NGB 2904 (hydrochloride)

NGB 2904 is an antagonist that is selective for the dopamine D₃ receptor (K_i = 1.4 nM).¹ It potently inhibits quinpirole-stimulated mitogenesis (IC₅₀ = 6.8 nM).² NGB 2904 attenuates cocaine- and stress-induced reinstatement of drug-seeking behavior in rats.^3,4 It also increases spontaneous and amphetamine-stimulated locomotion in mice.⁵

1.Yuan, J., Chen, X., Brodbeck, R., et al.NGB 2904 and NGB 2849: Two highly selective dopamine D3 receptor antagonistsBioorg. Med. Chem. Lett.8(19)2715-2718(1998) 2.Grundt, P., Carlson, E.E., Cao, J., et al.Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptorJ. Med. Chem.48(3)839-848(2005) 3.Gilbert, J.G., Newman, A.H., Gardner, E.L., et al.Acute administration of SB-277011A, NGB 2904, or BP 897 inhibits cocaine cue-induced reinstatement of drug-seeking behavior in rats: Role of dopamine D3 receptorsSynapse57(1)17-28(2005) 4.Xi, Z.-X., Newman, A.H., Gilbert, J.G., et al.The novel dopamine D3 receptor antagonist NGB 2904 inhibits cocaine's rewarding effects and cocaine-induced reinstatement of drug-seeking behavior in ratsNeuropsychopharmacology31(7)1393-1405(2006) 5.Pritchard, L.M., Newman, A.H., McNamara, R.K., et al.The dopamine D3 receptor antagonist NGB 2904 increases spontaneous and amphetamine-stimulated locomotionPharmacol. Biochem. Behav.86(4)718-726(2007)