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产品编号:  AD.Y00004-1kg 中文名称:  苹果酸阿莫曲坦
中文别名:  阿莫曲坦 英文名称:  Almotriptan
英文别名:  almotriptan malate 品牌: ANDY
规格型号:  1kg CAS号:  181183-52-8
分子式:  C21H31N3O7S 分子量: 469.55
外观与性状:  淡黄色固体 储存条件: 2-8°C
纯度:  99%
标准价:  询价篮 优惠价:  暂无
数量:  

单位:  
库存与货期:  订货

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商品信息

Almotriptan malate 是5-HT1B/1D受体激动剂,用于研究偏头痛。


生物活性

Almotriptan Malate is a 5-HT1B/1D-receptor agonist used to treat migraine. IC50: Target: 5-hydroxytryptamine1B/1D (5-HT1B/1D) Receptor Almotriptan Malate is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. Almotriptan showed low nanomolar affinity for the 5-HT(1B) and 5-HT(1D) receptors in several species, including the human, while affinity for 5-HT receptors other than 5-HT(1B/1D) was clearly less. Almotriptan did not exhibit significant affinity for several non-5-HT receptors studied up to 100 microM. Almotriptan inhibited forskolin-stimulated cyclic AMP accumulation in HeLa cells transfected with 5-HT(1B) or 5-HT(1D) human receptors [1]. Almotriptan had a mild antiemetic effect and a slight, transient diuretic effect in dogs, although the latter effect is probably of no clinical relevance. In addition, no effect on the respiratory system of conscious guinea pigs was observed following almotriptan treatment. These results indicate that almotriptan has a favourable safety profile with respect to the central nervous, renal and respiratory systems [2].

IC50 & Target

 

 

5-HT1B Receptor

5-HT1D Receptor

Clinical Trial

NCT Number

Sponsor

Condition

Start Date

Phase

NCT00212823

Ortho-McNeil Neurologics, Inc.

Migraine

June 2004

Phase 4

NCT00210483

Janssen-Ortho LLC|Ortho-McNeil Neurologics, Inc.

Migraine

July 2003

Phase 3

NCT00432549

The New England Center for Headache, P.C.|Ortho-McNeil Neurologics, Inc.

Analgesic Rebound Headache

January 2007

Phase 4

分子量

469.55

Formula

C??H??N?O?S

CAS

181183-52-8

中文名称

马来酸阿莫曲坦

SMILES

O=C(O)C(O)CC(O)=O.O=S(CC1=CC2=C(NC=C2CCN(C)C)C=C1)(N3CCCC3)=O

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder

-20°C

3 years

4°C

2 years

In solvent

-80°C

6 months

-20°C

1 month

溶解性数据

In Vitro: 

DMSO : 100 mg/mL (212.97 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

 

1 mM

2.1297 mL

10.6485 mL

21.2970 mL

5 mM

0.4259 mL

2.1297 mL

4.2594 mL

10 mM

0.2130 mL

1.0648 mL

2.1297 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用 以下溶剂前显示的百
分比是指该溶剂在您配制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

1.请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

2.请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

3.请依序添加每种溶剂: 10% DMSO    90% corn oil

Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

参考文献

[1]. Bou J , et al. Pharmacological characterization of almotriptan: an indolic 5-HT receptor agonist for the treatment of migraine. Eur J Pharmacol, 2000. 410(1): p. 33-41.

[2]. Gras J, et al. Safety profile of almotriptan, a new antimigraine agent. Effects on central nervous system, renal function and respiratory dynamics. Arzneimittelforschung, 2001. 51(9): p. 726-32.


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