189061-11-8
189061-11-8 structure
- Name: NGB 2904 hydrochloride
- Chemical Name: NGB 2904
- CAS Number: 189061-11-8
- Molecular Formula: C28H30Cl3N3O
- Molecular Weight: 530.916
- Catalog: Signaling Pathways GPCR/G Protein Dopamine Receptor
- Create Date: 2021-05-10 16:25:24
- Modify Date: 2024-01-13 19:09:12
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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].
| Name | NGB 2904 |
|---|---|
| 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) |
| 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 |
| Molecular Formula | C28H30Cl3N3O |
|---|---|
| Molecular Weight | 530.916 |
| Exact Mass | 529.145447 |
| RIDADR | NONH for all modes of transport |
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