Ecopipam 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 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 可用于精神分裂症、可卡因成瘾和肥胖症的研究。
产品描述
Ecopipam is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam 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 can be used for the research of schizophrenia, cocaine addition, and obesity.
体外活性
Ecopipam (2 μM) completely abolishes the proconvulsive effect of Dopamine (10 μM) in isolated corticohippocampal formation[2].
体内活性
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].
Cas No.
112108-01-7
分子式
C19H20ClNO
分子量
313.82
别名
Sch-39166;Sch 39166;UNII-0X748O646K
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years