Lobeline, MTD, and MTD analogs competitively inhibit [3H]DA uptake into vesicles prepared from rat striatum. Concentrations of lobeline (0.25 μM), MTD (0.23 μM), UKMH-105 (0.11 μM), and UKMH-106 (0.16 μM) approximated the Ki values for inhibiting [3H]DA uptake into isolated synaptic vesicles obtained from the data shown in Fig. 7. Km (top) and Vmax (bottom) values are mean ± S.E.M. *, p < 0.05 different from control; **, p < 0.01 different from control. n = 4–7 rats/analog).