Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1.
6-Nitroquipazine has been known as one of the most potent and selective inhibitors of serotonin transporter in vitro and in vivo. Nine derivatives of 6-nitroquipazine were synthesized and tested for their potential abilities to displace [3H]citalopram binding to the rat cortical membranes.
Lee
B S
BS
Department of Chemistry, Inha University, Inchon, South Korea.
Chu
S
S
Lee
B C
BC
Chi
D Y
DY
Choe
Y S
YS
Jeong
K J
KJ
Jin
C
C
D000818:Animals; D001667:Binding, Competitive; D002352:Carrier Proteins / Q000378:metabolism*; D002462:Cell Membrane / Q000378:metabolism; D002540:Cerebral Cortex / Q000378:metabolism; D015283:Citalopram / Q000493:pharmacokinetics; D015195:Drug Design; D007202:Indicators and Reagents; D007700:Kinetics; D008562:Membrane Glycoproteins / Q000378:metabolism*; D026901:Membrane Transport Proteins; D008961:Models, Structural; D008968:Molecular Conformation; D009419:Nerve Tissue Proteins; D011814:Quipazine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D013329:Structure-Activity Relationship
D002352:Carrier Proteins; D015283:Citalopram; D007202:Indicators and Reagents; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D011814:Quipazine; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors; C493232:Slc6a4 protein, rat; C031227:6-nitroquipazine