SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D 3 receptor (D 3 R) antagonist with K i values of 10.7 nM and 11.2 nM at rodent and human D 3 R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pK i s of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT 1B , and 5-HT 1D receptors, respectively .