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Synthesis and 5-hydroxytryptamine antagonist activity of 2-[[2-(dimethylamino) ethyl] thio]-3-phenylquinoline and its analogs

TP Blackburn, B Cox, AJ Guildford…

文献索引:Blackburn, Thomas P.; Cox, Barry; Guildford, Allen J.; Count, David J. Le; Middlemiss, Derek N.; et al. Journal of Medicinal Chemistry, 1987 , vol. 30, # 12 p. 2252 - 2259

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被引用次数: 29

摘要

A series of 2-[(2-aminoethyl) thio] quinolines substituted at the 3-position with alkyl, aryl, or heteroaryl groups has been prepared in the search for novel and selective 5-HT2 antagonists. The affinity of the compounds for 5-HT1 receptor sites was measured by their ability to displace [3H]-5-HT from rat brain synaptosomes whereas the affinity for 5-HT2 receptor sites was measured by their ability to displace [3H] spiperone from synaptosomes ...

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