Ecopipam (SCH 39166) hydrochloride 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 hydrochloride 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 hydrochloride 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 (SCH 39166) hydrochloride 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 hydrochloride 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 hydrochloride can be used for the research of schizophrenia, cocaine addition, and obesity [1] [3].
体外活性
Ecopipam (2 μM) hydrochloride 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.) hydrochloride abolishes Nicotine-induced enhancement of a sensory reinforcer in adult rats [3]. Ecopipam (10, mg/kg, oral administration) hydrochloride antagonizes Apomorphine-induced stereotypy in rats [4]. Ecopipam (5 and 10 μM, perfusion, 1 μL/min) hydrochloride reversibly and dose-dependently decreases acetylcholine release in the rat striatum [5]. Animal Model: Male young adult Long-Evans rats 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.
Cas No.
190133-94-9
分子式
C19H21Cl2NO
分子量
350.28
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