p-[18F]fluorobenzyltrozamicol ([18F]FBT): Molecular decomposition-reconstitution approach to vesamicol receptor radioligands for positron emission tomography

The potential ofo-bromo-trans-decalinvesamicol as a new PET ligand for vesicular acetylcholine transporter imaging

“…However, additional moderate to high affinity for sigma-1 (r 1 ) and sigma-2 (r 2 ) receptors (Efange et al, 1995) (DeGrado et al, 1994;Mulholland et al, 1998) (Jung et al, 1990;Sorger et al, 2000) and trozamicol, e.g. [ (Efange et al, 1994;Gage et al, 2000;Mach et al, 1997;Voytko et al, 2001), [ 123/125 I]MIBT (Efange et al, 1993Staley et al, 1997) (Fig. 1).…”

Enhanced Cholinergic Response in Pancreata of Nonhuman Primates with Impaired Glucose Tolerance Shown on [18F]Fluorobenzyltrozamicol Positron Emission Tomography

“…[ 18 F]FBT was synthesized as previously described. 14,17 Approximately 5 mCi of [ 18 F]FBT was injected intravenously into each subject. Each PET scan was acquired in a dynamic fashion from time of injection through 90 min post-injection.…”

Cholinergic activity of aged rhesus monkeys revealed by positron emission tomography

“…Vesamicol (and its analogs) noncompetitively inhibits the transport of ACh into synaptic vesicles from a variety of sources (reviewed in Parsons et al, 1993). Accordingly, a number of studies have revealed that the in vitro distribution of (Ϫ)-[ 3 H]vesamicol (Altar and Marien, 1988;Marien et al, 1987) and the in vivo distribution of many radiolabeled vesamicol analogs (Efange et al, 1994(Efange et al, , 1995Ingvar et al, 1993;Kuhl et al, 1994;Mach et al, 1997) is consistent with patterns of cholinergic innervation delineated by choline acetyltransferase (Kuczenski et al, 1975;Levey et al, 1983;Satoh et al, 1983;Stavinoha et al, 1974) and [ 3 H]hemicholinium-3 (Quirion, 1987). Moreover, the inhibitory action of vesamicol appears to be selective for recycling vesicles (Melega and Howard, 1984;Ricny and Whittaker, 1993;Toll and Howard, 1980).…”

“…Recently, we began a series of functional imaging studies, using positron emission tomography (PET) and the potent VAChT ligand and vesamicol analog (ϩ)-4-[ 18 F]fluorobenzyltrozamicol ((ϩ)-[ 18 F]FBT) (Efange et al, 1994) to examine the VAChT in monkeys. In our initial studies, we demonstrated that (ϩ)-[ 18 F]FBT has an appropriate binding profile for use in PET studies of the VAChT in primates (Mach et al, 1997) and has a low test-retest variability profile (Gage et al, 1998).…”