SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetratedopamineD₃receptorantagonist, withpK_is of 8.0, 6.0,<5.2 and 5.9 for D₃, D₂, 5-HT_1B, and 5-HT_1Dreceptors, respectively.

pKi: 8.0 (D₃receptor), 6.0 (D₂receptor),<5.2 (5-HT_1Breceptor), 5.9 (5-HT_1Dreceptor)^[1]

SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate dopamine D₃receptor antagonist, and restores ≥100-fold selectivity against the D₂, 5-HT_1B, and 5-HT_1Dreceptors, with pK_is of 8.0, 6.0,<5.2 and 5.9 for D₃, D₂, 5-HT_1B, and 5-HT_1Dreceptors, respectively^[1].

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].

511.49

C₂₈H₃₂Cl₂N₄O

1226917-67-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.