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Ecopipam hydrochloride

目录号 : GC70978

Ecopipam hydrochloride是一种有效的、选择性的、口服活性的多巴胺D1/D5受体拮抗剂,Kis分别为1.2 nM和2.0 nM。

Ecopipam hydrochloride Chemical Structure

Cas No.:190133-94-9

规格 价格 库存 购买数量
5 mg
¥1,080.00
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10 mg
¥1,710.00
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25 mg
¥3,420.00
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50 mg
¥5,400.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

Ecopipam (SCH 39166) hydrochloride 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 hydrochloride 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 hydrochloride can be used for the research of schizophrenia and obesity.

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

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].

References:
[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.
[3]. Satanove DJ, et al. Nicotine-induced enhancement of a sensory reinforcer in adult rats: antagonist pretreatment effects. Psychopharmacology (Berl). 2021 Feb;238(2):475-486.
[4]. R E Chipkin, et al. Pharmacological profile of SCH39166: a dopamine D1 selective benzonaphthazepine with potential antipsychotic activity. J Pharmacol Exp Ther. 1988 Dec;247(3):1093-102.
[5]. E Acquas, et al. Local application of SCH 39166 reversibly and dose-dependently decreases acetylcholine release in the rat striatum. Eur J Pharmacol. 1999 Nov 3;383(3):275-9.

Chemical Properties

Cas No. 190133-94-9 SDF
分子式 C19H21Cl2NO 分子量 350.28
溶解度 DMSO : 100 mg/mL (285.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) 储存条件 4°C, sealed storage, away from moisture
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1 mM 2.8549 mL 14.2743 mL 28.5486 mL
5 mM 0.571 mL 2.8549 mL 5.7097 mL
10 mM 0.2855 mL 1.4274 mL 2.8549 mL
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