Synthesis of heteroarylpiperazines and heteroarylbipiperidines with a restricted side chain and their affinities for 5-HT1A receptor.
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 low to moderate affinities for 5-HT(1A) receptor, with Ki values ranging from 6912 nM to 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.
Yoo
Kyung Ho
KH
Division of Life Sciences, Korea Institute of Science and Technology, Seoul 130-650, Korea. khyoo@kist.re.kr
Choi
Hyun Sik
HS
Kim
Dong Chan
DC
Shin
Kye Jung
KJ
Kim
Dong Jin
DJ
Song
Yun Seon
YS
Jin
Changbae
C
D000818:Animals; D002462:Cell Membrane / Q000378:metabolism; D006624:Hippocampus / Q000166:cytology / Q000378:metabolism; D066298:In Vitro Techniques; D008024:Ligands; D008297:Male; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D011985:Receptors, Serotonin / Q000378:metabolism*; D044263:Receptors, Serotonin, 5-HT1; D013329:Structure-Activity Relationship
D008024:Ligands; D010879:Piperazines; D010880:Piperidines; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1