title: Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 5: 2'-Substituted 6-nitroquipazines.
abstract: Five C2'-substituted 6-nitroquipazine (6-NQ) derivatives were prepared and evaluated in terms of their biological abilities (K(i)) to displace [(3)H]citalopram binding to serotonin transporter. The relationship between their structure and biological activities revealed that shorter alkyl groups tend to possess higher binding affinity. Both compounds 12a and 12c were found to have the equally highest binding affinity (K(i)=0.43+/-0.02 nM).
authors: Department of Chemistry, Inha University, 253 Yonghyundong, Namgu, Inchon 402-751, Republic of Korea.
authors: Jae Hak
authors: JH
authors: Lee
authors: Yong Hyun
authors: YH
authors: Choi
authors: Yoo Jin
authors: YJ
authors: Lim
authors: Byoung Se
authors: BS
authors: Lee
authors: Dae Yoon
authors: DY
authors: Chi
authors: Changbae
authors: C
authors: Jin
mesh_terms: D000818:Animals; D002855:Chromatography, Thin Layer; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D008297:Male; D013058:Mass Spectrometry; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry; D011814:Quipazine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D050486:Serotonin Plasma Membrane Transport Proteins / Q000187:drug effects / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013570:Synaptic Membranes / Q000187:drug effects / Q000378:metabolism
chemical_list: D007202:Indicators and Reagents; D010879:Piperazines; D050486:Serotonin Plasma Membrane Transport Proteins; D000077489:Piperazine; D011814:Quipazine; C031227:6-nitroquipazine