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抑制剂/激动剂
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/ Zolmitriptan/佐米曲普坦

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

货号：A130156 同义名： BW-311C90; 311C90

Zolmitriptan是 5-HT1B/5-HT1D 受体的激动剂，具有抗偏头痛作用。

Zolmitriptan/佐米曲普坦 化学结构 CAS号：139264-17-8
Zolmitriptan/佐米曲普坦 化学结构
CAS号：139264-17-8
Zolmitriptan/佐米曲普坦 3D分子结构
CAS号：139264-17-8
Zolmitriptan/佐米曲普坦 化学结构 CAS号：139264-17-8
Zolmitriptan/佐米曲普坦 3D分子结构 CAS号：139264-17-8
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Zolmitriptan/佐米曲普坦 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 ✔ 99%
Fluvoxamine maleate ✔ 99%
Iloperidone ✔ 99%
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 ✔ 97%
Sertraline HCl ++

5-HT, Ki: 13 nM

 		98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		98%
Latrepirdine 2HCl ✔ GluR 99%
Fluoxetine HCl ✔ 99.5%
Paroxetine HCl ✔ AChR 99%
BMY 7378 ++

5-HT1D, pIC50: 5.9

5-HT1A, pIC50: 6.4

 		+

5-HT2, pIC50: 5.5

 		97%
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		95%
LY310762 +

5-HT1D, Ki: 249 nM

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

5-HT2, Ki: 3.98 nM

 		99%
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

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

5-HT2A, pIC50: 8.7

 		99%
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

 		99%+
Loxapine succinate ++

5-HT2 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

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

5-HT2, Ki: 235 nM

 		SERT 99%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		98+%
RS-127445 ++++

5-HT2B, pKi: 9.5

5-HT2B, pIC50: 10.4

 		99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

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

5-HT3 receptor, Ki: 0.091 nM

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

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

 		99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

 		99%
Asenapine maleate +++

5-HT1A, pKi: 8.6

5-HT1B, pKi: 8.4

 		++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

 		+++

5-HT5A, pKi: 8.84

 		++++

5-HT6, pKi: 9.6

 		++++

5-HT7, pKi: 9.94

 		97%
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 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-HT1B, pKi: 6.1

5-HT1D, pKi: 6

 		++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

 		+

5-HT6, pKi: 5.9

 		+

5-HT7, pKi: 6.3

 		95%
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/佐米曲普坦 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/佐米曲普坦 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/佐米曲普坦 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/佐米曲普坦 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/佐米曲普坦 技术信息

CAS号139264-17-8
分子式C16H21N3O2
分子量 287.36
SMILES Code O=C1OC[C@H](CC2=CC3=C(NC=C3CCN(C)C)C=C2)N1
MDL No. MFCD00871503
别名 BW-311C90; 311C90; NSC 760383
运输蓝冰
InChI Key ULSDMUVEXKOYBU-ZDUSSCGKSA-N
Pubchem ID 60857
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二

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

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