| Bioactivity | 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]. |
| Invitro | 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: |
| Name | NGB 2904 hydrochloride |
| CAS | 189061-11-8 |
| Formula | C28H30Cl3N3O |
| Molar Mass | 530.92 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |