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Title: | Towards the development of new subtype-specific muscarinic receptor radiopharmaceuticals-radiosynthesis and ex vivo biodistribution of [18F] 3-(4-(2-(2-(2-fluoroethoxy) ethoxy) ethylthio)-1, 2, 5-thiadiazol-3-yl)-1-methyl-1, 2, 5, 6-tetrahydropyridine |
Authors: | van Oosten, Erik M. Wilson, Alan A. Mamo, David Pollock, Bruce G. Mulsant, Benoit H. Houle, Sylvain Vasdev, Neil |
Keywords: | Muscarinic receptors Tomography, Emission |
Issue Date: | 2010 |
Publisher: | N R C Research Press |
Citation: | van Oosten, E. M., Wilson, A. A., Mamo, D. C., Pollock, B. G., Mulsant, B. H., Houle, S., & Vasdev, N. (2010). Towards the development of new subtype-specific muscarinic receptor radiopharmaceuticals—Radiosynthesis and ex vivo biodistribution of [18F] 3-(4-(2-(2-(2-fluoroethoxy) ethoxy) ethylthio)-1, 2, 5-thiadiazol-3-yl)-1-methyl-1, 2, 5, 6-tetrahydropyridine. Canadian Journal of Chemistry, 88(12), 1222-1232. |
Abstract: | Muscarinic receptors have been implicated in neurological disorders including Alzheimer’s disease, Parkinson’s disease, and schizophrenia. Nineteen derivatives of thiadiazolyltetrahydropyridine (TZTP), a core that has previously shown high affinities towards muscarinic receptor subtypes, were synthesized and evaluated via in vitro binding assays. The title compound, a fluoro-polyethyleneglycol analog of TZTP (4c), was subsequently labelled with fluorine-18. Fluorine-18-labelled 4c was produced, via an automated synthesis, in an average radiochemical yield of 36% (uncorrected for decay), with high radiochemical purity (>99%) and high specific activity (326 GBq/µmol; end-of-bombardment), within 40 min (n = 3). Ex vivo biodistribution studies following tail-vein injection of [18F]4c in conscious rats displayed sufficient brain uptake (0.4%–0.7% injected dose / gram of wet tissue in all brain regions at 5 min post injection); however, there were substantial polar metabolites present in the brain, thereby precluding future use of [18F]4c for imaging in the central nervous system. |
URI: | https://www.um.edu.mt/library/oar//handle/123456789/23717 |
Appears in Collections: | Scholarly Works - FacM&SPsy |
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File | Description | Size | Format | |
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Towards_the_development_of_new_subtype-specific_mu.pdf | 435.94 kB | Adobe PDF | View/Open |
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