Eplivanserin hemifumarate|130580-02-8|-陌孚医药/Medlife

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Eplivanserin hemifumarate

目录号: PL01823 纯度: ≥98%

CAS No. :130580-02-8

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中文名称	Eplivanserin hemifumarate
中文别名	富马酸依利色林;依利色林;紫黄素
英文名称	Eplivanserin hemifumarate
英文别名	2-Propen-1-one,1-(2-fluorophenyl)-3-(4- hydroxyphenyl)-,O-[2-(dimethylamino)ethyl]- oxime,(1Z,2E)-,(2E)-2-butenedioate (2:1) (salt);2-Propen-1-one,1-(2-fluorophenyl)-3-(4- hydroxyphenyl)-,O-[2-(dimethylamino)ethyl]- oxime,(1Z,...;2-Propen-1-one,1-(2-fluorophenyl)-3-(4- hydroxyphenyl)-,O-[2-(dimethylamino)ethyl]- oxime,(1Z,2E)-,(2E)-2-butenedioate (2:1) ;EPLIVANSERIN FUMARATE;(Z,E)-1-(2-Fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one O-[2-(dimethylamino)ethyl]oxime fumarate (2:1);SR-46349 hemifumarate salt;TRANS-2'-FLUORO-4-HYDROXYCHALCONE O-[(Z)-2-(DIMETHYLAMINO)ETHYL]OXIME--FUMARIC ACID (2:1);4-((3Z)-3-(2-Dimethylaminoethyl)oxyimino-3-(2-fluorophenyl)propen-1-yl)phenol hemifumarate salt;Eplivanserin hemifumarate salt;SR-46349B;SR 46349B;Eplivanserin hemifumarate;TRANS-2''-FLUORO-4-HYDROXYCHALCONE O-[(Z)-2-(DIMETHYLAMINO)ETHYL]OXIME--FUMARIC ACID (2:1)
Cas No.	130580-02-8
分子式	₂[C₁₉H₂₁N₂O₂F]^.C₄H₄O₄
分子量	772.83
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Eplivanserin (SR-46349) hemifumarate 是一种有效的，选择性的，具有口服活性的 5-HT₂ receptor 拮抗剂，在大鼠皮层膜中，IC₅₀ 值为 5.8 nM，同时对 5-HT₂ receptor 的 K_d 值为 1.14 nM。Eplivanserin hemifumarate 对 5-HT_2A 的选择性比对 5-HT_2B 和 5-HT_2C 高 20 倍以上。

生物活性

Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT 2A receptor antagonist, with an IC 50 of 5.8 nM in rat cortical membrane, and a K d of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT 2A than 5-HT 2B and 5-HT 2C .

性状

Solid

IC50 & Target[1][2]

5-HT2A Receptor 5.8 nM (IC50) 5-HT2C Receptor

体外研究(In Vitro)

Eplivanserin hemifumarate (SR 46349B) shows weak inhibition on other 5-HT kinases, with IC50s of 0.12 μM (Pig cortex 5-HT1C), 14 μM (Rat hippocampus 5-HT1A), and 16 μM (Rat stnatum 5-HT1B, Ox caudate nucleus 5-HT1D). Eplivanserin also has inhibitory effects on rat cortex adrenergic α1 and α2, rat whole brain histammine H1, Na channel, and rat striatum dopamine D1 and D2, with IC50s of 3.4 μM, 1.0 μM, 5.0 μM, 39 μM, 9 μM and 28 μM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Eplivanserin hemifumarate (SR 46349B) inhibits 5-HT 2 receptor binding of [H]ketanserin with an ED 50 of 0.087 mg/kg after i.p. injection, and 0.097 mg/kg after p.o administration in mice.
SR 46349B (0.25-1 mg/kg; i.p.) blocks Cocaine-evoked hyperactivity following repeated Cocaine treatment in rats. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Rinaldi-Carmona M, et al. Biochemical and pharmacological properties of SR 46349B, a new potent and selective 5-hydroxytryptamine2 receptor antagonist. J Pharmacol Exp Ther. 1992 Aug;262(2):759-68.
[2]. Malgorzata Filip, et al. Contribution of serotonin (5-hydroxytryptamine; 5-HT) 5-HT2 receptor subtypes to the hyperlocomotor effects of cocaine: acute and chronic pharmacological analyses. J Pharmacol Exp Ther. 2004 Sep;310(3):1246-54.

溶解度数据	In Vitro: DMSO : 25 mg/mL (64.69 mM; ultrasonic and warming and heat to 60°C)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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