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Synthesis of heteroarylpiperazines and heteroarylbipiperidines with a restricted side chain and their affinities for 5-HT1A receptor

Authors
Yoo K.H.Choi H.S.Kim D.C.Shin K.J.Kim D.J.Song Y.S.Jin C.
Issue Date
Jul-2003
Publisher
John Wiley & Sons Ltd.
Keywords
5-HT1A receptor affinities; Heteroarylbipiperidines; Heteroarylpiperazines; Restricted side chain
Citation
Archiv der Pharmazie, v.336, no.4-5, pp.208 - 215
Journal Title
Archiv der Pharmazie
Volume
336
Number
4-5
Start Page
208
End Page
215
URI
https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/149122
DOI
10.1002/ardp.200300721
ISSN
0365-6233
Abstract
Heteroarylpiperazine and heteroarylbipiperidine derivatives, bearing a 4-piperidine ring instead of an alkylamino side chain to give the semi-rigidity, were prepared and evaluated for their abilities to displace [3H] 8-OH-DPAT binding to the rat hippocampal synaptic membranes. These compounds showed low to moderate affinities for 5-HT1A receptor, with Ki values ranging from 6912 nM to 232 nM. Of these compounds, 8 b and 15 e exhibited the best affinities for 5-HT1A receptor with Ki values of 232 nM and 338 nM, respectively.
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