SB-277011 dihydrochloride  (Synonyms: SB-277011A 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.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 inhibits self-administration in rats. When it increases to 50 mg/kg, SB-277011A can significantly inhibit basal and addictive agent-enhanced locomotion in rats^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

511.49

C₂₈H₃₂Cl₂N₄O

1226917-67-4

O=C(C1=CC=NC2=CC=CC=C12)N[C@H]3CC[C@H](CCN4CC5=C(C=C(C#N)C=C5)CC4)CC3.[H]Cl.[H]Cl

Room temperature in continental US; may vary elsewhere.

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

• [1]. Stemp G, et al. Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat. J Med Chem. 2000 May 4;43(9):1878-85.  [Content Brief]

  [2]. Rui Song, et al. YQA14: A Novel Dopamine D3 Receptor Antagonist That Inhibits Cocaine Self-Administration in Rats and Mice, but Not in D3 Receptor-Knockout Mice. Addict Biol  [Content Brief]