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Synthesis and biological activities of new 5-HT2A selective ligands--N-substituted-piperidinyl-4-phenylthioether and sulfone derivatives

Wang, H.; Wen, R.; Huang, L.; Bi, R.; Tan, P.Z.

Yao Xue Xue Bao 36(4): 274-277

2001

ISSN/ISBN: 0513-4870
PMID: 12580055
Document Number: 536706
A series of 4-piperidinylthioether and sulfone derivatives of 4-[1-hydroxy-1-(2,3-dimethoxyphenyl) methyl]-N-2-(4-fluorophenylethyl) piperidine (MDL 100907) were synthesized in order to find new 5-HT2A selective ligands. Title compounds 2a-2c were synthesized from 2, 3-dimethoxythiophenol and tested for their affinities to 5-HT2A, 5-HT2C, 5-HT6 and 5-HT7 receptors and some other nervous transmitter receptors in vitro. Compounds 2a-2c are new compounds. The results of the binding assay demonstrated that they have relatively high selectivity for 5-HT2A receptor in vitro. Some sulfur containing analogues of MDL 100907 showed selective affinity to 5-HT2A receptor and are worth further study.

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