NGB 2904 hydrochloride

Names

[ Name ]:
NGB 2904 hydrochloride

[Synonym ]:
MFCD09971107
N-{4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butyl}-9H-fluorene-2-carboxamide hydrochloride (1:1)
N-[4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butyl]-9H-fluorene-2-carboxamide hydrochloride
NGB 2904 hydrochloride
9H-Fluorene-2-carboxamide, N-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyl]-, hydrochloride (1:1)
NGB 2904 (hydrochloride)
N-{4-[4-(2,3-Dichlorophenyl)piperazin-1-yl]butyl}-9H-fluorene-2-carboxamide hydrochloride (1:1)

Biological Activity

[Description]:

NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=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].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

[Target]

D3 Receptor:1.4 (Ki)

[In Vitro]

NGB 2904 antagonizes Quinpirole (100 nM)-stimulated mitogenesis, with an IC50 of 5.0 nM[1].

[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: Naïve 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.

[References]

[1]. Yuan J, et, al. NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists. Bioorg Med Chem Lett. 1998 Oct 6;8(19):2715-8.

[2]. Xi ZX, et, al. The novel dopamine D3 receptor antagonist NGB 2904 inhibits cocaine's rewarding effects and cocaine-induced reinstatement of drug-seeking behavior in rats. Neuropsychopharmacology. 2006 Jul;31(7):1393-405.

[3]. Pritchard LM, et, al. The dopamine D3 receptor antagonist NGB 2904 increases spontaneous and amphetamine-stimulated locomotion. Pharmacol Biochem Behav. 2007 Apr;86(4):718-26.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₈H₃₀Cl₃N₃O

[ Molecular Weight ]:
530.916

[ Exact Mass ]:
529.145447

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

The dopamine D3 receptor antagonist NGB 2904 increases spontaneous and amphetamine-stimulated locomotion.

Pharmacol. Biochem. Behav. 86(4) , 718-26, (2007)

The dopamine D3 receptor is believed to play an important role in regulation of rodent locomotor behavior, and has been proposed as a therapeutic target for substance abuse, psychotic disorders, and P...

Related Compounds

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