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


CONCLUSIONS
Some sulfur containing analogues of MDL 100907 showed selective affinity to 5-HT2A receptor and are worth further study.
Wang
H
H
Department of Medicinal Chemistry of Fudan University, Shanghai 200032, China.
Wen
R
R
Huang
L
L
Bi
R
R
Tan
P Z
PZ
D000818:Animals; D005464:Fluorobenzenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D066298:In Vitro Techniques; D008024:Ligands; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D044402:Receptor, Serotonin, 5-HT2A; D011985:Receptors, Serotonin / Q000737:chemistry*; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D005464:Fluorobenzenes; D008024:Ligands; D010880:Piperidines; D044402:Receptor, Serotonin, 5-HT2A; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; C079049:volinanserin