Comparison of pharmacological potencies of tropane analogs in blocking nicotine-induced antinociception (tail-flick test) and hypothermia after systemic administration to their binding affinities to [3H]monoamine transporters in brain
| Analog | AD50 Tail-Flick | AD50Hypothermia | Dopamine [3H]WIN 35,428 IC50 | Serotinin [3H]Paroxetine IC50 | Norepinephrine [3H]Nisoxetime IC50 |
|---|---|---|---|---|---|
| μmol/kg | μmol/kg | nM | nM | nM | |
| Cocaine | 3.2 | 20% @32 | 102 | 1060 | 3830 |
| RTI-29 | 6.8 | NT1-b | 9.8 | 5110 | 151 |
| RTI-31 | 7.2 | 1.1 | 1.12 | 44.5 | 37 |
| RTI-32 | 2.0 | 31.7 | 1.7 | 240 | 60 |
| RTI-51 | 1.0 | NT1-a | 1.69 | 10.6 | 37.4 |
| RTI-55 | 0.9 | 1.2 | 1.26 | 4.2 | 63 |
| RIT-70 | 0% @90 | 40% @ 90 | 2070 | 59,500 | >200,000 |
| RTI-110 | 1.0 | NT1-b | 0.62 | 4.1 | 5.45 |
| RTI-111 | 1.3 | NT1-b | 0.79 | 3.1 | 17.9 |
| RTI-112 | 3.5 | 1.5 | 0.8 | 10.5 | 36.2 |
| RTI-113 | 5.6 | NT1-b | 1.98 | 2340 | 2926 |
| RTI-114 | 5.3 | 9 | 1.4 | 1404 | 778 |
| RTI-120 | 4.0 | NT1-b | 3.26 | 24,500 | 5830 |
| RTI-121 | 0.3 | 49 | 0.4 | 66.8 | 285 |
| RTI-147 | 5.7 | NT1-b | 1.38 | 12,400 | 3950 |
| RTI-229 | 3.6 | NT1-b | 0.37 | 1730 | 990 |
| RTI-258 | 19.1 | NT1-b | 22.7 | 66.3 | 760 |
| WIN 35,065-2 | 8.0 | 6.7 | 23 | 1962 | 920 |