NGB 2904 hydrochloride

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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。

CAS NO:

189061-11-8

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

NGB 2904 hydrochloride 是一种有效，选择性，具有口服活性和可透过血脑屏障的多巴胺D3受体的拮抗剂，K_i值为 1.4 nM。NGB 2904 hydrochloride 对 D3 的选择性高于 D2，5-HT2，α1，D4，D1 和 D5 受体 (K_i=217，223，642，>5000，>10000 和 >10000 nM)。NGB 2904 hydrochloride 可拮抗 Quinpirole 刺激的有丝分裂。NGB 2904 hydrochloride 还可以抑制可卡因 (Cocaine) 的奖赏效应 (成瘾) 和可卡因诱导的觅药行为的恢复。

生物活性

NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist ofdopamine D3 receptor, with aK_iof 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (K_is=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 hydrochloride antagonizes Quinpirole-stimulated mitogenesis. NGB 2904 hydrochloride can inhibit Cocaine's rewarding effects and Cocaine-induced reinstatement of drug-seeking behavior^[1]^[2].

IC₅₀& Target^[1]

D₃Receptor

1.4 (Ki)

体外研究
(In Vitro)

NGB 2904 antagonizes Quinpirole (100 nM)-stimulated mitogenesis, with an IC₅₀of 5.0 nM^[1].

体内研究
(In Vivo)

NGB 2904 (0.1-5 mg/kg; i.p. 30 min prior to test) attenuates Cocaine's rewarding effects as assessed by PR self-administration, BSR, and Cocaine-triggered reinstatement of Cocaine-seeking behavior in rats^[2].
NGB 2904 (26 μg/kg; a single s.c.) enhances amphetamine (26 mg/kg)-stimulated locomotion in wild-type mice^[3].
NGB 2904 (0.026 μg-1 mg/kg; a single s.c. or once daily for 7 d) stimulates spontaneous locomotion in wild-type mice^[3].

Animal Model:	Naive male Long-Evans rats (250-300g)^[2]
Dosage:	0.1, 1, 5 mg/kg
Administration:	I.p. 30 min prior to test
Result:	Lowered the break-point for Cocaine (0.5 mg/kg; infusion) self-administration under progressive-ratio (PR) reinforcement. Inhibited the Cocaine (2 mg/kg; i.p.)-enhanced electrical brain stimulation reward (BSR). Inhibited Cocaine (10 mg/kg; i.p.)-triggered reinstatement of extinguished drug-seeking behavior.

分子量

530.92

Formula

C₂₈H₃₀Cl₃N₃O

CAS 号

189061-11-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.