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  • Title: [Synthesis and biological activities of new 5-HT2A selective ligands--N-substituted-piperidinyl-4-phenylthioether and sulfone derivatives].
    Author: Wang H, Wen R, Huang L, Bi R, Tan PZ.
    Journal: Yao Xue Xue Bao; 2001 Apr; 36(4):274-7. PubMed ID: 12580055.
    Abstract:
    AIM: 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. METHODS: 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. RESULTS: 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. CONCLUSION: Some sulfur containing analogues of MDL 100907 showed selective affinity to 5-HT2A receptor and are worth further study.
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