SB-277011 (dihydrochloride)

SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D₃ receptor antagonist, with pK_is of 8.0, 6.0, <5.2 and 5.9 for D₃, D₂, 5-HT_1B, and 5-HT_1D receptors, respectively. IC50 & Target: pKi: 8.0 (D₃ receptor), 6.0 (D₂ receptor), <5.2 (5-HT_1B receptor), 5.9 (5-HT_1D receptor)^[1] In Vitro: SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate dopamine D₃ receptor antagonist, and restores ≥100-fold selectivity against the D₂, 5-HT_1B, and 5-HT_1D receptors, with pK_is of 8.0, 6.0, <5.2 and 5.9 for D₃, D₂, 5-HT_1B, and 5-HT_1D receptors, respectively^[1]. In Vivo: SB-277011 dihydrochloride (SB 277011; 3 mg/kg, p.o.) completely reverses the effects of quinelorane in the nucleus accumbens, but does not reverse the effects of quinelorane in the striatum at 93 mg/kg in rats^[1].
SB-277011A (intraperitoneal injection; 12.5-25 mg/kg) significantly and dose-dependently reduces intravenous cocaine self-administration under both low fixed-ratio and progressive-ratio reinforcement conditions in rats. When it increases to 50 mg/kg, SB-277011A can significantly inhibit basal and cocaine-enhanced locomotion in rats^[2].