Premium
Synthesis of Heteroarylpiperazines and Heteroarylbipiperidines with a Restricted Side Chain and Their Affinities for 5‐HT 1A Receptor
Author(s) -
Yoo Kyung Ho,
Choi Hyun Sik,
Kim Dong Chan,
Shin Kye Jung,
Kim Dong Jin,
Song Yun Seon,
Jin Changbae
Publication year - 2003
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200300721
Subject(s) - affinities , chemistry , piperidine , stereochemistry , 5 ht1a receptor , side chain , binding affinities , receptor , 5 ht receptor , biochemistry , serotonin , organic chemistry , polymer
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 [ 3 H]8‐OH‐DPAT binding to the rat hippocampal synaptic membranes. These compounds showed lowto moderate affinities for 5‐HT 1A receptor, with Ki values ranging from 6912 nMto 232 nM. Of these compounds, 8b and 15e exhibited the best affinities for 5‐HT 1A receptor with Ki values of 232 nM and 338 nM, respectively.