Contrast Media & Molecular Imaging / 2018 / Article / Tab 1 / Review Article
In Vivo and In Vitro Characteristics of Radiolabeled Vesamicol Analogs as the Vesicular Acetylcholine Transporter Imaging Agents Table 1 Binding affinity of vesamicol analogs for VAChT, σ 1 , and σ 2 .
The ratio of vesamicol analogs (1 –22 ) to vesamicol for Ki value Tissue preparations for VAChT VAChT σ 1 σ 2 Vesamicol 1 1 1 — Benzovesamicol (BV) 0.56 0.80 0.86 Rat brain membranes Decalinvesamicol (DV) 0.50 2.75 0.31 Rat brain membranes (−)-IBVM (1 ) — — — — (−)-FEOBV (2 )45 ] 0.41 10.25 — rVAChT-PC12 cell (−)-MABV (3 ) [48 ] — — — — (−)-NEFA (4 ) [49 ] 0.32 — — Torpedo californica (5 ) [51 ] 1.17 22.84 11.38 rVAChT-PC12 cell (6 ) [53 ] 0.49 3.19 0.54 rVAChT-PC12 cell (7 ) [53 ] 0.14 0.44 2.30 rVAChT-PC12 cell MIBT (8 ) [55 ] 0.065 3.54 5.59 Torpedo californica (+)-MIBT (8 ) [55 ] 0.11 0.13 0.51 Rat brain membranes FBT (9 ) [55 ] 0.25 0.04 0.66 Rat brain membranes (+)-FBT (9 ) [60 ] 0.22 0.84 1.04 Torpedo californica oIV(10 ) [62 ] 0.42 0.077 0.83 Rat brain membranes (−)-oIV (10 ) [62 ] 1.15 0.83 1.32 Rat brain membranes (−)-OMV (11 ) [63 ] 1.52 0.46 0.77 Rat brain membranes 3′-IBVM (12 ) [64 ] 0.21 5.75 1.37 Torpedo californica OIDV (13 ) [65 ] 0.61 10.94 1.37 Rat brain membranes (−)-OIDV (13 ) [66 ] 0.95 8.66 0.86 Rat brain membranes OBDV (14 ) [67 ] 0.41 6.82 1.59 Rat brain membranes OMDV (15 ) [68 ] 0.56 3.38 0.31 Rat brain membranes FAMV (16 ) [69 ] — — — rVAChT-PC12 cell FBMV (17 ) [70 ] — — — rVAChT-PC12 cell (−)-FBBV (18 ) [71 ] 0.51 13.90 9.25 Torpedo californica (−)-19 — — — rVAChT-PC12 cell (−)-TZ659 (20 ) — — — rVAChT-PC12 cell (−)-VAT (21 ) — — — rVAChT-PC12 cell (−)-22 — — — rVAChT-PC12 cell
The affinity of these vesamicol analogs for VAChT,
σ 1, and
σ 2 had not been reported.
The affinity of vesamicol, as a reference, for VAChT,
σ 1, and
σ 2 was not investigated by the same in vitro binding assay method.
