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/ Zolmitriptan

佐米曲普坦 /Zolmitriptan {[allProObj[0].p_purity_real_show]}

货号：A130156 同义名： BW-311C90;311C90

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

Zolmitriptan 化学结构 CAS号：139264-17-8
Zolmitriptan 化学结构
CAS号：139264-17-8
Zolmitriptan 3D分子结构
CAS号：139264-17-8
Zolmitriptan 化学结构 CAS号：139264-17-8
Zolmitriptan 3D分子结构 CAS号：139264-17-8
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Zolmitriptan 纯度/质量文件 产品仅供科研

货号：A130156 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 5-HT ↓ 5-HT1 ↓ 5-HT2 ↓ 5-HT3 ↓ 5-HT5 ↓ 5-HT6 ↓ 5-HT7 ↓ 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

 		98%
Lamotrigine +

5-HT (human platelets), IC50: 240 μM

5-HT (rat brain synaptosomes), IC50: 474 μM

 		98%
Venlafaxine ✔ 98%
Fluvoxamine maleate ✔ 99%
Iloperidone ✔ 98%
Ziprasidone HCl ✔ 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

 		98%
Dapoxetine HCl ✔ 97%
Trazodone ✔ 98+%
Clomipramine HCl ✔ 98%
Mirtazapine ✔ 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

 		97%
Duloxetine ✔ 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

 		98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		98%
Latrepirdine 2HCl ✔ GluR 98%
Fluoxetine HCl ✔ 99.5%
Paroxetine hydrochloride ✔ AChR 97%
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

 		+

5-HT2, pIC50: 5.5

 		97%
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		98%
LY310762 +

5-HT1D, Ki: 249 nM

 		99%+
Cyclobenzaprine HCI ✔ 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

 		98% HPLC
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

 		99+%
Olanzapine ✔ 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

 		99%
Ketanserin +++

5-HT2C (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

 		99%+
Loxapine succinate ++

5-HT2 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

 		99%
Agomelatine ✔ 98%
Clozapine ✔ 98%
Amitriptyline +

5-HT2, Ki: 235 nM

 		SERT 98%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		98+%
RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

 		99%+
Sarpogrelate HCl ++++

5-HT2A, Kd: 2.1 nM

5-HT2C, Kd: 1.1 nM

 		98%
Tropisetron ✔ 99%
Palonosetron ✔ 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

 		98%
Ondansetron ✔ 99%
Granisetron ✔ 98%
Alosetron HCl ✔ 98%
Ondansetron hydrochloride dihydrate ✔ 98%
VUF10166 ++++

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

 		99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

 		98%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

 		++++

5-HT2A, pKi: 9.75

5-HT2C, pKi: 10.46

 		+++

5-HT5A, pKi: 8.84

 		++++

5-HT6, pKi: 9.6

 		++++

5-HT7, pKi: 9.94

 		97%
Risperidone ++

5-HT1B, Ki: 14.9 nM

5-HT1D, Ki: 84.6 nM

 		++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 nM

 		+

5-HT5A, Ki: 206 nM

 		++

5-HT7, Ki: 6.6 nM

 		98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

 		99%+
Intepirdine ++++

5-HT6, pKi: 9.63

 		99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

 		98+%
BRL 15572 ++

5-HT1D, pKi: 6

5-HT1B, pKi: 6.1

 		++

5-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

 		+

5-HT6, pKi: 5.9

 		+

5-HT7, pKi: 6.3

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Zolmitriptan 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].

Zolmitriptan 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 - -

Zolmitriptan 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.

Zolmitriptan 实验方案

计算器
存储液制备 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

Zolmitriptan 技术信息

CAS号139264-17-8
分子式C16H21N3O2
分子量 287.36
别名 BW-311C90;311C90;NSC 760383
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
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

Tags: Zolmitriptan | BW-311C90;311C90;NSC 760383 | Neurotransmitter | 5-HT Receptor | AmBeed-信号通路专用抑制剂 | Zolmitriptan 纯度/质量文件 | Zolmitriptan 亚型比较 | Zolmitriptan 生物活性 | Zolmitriptan 临床数据 | Zolmitriptan 参考文献 | Zolmitriptan 实验方案 | Zolmitriptan 技术信息

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