Drug intelligence / Profile preview

SB-277011-A

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intraperitoneal (preclinical/animal Studies)
01

Overview

SB-277011-A is a potent and highly selective small molecule antagonist of the dopamine D3 receptor, with approximately 80–100-fold selectivity for D3 over D2 receptors and no partial agonist activity. It is brain penetrant and has been widely used in preclinical research to study addiction mechanisms. In animal models, it blocks cue-induced reinstatement of drug-seeking behavior for substances such as nicotine, cocaine, alcohol, and methamphetamine. This suggests potential utility in treating substance use disorders by interfering with the rewarding effects of these drugs and preventing relapse. Additionally, it has been investigated for possible application in schizophrenia (especially comorbid with addiction) but may exacerbate certain side effects like tardive dyskinesia when combined with antipsychotics[1][2][3][4][5][6].

Other names
SB-277011A dihydrochlorideSB277011A dihydrochlorideSB 277011A dihydrochloride
02

Targets

DRD3 (Dopamine receptor D3)DRD2 (Dopamine D2 Receptor)

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