Ecopipam hydrobromide

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CAS NO:

2587360-22-1

SCH 39166 hydrobromide

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，K_i值分别为 1.2 nM 和 2.0 nM。Ecopipam hydrobromide 对 D2、D4、5-HT 和 α2a 受体 (K_i=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, withK_is 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^[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)