Radioiodinated 2-hydroxy-3-(4-iodophenyl)-1-(4-phenylpiperidinyl)propane: Potential radiotracer for mapping central cholinergic innervation in vivo

S.M.N. Efange1, A.K. Dutta1, R.H. Michelson1, H.F. Kung2, J.R. Thomas1, J. Billings2, R.J. Boudreau1
1Departments of Radiology and Medicinal Chemistry, University of Minnesota, Minneapolis, MN 55455, U.S.A.
2Department of Radiology, Hospital of the University of Pennsylvania, Philadelphia, PA 19104, U.S.A.

Tài liệu tham khảo

Altar, 1988, [3H]Vesamicol binding in brain: autoradiographic distribution, pharmacology, and effects of cholinergic lesions, Synapse, 2, 486, 10.1002/syn.890020504 Bowen, 1983, Biochemical assessment of serotonergic and cholinergic dysfunction and cerebral atrophy in Alzheimer's disease, J. Neurochem., 41, 226, 10.1111/j.1471-4159.1983.tb11838.x Brittain, 1969, The neuromuscular blocking action of 2-(4-phenylpiperidino)cyclohexanol (AH5183), Eur. J. Pharmacol., 8, 93, 10.1016/0014-2999(69)90133-2 Efange, 1991, Acyclic analogs of 2-(4-phenylpiperidino)cyclohexanol (vesamicol): conformationally mobile inhibitors of vesicular acetylcholine transport, J. Med. Chem., 34, 2638, 10.1021/jm00112a044 Jones, 1970, Electronic effects in solvolysis reactions. III. Solvolysis of allyl-substituted cumyl derivatives, J. Org. Chem., 35, 1777, 10.1021/jo00831a013 Jung, 1990, A radiotracer for mapping cholinergic neurons of the brain, J. Med. Chem., 33, 2065, 10.1021/jm00170a002 Kaufman, 1989, Fractional vesamicol receptor occupancy and acetylcholine active transport inhibition in synaptic vesicles, Molec. Pharmacol., 36, 452 Kornreich, 1988, Sideness and chemical and kinetic properties of the vesamicol receptor of cholinergic synaptic vesicles, Biochemistry, 27, 5262, 10.1021/bi00414a047 Marien, 1987, Quantitative autoradiography of brain binding sites for the vesicular acetylcholine transport blocker 2-(4-phenyl-piperidino)cyclohexanol (AH 5183), 84, 876 Marshall, 1987, The vesicular acetylcholine transport system, TINS, 10, 174 Mountjoy, 1984, Correlation of cortical cholinergic and GABA deficits with quantitative neuropathological findings in senile dementia, Brain, 107, 507, 10.1093/brain/107.2.507 Parsons, 1987, Acetylcholine transport: fundamental properties and effects of pharmacologic agents, Ann. N. Y. Acad. Sci., 493, 220, 10.1111/j.1749-6632.1987.tb27203.x Reisine, 1978, Pre- and postsynaptic neurochemical alterations in Alzheimer's disease, Brain Res., 159, 477, 10.1016/0006-8993(78)90562-0 Rogers, 1990, Very high-affinity analogs of vesamicol, an acetylcholine storage inhibitor, Neuroreport, 1, 11 Rogers, 1989, Synthesis, in vitro acetylcholine-storage-blocking activities, and biological properties of derivatives and analogues of trans-2-(4-phenylpiperidino) cyclohexanol (Vesamicol), J. Med. Chem., 32, 1217, 10.1021/jm00126a013 Rossor, 1982, A post-mortem study of the cholinergic and GABA systems in senile dementia, Brain, 105, 313, 10.1093/brain/105.2.313