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Nuclear Medicine and Biology
Volume 35, Issue 2
, Pages 185-195
, February 2008
A new 18F-labeled fluoroacetylmorpholino derivative of vesamicol for neuroimaging of the vesicular acetylcholine transporter
References
- . The significance of the cholinergic system in the brain during aging and in Alzheimer's disease. J Neural Transm. 2006;113:1625–1644
- . Towards a unifying hypothesis of Alzheimer's disease: cholinergic system linked to plaques, tangles and neuroinflammation. Curr Med Chem. 2006;13:2179–2188
- . Alzheimer's disease and senile dementia: loss of neurons in the basal forebrain. Science. 1982;215:1237–1239
- Chemical pathology of organic dementias. I. Validity of biochemical measurements on human post-mortem brain specimens. Brain. 1977;100:397–426
- . Nucleus basalis neuronal loss, neuritic plaques and choline acetyltransferase activity in advanced Alzheimer's disease. Neuroscience. 1986;19:1279–1291
- . The 12th J. A. F. Stevenson memorial lecture. Aging, Alzheimer's disease, and the cholinergic system. Can J Physiol Pharmacol. 1984;62:741–754
- . The cholinergic gene locus. J Neurochem. 1998;70:2227–2240
- Functional identification of a vesicular acetylcholine transporter and its expression from a "cholinergic" gene locus. J Biol Chem. 1994;269:21929–21932
- . Analysis of uptake and release of newly synthesized acetylcholine in PC12 cells overexpressing the rat vesicular acetylcholine transporter (VAChT). Brain Res Mol Brain Res. 2002;100:21–30
- The cholinergic locus: ChAT and VAChT genes. J Physiol Paris. 1998;92:145–147
- . Autoradiographic comparison of [3H](−)nicotine, [3H]cytisine and [3H]epibatidine binding in relation to vesicular acetylcholine transport sites in the temporal cortex in Alzheimer's disease. Neuroscience. 1999;94:685–696
- Reduction of vesicular acetylcholine transporter in beta-amyloid protein-infused rats with memory impairment. Nucl Med Commun. 2000;21:933–937
- . [3H]Vesamicol binding in brain: autoradiographic distribution, pharmacology, and effects of cholinergic lesions. Synapse. 1988;2:486–493
- . Quantitative autoradiography of brain binding sites fore the vesicular acetylcholine transport blocker 2-(4-phenylpiperidino)cyclohexanol (AH5183). Proc Natl Acad Sci. U S A. 1987;84:876–880
- . Acetylcholine transporter — vesamicol receptor pharmacology and structure. Prog Brain Res. 1993;98:175–181
- Synthesis, in vitro acetylcholine-storage-blocking activities, and biological properties of derivatives and analogues of trans-2-(4-phenylpiperidino)cyclohexanol (Vesamicol). J Med Chem. 1989;32:1217–1230
- . Selective antibody-induced cholinergic cell and synapse loss produce sustained hippocampal and cortical hypometabolism with correlated cognitive deficits. Exp Neurol. 2001;170:36–47
- In vivo [125I]-iodobenzovesamicol binding reflects cortical cholinergic deficiency induced by specific immunolesion of rat basal forebrain cholinergic system. Nucl Med Biol. 2000;27:23–31
- Decreased vesicular acetylcholine transporter and alpha(4)beta(2) nicotinic receptor density in the rat brain following 192 IgG-saporin immunolesioning. Neurosci Lett. 2007;415:97–101
- [3H]Vesamicol binding in human brain cholinergic deficiency disorders. Neurosci Lett. 1990;117:347–352
- Choline acetyltransferase activity and [3H]Vesamicol binding in the temporal cortex of patients with Alzheimer's disease, Parkinson's disease, and rats with basal forebrain lesions. Neuroscience. 1990;35:327–333
- . Vesicular acetylcholine transporter density and Alzheimer's disease. Neurobiol Aging. 1997;18:407–413
- In vivo mapping of cholinergic neurons in the human brain using SPECT and IBVM. J Nucl Med. 1993;35:405–410
