|(S)-4-((3-(2-(二甲氨基)乙基)-1H-吲哚-5-基)甲基)恶唑烷-2-酮|CsnPharm

CAS No.: 139264-17-8

佐米曲普坦 Catalog No. CSN12245

Synonyms: BW 311C90;311C90;Flezol

Zolmitriptan is an agonist of 5-HT1B/5-HT1D receptors with anti-migraine properties.

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靶点选择性

生物活性

实验方案

技术信息

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 - -
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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4800 mL
- 17.4000 mL
- 34.7999 mL
- 5 mM
- 0.6960 mL
- 3.4800 mL
- 6.9600 mL
- 10 mM
- 0.3480 mL
- 1.7400 mL
- 3.4800 mL

技术信息

CAS号

139264-17-8

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H21N3O2

运输

蓝冰

分子量

287.36

别名

BW 311C90;311C90;Flezol;zolmitriptan;brand names Zomig;Zomigon (Argentina;Canada & Greece);AscoTop (Germany) and Zomigoro (France)

溶解度

DMSO	57.0 mg/mL (198.4 mM)
Water	Insoluble
Ethanol	58.0 mg/mL (201.8 mM)

动物实验配方

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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	-	-
NCT01332500	-	-	Completed	-	-
NCT01435941	-	-	Completed	-	-
NCT00442936	Migraine	Phase 3	Completed	-	-
NCT01086358	Workplace Migraine Treatment	Phase 4	Completed	-	United States, Ohio ... more >> Cleveland Clinic, 9500 Euclid Avenue, C-21 Cleveland, Ohio, United States, 44195 Collapse <<
NCT01086358	-	-	Completed	-	-
NCT03282227	Migraine	Phase 3	Active, not recruiting	March 2019	-
NCT02670161	Brain Tumors ... more >>Epilepsy Migraine Mild Cognitive Impairment Concussion Multiple Sclerosis Neuropathy Parkinson's Restless Legs Syndrome Stroke Collapse <<	Phase 4	Enrolling by invitation	April 2020	-
NCT00442936	-	-	Completed	-	-
NCT01587170	-	-	Completed	-	Canada, Alberta ... more >> University of Alberta Edmonton, Alberta, Canada Collapse <<
NCT01211145	Migraine Headache	Phase 4	Completed	-	-
NCT01211145	-	-	Completed	-	-
NCT00617747	Migraine	Phase 3	Completed	-	-
NCT03275922	Migraine	Phase 3	Recruiting	May 2020	-
NCT00637286	Migraine	Phase 4	Completed	-	-
NCT01276977	Acute Migraine ... more >> Migraine Headache Headache Disorders Collapse <<	Not Applicable	Completed	-	United States, California ... more >> California Medical Clinic for Headache Santa Monica, California, United States, 90404 Collapse <<
NCT02905227	Migraine	Phase 1	Completed	-	United States, Massachusetts ... more >> Site #103 North Dartmouth, Massachusetts, United States, 02747 United States, Nebraska Site #102 Lincoln, Nebraska, United States, 68502 United States, Texas Site #101 Dallas, Texas, United States, 75247 Collapse <<
NCT02745392	Acute Migraine	Phase 2 Phase 3	Completed	-	-
NCT02745392	-	-	Completed	-	-
NCT01085123	Migraine	Phase 1	Completed	-	Sweden ... more >> Research Site Uppsala, Sweden Collapse <<
NCT02609945	Migraine	Phase 1	Completed	-	United States, Florida ... more >> Site 001 Daytona Beach, Florida, United States, 32117 United States, Texas Site 002 Dallas, Texas, United States, 75247 Collapse <<
NCT03145467	Acute Migraine Headache	Phase 4	Completed	-	Turkey ... more >> Pamukkale University Denizli, Turkey, 20070 Collapse <<
NCT03708744	Migraine	Phase 1	Active, not recruiting	January 2019	United States, New Jersey ... more >> Hill Top Research, Inc. Neptune, New Jersey, United States, 07753 Collapse <<
NCT03377257	Cluster Headache	Phase 4	Not yet recruiting	April 30, 2019	-
NCT00617695	Migraine	Phase 3	Completed	-	-

佐米曲普坦 Catalog No. CSN12245

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