Table I.
Effects of Organic Cation Transporter Modulators on [3H]-nicotine Transport at the Mouse BBB
| Compound | Concentration (mM) | Relative transport rate (%) |
|---|---|---|
| Agmatine | 10 | 98 ± 14 |
| Carnitine | 15 | 96 ± 17 |
| Choline | 15 | 94 ± 16 |
| Dopamine | 10 | 99 ± 15 |
| Histamine | 10 | 97 ± 8 |
| Serotonin | 10 | 99 ± 9 |
| Tetraethylammonium | 15 | 105 ± 13 |
Cis-inhibition of [3H]-nicotine (8 nM) transport at the BBB by an unlabelled compound was evaluated by in situ brain perfusion with Krebs carbonate perfusion fluid (pHe 7.40) for 60 s in Swiss mice. Brain transport (K in) for [3H]-nicotine (8 nM) in controls, set at 100%, was 17.9 ± 1.1 μl/s/g (100 ± 6%). Data represent the means ± SD (n = 4–6)