- In vivo mapping of cholinergic terminals in normal aging. Alzheimer's disease and Parkinson's disease. Ann Neurol. 1996;40:399–410
- . The application of positron-emitting molecular imaging tracers in Alzheimer's disease. Mol Imaging Biol. 2007;9:204–216
- . Vesamicol and some of its derivatives: questionable ligands for selectively labelling acetylcholine transporters in rat brain. Eur J Pharmacol. 1997;338:177–183
- Vesamicol analogues as sigma ligands. Molecular determinants of selectivity at the vesamicol receptor. Biochem Pharmacol. 1995;49:791–797
- Piperazine analog of vesamicol: in vitro and in vivo characterization for vesicular acetylcholine transporter. Synapse. 2000;38:27–37
- Synthesis and evaluation of radiolabeled piperazine derivatives of vesamicol as SPECT agents for cholinergic neurons. Nucl Med Biol. 2001;28:251–260
- . Synthesis and biological characterization of stable and radioiodinated (+/−)-trans-2-hydroxy-3-P[4-(3-iodophenyl)piperidyl]-1,2,3,4-tetrahydronaphthalene (3'-IBVM). Nucl Med Biol. 2000;27:749–755
- Synthesis of novel 4- and 5-substituted benzyl ether derivatives of vesamicol and in vitro evaluation of their binding properties to the vesicular acetylcholine transporter site. Bioorg Med Chem. 2004;12:1459–1465
- . Synthesis and binding affinities of methylvesamicol analogs for the acetylcholine transporter and sigma receptor. Bioorg Med Chem. 2006;14:2620–2626
- Structural changes of benzylether derivatives of vesamicol and their influence on the binding selectivity to the vesicular acetylcholine transporter. Eur J Med Chem. 2005;40:1197–1205
- Synthesis and in vitro evaluation of new benzovesamicol analogues as potential imaging probes for the vesicular acetylcholine transporter. Bioorg Med Chem. 2005;13:745–753
- Sequential ring-opening of trans-1,4-cyclohaxadiene dioxide for an expedient modular approach to 6,7-disubstituted (±) hexahydro-benzo [1,4]oxazin-3-ones. Tetrahedron Lett. 2007;48:5497–5501
- . Hydroxylated decahydroquinolines as ligands for the vesicular acetylcholine transporter: synthesis and biological evaluation. J Med Chem. 1999;42:2862–2869
- . 18F-labelled vesamicol derivatives: Syntheses and preliminary in vivo small animal Positron Emission Tomography evaluation. Nucl Med Biol. 1994;21:219–230
- . Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50% inhibition (IC50) of an enzymatic reaction. Biochem Pharmacol. 1973;22:3099–3108
- Molecular cloning of a putative vesicular transporter for acetylcholine. Proc Natl Acad Sci U S A. 1994;91:10620–10624
- . Synthesis and structure-activity relationships of N-(1-benzylpiperidin-4-yl)arylacetamide analogues as potent sigma1 receptor ligands. J Med Chem. 2001;44:4404–4415
- . Vesicular acetylcholine transporter (VAChT) protein: a novel and unique marker for cholinergic neurons in the central and peripheral nervous systems. J Comp Neurol. 1997;378:454–467
- . Studies on the blocking action of 2-(4-phenyl piperidino) cyclohexanol (AH5183). Br J Pharmacol. 1970;38:503–516
- . Brain radioligands — state of the art and new trends. Q J Nucl Med. 2001;45:139–152
- [18F]fluoroethoxy-benzovesamicol, a PET radiotracer for the vesicular acetylcholine transporter and cholinergic synapses. Synapse. 1998;30:263–274
- . Is fluoroacetate-specific defluorinase a glutathione S-transferase?. Comp Biochem Physiol C Toxicol Pharmacol. 2006;143:59–66
- . Glutathione S-transferase isoenzymes in rat brain neurons and glia. J Neurosci. 1993;13:2013–2023
☆ This work was supported by a grant from Sächsisches Ministerium für Wissenschaft und Kunst, contract no. 7531.50-03-0361-01/6.
PII: S0969-8051(07)00252-1
doi: 10.1016/j.nucmedbio.2007.10.004
© 2008 Elsevier Inc. All rights reserved.
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Nuclear Medicine and Biology
Volume 35, Issue 2
, Pages 185-195
, February 2008
