No reduction of dopamine transporter binding sites in mice following treatment with the TIQ analogue 1-benzyl-1,2,3,4-tetrahydroisoquinoline

Abstract 1-Benzyl-1,2,3,4-tetrahydroisoquinoline (1-BnTIQ) and TIQ are endogenous substances inducing bradykinesia, one of the symptoms of parkinsonism, in rodents and primates, and 2-methyl-TIQ is postulated to be an active form of TIQ. We investigated the effect of 1-BnTIQ-, TIQ- or 2-methyl-TIQ-treatment on the binding of 2-β-carbomethoxy-3-β-(4-fluorophenyl)-[ N -methyl- 11 C]tropane to striatal dopamine transporters (DATs) in mice. Neither 1-BnTIQ (80 mg/kg, i.p., twice per day for 10 days) nor 2-methyl-TIQ (40 mg/kg, i.p., twice per day for 10 days) affected the radioligand–DAT binding, while TIQ (80 mg/kg, i.p., twice per day for 10 days) induced a 14% decrease. These results indicate that 1-BnTIQ does not affect the density of DATs on dopaminergic neurons, and that it is not clear whether or not 2-methyl-TIQ is an active form of TIQ.