharmacol. 1996 Oct;42(4):431-41. doi: 10.1046/j.1365-2125.1996.04217.x. PMID: 8904614; PMCID: PMC2042688.

[5]Longmore J, Razzaque Z, Shaw D, Davenport AP, Maguire J, Pickard JD, Schofield WN, Hill RG. Comparison of the vasoconstrictor effects of rizatriptan and sumatriptan in human isolated cranial arteries: immunohistological demonstration of the involvement of 5-HT1B-receptors. Br J Clin Pharmacol. 1998 Dec;46(6):577-82. doi: 10.1046/j.1365-2125.1998.00821.x. PMID: 9862247; PMCID: PMC1873795.

[6]Yao G, Han X, Hao T, Huang Q, Yu T. Effects of rizatriptan on the expression of calcitonin gene-related peptide and cholecystokinin in the periaqueductal gray of a rat migraine model. Neurosci Lett. 2015 Feb 5;587:29-34. doi: 10.1016/j.neulet.2014.12.021. Epub 2014 Dec 15. PMID: 25524408.

[7]Su M, Ran Y, Han X, Liu Y, Zhang X, Tan Q, Li R, Yu S. Rizatriptan overuse promotes hyperalgesia induced by dural inflammatory stimulation in rats by modulation of the serotonin system. Eur J Neurosci. 2016 Aug;44(4):2129-38. doi: 10.1111/ejn.13296. Epub 2016 Jun 28. PMID: 27288111.