In Vivo and In Vitro Characteristics of Radiolabeled Vesamicol Analogs as the Vesicular Acetylcholine Transporter Imaging Agents

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 P_o/w = log₁₀ (radioactivity in n-octanol/radioactivity in 0.1 M phosphate buffer (pH = 7.4)).