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Zolmitriptan

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Chemical Structure| 139264-17-8 同义名 : BW-311C90;311C90;NSC 760383
CAS号 : 139264-17-8
货号 : A130156
分子式 : C16H21N3O2
纯度 : 98%
分子量 : 287.36
MDL号 : MFCD00871503
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(365.4 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Zolmitriptan, a novel 5-HT1B/1D receptor agonist, has been proven efficacy in the acute treatment of migraine. In vitro studies, zolmitriptan showed a partial agonist efficacy for 5-HT1B receptor in rabbit saphenous vein and primate basilar artery, with the p[A50]=6.79+/-0.06 and p[A50]=6.92+/-0.07 respectively. Besides this, it was also found that zolmitriptan displayed high affinity for recombinant human 5-HT1D and 5-HT1B receptors in transfected CHO-K1 cell, with pIC50 values=9.16+/-0.12 and 8.32+/-0.09 respectively[3]. In vivo studies, zolmitriptan could contribute to the inhibition of evoked trigeminovascular activity within the trigeminal nucleus when given 100micrograms/kg through intravenous administration in adult cats, and this effect may play a role in the anti-migraine actions[4]. In addition, [3H]-zolmitriptan has the special binding effect in the superficial laminae of the trigeminal nucleus caudalis and dorsal horns of the C1 and C2 cervical spinal cord in cat, which demonstrates the existence of receptors that specifically bind zolmitriptan[5].
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
NCT01381497 - Completed - -
NCT01332500 - Completed - -
NCT01381523 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.48mL

0.70mL

0.35mL

17.40mL

3.48mL

1.74mL

34.80mL

6.96mL

3.48mL
参考文献

[1]Le Grand B, Panissie A, Perez M, Pauwels PJ, John GW. Zolmitriptan stimulates a Ca(2+)-dependent K(+) current in C6 glioma cells stably expressing recombinant human 5-HT(1B) receptors. Eur J Pharmacol. 2000 Jun 2;397(2-3):297-302.

[2]Martin GR, Robertson AD, MacLennan SJ, Prentice DJ, Barrett VJ, Buckingham J, Honey AC, Giles H, Moncada S. Receptor specificity and trigemino-vascular inhibitory actions of a novel 5-HT1B/1D receptor partial agonist, 311C90 (zolmitriptan). Br J Pharmacol. 1997 May;121(2):157-64.

[3]Martin GR, Robertson AD, MacLennan SJ, Prentice DJ, Barrett VJ, Buckingham J, Honey AC, Giles H, Moncada S. Receptor specificity and trigemino-vascular inhibitory actions of a novel 5-HT1B/1D receptor partial agonist, 311C90 (zolmitriptan). Br J Pharmacol. 1997 May;121(2):157-64. doi: 10.1038/sj.bjp.0701041. PMID: 9154322; PMCID: PMC1564661.

[4]Goadsby PJ, Hoskin KL. Inhibition of trigeminal neurons by intravenous administration of the serotonin (5HT)1B/D receptor agonist zolmitriptan (311C90): are brain stem sites therapeutic target in migraine? Pain. 1996 Oct;67(2-3):355-9. doi: 10.1016/0304-3959(96)03118-1. PMID: 8951929.

[5]Goadsby PJ, Knight YE. Direct evidence for central sites of action of zolmitriptan (311C90): an autoradiographic study in cat. Cephalalgia. 1997 May;17(3):153-8. doi: 10.1046/j.1468-2982.1997.1703153.x. PMID: 9170337.