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In vitro vesicular monoamine transporter 2 (VMAT2) binding affinity in the rat brain and inhibition of [3H]DA uptake in rat striatal synaptosomes.
| Compounds | Binding (nM) | Uptake (nM) | ||
|---|---|---|---|---|
| IC50 | Ki | IC50 | IC90 | |
| 13e | 5.45 | 3.18 | 7.89 | 36.7 |
| (+)-13e | 2.54 | 1.48 | 6.11 | 34.1 |
| (−)-13e | 470 | 270 | 129 | 1,598 |
| HTBZ | 7.23 | 4.22 | 30.6 | 277 |
| TBZ | 23.0 | 13.5 | 7.17 | 96.9 |
