Synthesis, crystal structure analysis, and pharmacological characterization of desmethoxy-sila-venlafaxine, a derivative of the serotonin/noradrenaline reuptake inhibitor sila-venlafaxine |
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Authors: | Jürgen O Daiß John S Mills Graham A Showell Reinhold Tacke |
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Institution: | a Institut für Anorganische Chemie, Universität Würzburg, Am Hubland, D-97074 Würzburg, Germany b Paradigm Therapeutics Ltd., 162 Cambridge Science Park, Milton Road, Cambridge CB4 0GP, UK |
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Abstract: | rac-Desmethoxy-sila-venlafaxine (rac-3) is a derivative of the noradrenaline-selective serotonin/noradrenaline reuptake inhibitor rac-sila-venlafaxine (rac-1b), a silicon analogue of the serotonin-selective serotonin/noradrenaline reuptake inhibitor rac-venlafaxine (rac-1a) (rac-1a, rac-1-2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexan-1-ol; rac-1b, rac-1-2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]-1-silacyclohexan-1-ol). The synthesis and crystal structure analyses of rac-3 and rac-3 · HCl are reported, and the pharmacological properties of rac-1a, rac-1b, rac-2 (a sila-venlafaxine derivative with a silacyclopentanol skeleton instead of a silacyclohexanol framework), and rac-3 are compared (comparison of the pharmacological selectivity profiles with respect to serotonin, noradrenaline, and dopamine reuptake inhibition). |
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Keywords: | Sila-venlafaxine Silicon Silicon-based drugs Serotonin/noradrenaline reuptake inhibitor Structure-activity relationships Venlafaxine |
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