SB-277011 dihydrochloride is a selective, orally bioavailable and brain penetrate antagonist of dopamine D3 receptor, and restores ≥100-fold selectivity against the D2, 5-HT1B, and 5-HT1D receptors(pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively).

the effects of quinelorane in the nucleus accumbens completely reversed by SB-277011 dihydrochloride (SB 277011; 3 mg/kg, p.o.), but does not reverse the effects of quinelorane in the striatum at 93 mg/kg in rats.