In an attempt to identify novel ligands for the dopamine transporter, a series of 4-substituted-2-phenylquinazolines were synthesized and evaluated. Among the compounds studied, 4-[(diphenylmethyl)amino]-2-phenylquinazoline (4 g) was identified as a novel partial inhibitor of [(125)I]RTI-55 binding to the dopamine transporter and a partial inhibitor of [(3)H]dopamine uptake.