Table 2.
Accumulation of vesamicol analogs (1–22) in the striatum and cortex and the ratio of the striatum to cortex (ST/CTX) for radiolabeled vesamicol analogs accumulation.
| %ID/g | ST/CTX | Animal | Molecular weight | Partition coefficient | ||
|---|---|---|---|---|---|---|
| Cortex | Striatum | |||||
| [3H]vesamicol [74] | 0.68 (60 min) | 0.74 (60 min) | 1.09 (60 min) | Rats | 259 | 1.40∗ |
| Benzovesamicol | — | — | — | — | 307 | 2.44∗ |
| [123I]IBVM (1) [37, 42] | 2.56 (240 min) | 6.26 (240 min) | 2.45 (240 min) | Mice | 429 | — |
| 0.3 (120 min) | 0.53 (120 min) | 1.77 (120 min) | Rats | — | ||
| (−)-[18F]FEOBV (2) [46] | 4.65 (45 min) | 8.09 (45 min) | 1.74 (45 min) | Mice | 368 | — |
| (−)-[11C]MABV (3) [48] | 3.99 (45 min) | 8.1 (45 min) | 2.6 (75 min) | Mice | 336 | — |
| (−)-[18F]NEFA (4) [49] | — | — | 2.5–3 (50 min) | Monkeys | 406 | — |
| (+)-[125I]MIBT (8) [56] | 0.40 (120 min) | 0.67 120 min) | 1.68 (120 min) | Rats | 474 | — |
| (+)-[18F]FBT (9) [72] | 0.58 (60 min) | 0.74 (60 min) | 1.28 (60 min) | Rats | 367 | 1.99∗ |
| (−)-[125I]oIV (10) [74] | 1.55 (60 min) | 1.57 (60 min) | 1.01 (60 min) | Rats | 383 | 2.15∗∗ |
| (−)-[11C]OMV (11) [75] | 1.16 (30 min) | 1.07 (30 min) | 0.92 (30 min) | Rats | 272 | — |
| 3′-[125I]IBVM (12) [64] | 0.38 (60 min) | 0.61 (60 min) | 1.61 (60 min) | Rats | 431 | — |
| (−)-[123I]OIDV (13) [66] | 0.62 (30 min) | 0.63 (30 min) | 1.02 (30 min) | Rats | 435 | 2.46∗∗ |
| [77Br]OBDV (14) [67] | 0.52 (30 min) | 0.59 (30 min) | 1.13 (30 min) | Rats | 389 | 2.93∗∗ |
| [11C]OMDV (15) [68] | 0.57 (60 min) | 0.72 (60 min) | 1.26 (60 min) | Rats | 326 | 2.37∗∗ |
| [18F]FAMV (16) [69] | — | — | 4.5 (60 min) | Rats | 361 | 1.88 |
| [18F]FBMV (17) [70] | 0.09 (60 min) | 0.17 (60 min) | 3.4 (60 min) | Rats | 423 | 2.10 |
| (−)-[18F]FBBV (18) [71] | — | — | 1.36 (60 min) | Rats | 352 | 2.99∗ |
| (−)-[11C]19 [80] | 0.331 (30 min) | 0.546 (30 min) | 1.65 (30 min) | Rats | 364 | — |
| (−)-[11C]TZ659 (20) [81] | 0.262 (30 min) | 0.593 (30 min) | 2.26 (30 min) | Rats | 363 | 2.61∗ |
| (−)-[18F]VAT (21) [83] | — | — | 4.19 (60 min) | Rats | 414 | 3.45∗ |
| (−)-[18F]22 [84] | — | — | 1.76 (60 min) | Monkeys | 395 | 2.91∗ |
∗Calculated value (Log P) at pH 7.4 by ACD/Laboratories, version 7.0 (Advanced Chemistry Development, Inc., Canada). ∗∗Log Po/w = log10 (radioactivity in n-octanol/radioactivity in 0.1 M phosphate buffer (pH = 7.4)).