NGB 2904 hydrochloride

Modify Date: 2024-01-13 19:09:12

NGB 2904 hydrochloride Structure
NGB 2904 hydrochloride structure
Common Name NGB 2904 hydrochloride
CAS Number 189061-11-8 Molecular Weight 530.916
Density N/A Boiling Point N/A
Molecular Formula C28H30Cl3N3O Melting Point N/A
MSDS USA Flash Point N/A

 Use of NGB 2904 hydrochloride


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].

 Names

Name NGB 2904
Synonym More Synonyms

 NGB 2904 hydrochloride 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
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

 Articles1

More 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...

 Synonyms

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)