Ecopipam hydrobromide (Synonyms: SCH 39166 hydrobromide)
目录号: PL11596 纯度: ≥99.0%
CAS No. :2587360-22-1
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中文名称
Ecopipam hydrobromide
英文名称
Ecopipam hydrobromide
英文别名
(6aS-trans)-11-Chloro-6,6a,7,8,9,13b-hexahydro-7-methyl-5H-benzo[d]naphth[2,1-b]azepin-12-ol hydrobromide;Ecopipam (hydrobromide);rel-Ecopipam (hydrobromide);1227675-51-5;CHEMBL1535402;SCH 39166 hydrobromide;(6aS,13bR)-11-chloro-7-methyl-6,6a,7,8,9,13b-hexahydro-5H-benzo[d]naphtho[2,1-b]azepin-12-ol hydrobromide;CS-0032856;(6as-trans)-11-chloro-6,6a,7,8,9,13b-hexahydro-7-methyl-5hbenzo[d]naphth[2,1-b]azepin-12-ol hydrobromide;HY-110033;MS-26640;HY-14690B;J-004853;Ecopipam hydrobromide;AKOS024457035;CS-0904161;NCGC00092362-01;DTXSID9042596;SCH 39166 (hydrobromide);sch39166 hydrobromide;2587360-22-1;5H-Benzo[d]naphth[2,1-b]azepin-12-ol, 11-chloro-6,6a,7,8,9,13b-hexahydro-7-methyl-, hydrobromide (1:1), (6aS,13bR)-
Cas No.
2587360-22-1
分子式
C19H21BrClNO
分子量
394.73
包装储存
-20°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
Ecopipam (SCH 39166) hydrobromide 是一种有效的、选择性、具有口服活性的多巴胺 D1/D5 受体拮抗剂,Ki 值分别为 1.2 nM 和 2.0 nM。Ecopipam hydrobromide 对 D2、D4、5-HT 和 α2a 受体 (Ki=0.98,5.52,0.08 和 0.73 μM) 显示出超过 40 倍的选择性。Ecopipam hydrobromide 可用于精神分裂症、可卡因成瘾和肥胖症的研究。
生物活性
Ecopipam (SCH 39166) hydrobromide is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with K i s of 1.2 nM and 2.0 nM, respectively. Ecopipam hydrobromide shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (K i =0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrobromide can be used for the research of schizophrenia, cocaine addition, and obesity.
性状
Solid
IC50 & Target[1][2]
D1 Receptor 1.2 nM (Ki) D5 Receptor <
体外研究(In Vitro)
Ecopipam (2 μM) hydrobromide completely abolishes the proconvulsive effect of Dopamine (10 μM) in isolated corticohippocampal formation. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Ecopipam (0.003-0.3 mg/kg; a single s.c.) abolishes Nicotine-induced enhancement of a sensory reinforcer in adult rats.
Ecopipam (10, mg/kg, oral administration) antagonizes Apomorphine-induced stereotypy in rats.
Ecopipam (5 and 10 μM, perfusion, 1 μL/min) reversibly and dose-dependently decreases acetylcholine release in the rat striatum.
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
-20°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]. Wu WL, et al. Dopamine D1/D5 receptor antagonists with improved pharmacokinetics: design, synthesis, and biological evaluation of phenol bioisosteric analogues of benzazepine D1/D5 antagonists. J Med Chem. 2005 Feb 10;48(3):680-93.
[2]. Sharopov S, et al. Dopaminergic modulation of low-Mg2?-induced epileptiform activity in the intact hippocampus of the newborn mouse in vitro. J Neurosci Res. 2012 Oct;90(10):2020-33.
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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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