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- W2024472772 abstract "The unsaturated HHSiD (1) and p-F-HHSiD (2) derivatives (E)-cyclohexyl(phenyl)(3-piperidino-1-propen-1-yl)silanol (5, isolated as 5 · HCl) and (E)-cyclohexyl(4-fluorophenyl)(3-piperidino-1-propen-1-yl)silanol (6, isolated as 6 · HCl) were synthesized in four steps, starting from (CH3O)3SiH. Reaction of 5 and 6 with CH3Cl gave the corresponding methochlorides 7 and 8, respectively. All compounds were obtained as racemic mixtures. The binding affinities at muscarinic receptor subtypes (M1–M4) of the silanols 5–8 were determined and compared with those of the selective muscarinic antagonists 1 and 2 and their methiodides 3 and 4. These studies demonstrated that the ammonium compounds 3, 4, 7 and 8 display similar binding affinities at M1–M4 receptors and comparable receptor subtype selectivities. On the other hand, the conformationally restricted amines 5 and 6 ((E)SiCHCHCH2N moiety) exhibit higher affinities but lower receptor subtype selectivities than the more flexible parent compounds 1 and 2 SiCH2CH2CH2N moiety)." @default.
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- W2024472772 date "1995-12-01" @default.
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- W2024472772 title "Unsaturated derivatives of the muscarinic antagonists hexahydro-sila-difenidol (HHSiD) and p-fluoro-hexahydro-sila-difenidol (p-F-HHSiD) with an (E)-SiCHCHCH2rmN moiety: Syntheses and binding affinities at muscarinic receptor subtypes" @default.
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- W2024472772 doi "https://doi.org/10.1016/0022-328x(95)05584-7" @default.
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