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Ecopipam hydrobromide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ecopipam hydrobromide图片
CAS NO:2587360-22-1
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品名称
SCH 39166 hydrobromide
产品介绍
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 ofdopamine D1/D5 receptor, withKis 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 (Ki=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[1].

IC50& Target[1]

D1Receptor

1.2 nM (Ki)

D5Receptor

2.0 nM (Ki)

D2Receptor

980 nM (Ki)

D4Receptor

5520 nM (Ki)

5-HT Receptor

80 nM (Ki)

Alpha-2A adrenergic receptor

731 nM (Ki)

体外研究
(In Vitro)

Ecopipam (2 μM) hydrobromide completely abolishes the proconvulsive effect of Dopamine (10 μM) in isolated corticohippocampal formation[2].

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[3].
Ecopipam (10, mg/kg, oral administration) antagonizes Apomorphine-induced stereotypy in rats[4].
Ecopipam (5 and 10 μM, perfusion, 1 μL/min) reversibly and dose-dependently decreases acetylcholine release in the rat striatum[5].

Animal Model:Male young adult Long-Evans rats were injected with Nicotine[3]
Dosage:0.003, 0.01, 0.03, 0.1, 0.3 mg/kg
Administration:A single s.c. 20 min before Nicotine (0.1 mg/kg)
Result:Dose-dependently reduced pressing on both active and inactive levers.
Clinical Trial
分子量

394.73

性状

Solid

Formula

C19H21BrClNO

CAS 号

2587360-22-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

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