TABLE 3

Lobeline, lobelane, and MTD inhibit [125I]RTI-55 binding and [3H]neurotransmitter uptake into recombinant hDAT, hSERT, and hNET stably expressed in HEK-293 cells


Compound

[125I]RTI-55 Binding Ki

Hill Coefficient

[3H]Neurotransmitter Uptake IC50
μM μM
HEK-hDAT cells
   Lobeline 5.40 ± 1.30a –1.03 ± 0.10 >10
   Lobelane 0.097 ± 0.033 –0.92 ± 0.06 0.087 ± 14
   MTD 0.043 ± 0.015 –0.80 ± 0.07 0.117 ± 0.033
   Cocaine 0.469 ± 0.037 –1.19 ± 0.12 0.524 ± 0.055
HEK-hSERT cells
   Lobeline >10 ND
   Lobelane 0.530 ± 0.130 –0.930 0.830 ± 0.320
   MTD 1.89 ± 0.29 –0.99 ± 0.09 4.80 ± 1.20
   Cocaine 0.353 ± 0.030 –1.07 ± 0.03 0.419 ± 0.037
HEK-hNET cells
   Lobeline 1.87 ± 0.82 –0.58 ± 0.05 2.79 ± 0.480
   Lobelane 1.80 ± 0.47 –0.97 ± 0.14 0.085 ± 0.006
   MTD 0.277 ± 0.082 –0.79 ± 0.04 0.198 ± 0.070
   Cocaine
2.42 ± 0.12
–0.87 ± 0.04
0.370 ± 0.056
  • ND, not determined.

  • a Values are presented as means (±S.E.M.) from at least three independent experiments. Each experiment was conducted in duplicate (binding) or triplicate (uptake)