Table 3.
The ratio of binding affinity (Ki) of enantiomers of vesamicol analogs for VAChT, σ1, and σ2 receptors ((−)-body/(+)-body).
| The ratio of binding affinity (Ki) of enantiomers of vesamicol analogs for VAChT, σ1, and σ2 receptors ((−)-body/(+)-body) | Tissue preparations for VAChT | |||
|---|---|---|---|---|
| VAChT | σ 1 | σ 2 | ||
| Vesamicol [55] | 0.034 | 4.88 | 1.12 | Rat brain membranes |
| FEOBV (2) [45] | 0.344 | 0.78 | — | rVAChT-PC12 cell |
| MIBT (8) [55] | 39.6 | 0.23 | 1.45 | Rat brain membranes |
| FBT (9) [60] | 72.7 | 1.03 | 3.05 | Torpedo californica |
| oIV (10) [62] | 0.063 | 4.29 | 2.80 | Rat brain membranes |
| OMV (11) [63] | 0.30 | 3.15 | 1.22 | Rat brain membranes |
| OIDV (13) [66] | 0.28 | 0.53 | 0.59 | Rat brain membranes |
| FBBV (18) [71] | 0.038 | 3.54 | 1.15 | Torpedo californica |
| 19 ∗∗ [80] | 0.047 | 0.47 | 1.74 | rVAChT-PC12 cell |
| TZ659 (20) [81] | 0.041 | 0.85 | 1.47 | rVAChT-PC12 cell |
| VAT (21) [71] | 0.045 | 1.0 | >1.28 | rVAChT-PC12 cell |
| 22 [84] | 0.13 | 1.50 | 0.55 | rVAChT-PC12 cell |