SYNTHESIS AND BIOLOGICAL ACTIVITIES OF NEW 5-HT2A SELECTIVE LIGANDSN-SUBSTITUTED-PIPERIDINYL4-PHENYLTHIOETHER AND SULFONE DERIVATIVES / 药学学报
Acta Pharmaceutica Sinica
;
(12): 274-277, 2001.
Article
in Chinese
| WPRIM
| ID: wpr-410644
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.
Full text:
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Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2001
Type:
Article
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