Table 3. Ki Values for Pentamidine Determined for Selected CNS targets together with the relative selectivity value when the Ki is compared to trypanocidal activity (IC50).These results, together with the calculated relative selectivity values compared with trypanocidal affinity, are listed in Table 3.
| Target | Ki (μM) | Relative to trypanocidal activity |
|---|---|---|
| Trypanocidal Activity | 0.01 | 1.0 |
| Imidazoline 12 | 0.001 | 0.1 |
| Monoamine oxidase B | 0.181 | 18 |
| Monoamine oxidase A | 0.217 | 22 |
| Adrenergic alpha1 | 0.273 | 27 |
| Muscarinic (central) | 0.281 | 28 |
| Histamine H2 | 7.21 | 721 |
| Opioid | 1.41 | 141 |
| DA transporter | 2.11 | 211 |
| Adrenergicalpha2 | 10 | 1000 Estimate from single-point screen |
| Adrenergic β | 10 | 1000 Estimate from single-point screen |
| 5HT transporter | 10 | 1000 Estimate from single-point screen |