Sa. Lomenzo et al., THE EFFECTS OF ALKYL SUBSTITUENTS AT THE 6-POSITION OF COCAINE ANALOGS ON DOPAMINE TRANSPORTER BINDING-AFFINITY AND DOPAMINE UPTAKE INHIBITION, Medicinal chemistry research, 8(1-2), 1998, pp. 35-42
A series of 6-alkyl-3 beta-benzyl-2-(methoxycarbonylmethyl)tropane ana
logues were synthesized and evaluated as cocaine binding-site ligands
at the dopamine transporter (DAT). The in vitro inhibition of [3H]dopa
mine and the DAT binding affinity (K-i, [H-3]WIN 35,428) were measured
in rat caudate putamen tissue. Generally, substitution at the B-posit
ion was found to reduce ligand potency.