TY - JOUR
T1 - Synthesis and biological characterization of stable and radioiodinated (±)-trans-2-hydroxy-3-P{4-(3-iodophenyl)piperidyl}-1,2,3,4-tetrahyd ronaphthalene (3′-IBVM)
AU - Efange, S. M.N.
AU - Von Hohenberg, K.
AU - Khare, A. B.
AU - Tu, Z.
AU - Mach, R. H.
AU - Parsons, Stanley M.
N1 - Funding Information:
Financial support for these studies was provided by the National Institutes of Health under grant no. AG13621 (SMNE).
PY - 2000
Y1 - 2000
N2 - The vesamicol analogue (±)-trans-2-Hydroxy-3-{4-(3-iodophenyl)piperidyl}-1,2,3,4-tetrahydr onaphthalene (3′-IBVM), a potent ligand for the vesicular acetylcholine transporter (VAChT), was evaluated as a potential radiotracer for studying VAChT density in vivo. In radioligand binding experiments, 3′-IBVM displays subnanomolar affinity for VAChT and 100-fold selectivity for VAChT over σ1 and σ2 receptors. Consistent with this profile, radioiodinated (±)-3′-IBVM distributed heterogenously in the rat brain following a bolus IV injection, displaying high concentrations in the striatum and moderate to low concentrations in the cortex and cerebellum, respectively. However, co-injection of the radiotracer with the sigma ligand haloperidol resulted in significant reductions of radiotracer levels in all brain regions examined. Therefore, radioiodinated (±)-IBVM appears to bind to both VAChT and sigma receptors in vivo.
AB - The vesamicol analogue (±)-trans-2-Hydroxy-3-{4-(3-iodophenyl)piperidyl}-1,2,3,4-tetrahydr onaphthalene (3′-IBVM), a potent ligand for the vesicular acetylcholine transporter (VAChT), was evaluated as a potential radiotracer for studying VAChT density in vivo. In radioligand binding experiments, 3′-IBVM displays subnanomolar affinity for VAChT and 100-fold selectivity for VAChT over σ1 and σ2 receptors. Consistent with this profile, radioiodinated (±)-3′-IBVM distributed heterogenously in the rat brain following a bolus IV injection, displaying high concentrations in the striatum and moderate to low concentrations in the cortex and cerebellum, respectively. However, co-injection of the radiotracer with the sigma ligand haloperidol resulted in significant reductions of radiotracer levels in all brain regions examined. Therefore, radioiodinated (±)-IBVM appears to bind to both VAChT and sigma receptors in vivo.
KW - Acetylcholine transporter
KW - Synaptic vesicles
KW - Vesamicol analogue
UR - http://www.scopus.com/inward/record.url?scp=0034528043&partnerID=8YFLogxK
U2 - 10.1016/S0969-8051(00)00157-8
DO - 10.1016/S0969-8051(00)00157-8
M3 - Article
C2 - 11150707
AN - SCOPUS:0034528043
VL - 27
SP - 749
EP - 755
JO - Nuclear Medicine and Biology
JF - Nuclear Medicine and Biology
SN - 0969-8051
IS - 8
ER -