Description: SB269652 is a novel and potent drug-like allosteric modulator of the dopamine D2 receptor (D2R). SB269652 acts by binding in a bitopic manner at one protomer of a D2R dimer and modulating the binding of dopamine at a second protomer. SB269652 potently abolished specific binding of [(3)H]nemanopride and [(3)H]spiperone to Chinese hamster ovary-transfected D(3) receptors when radioligands were used at 0.2 and 0.5 nM, respectively.