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.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-07, Vol.10 (14), p.1559-1562
Hauptverfasser:	Lee, Byoung Se, Chu, Soyoung, Lee, Byung Chul, Chi, Dae Yoon, Choe, Yearn Seong, Jeong, Kyung Ja, Jin, Changbae
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding, Competitive Biological and medical sciences Carrier Proteins - metabolism Cell Membrane - metabolism Cerebral Cortex - metabolism Citalopram - pharmacokinetics Drug Design Indicators and Reagents Kinetics Medical sciences Membrane Glycoproteins - metabolism Membrane Transport Proteins Models, Structural Molecular Conformation Nerve Tissue Proteins Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Quipazine - analogs & derivatives Quipazine - chemical synthesis Quipazine - chemistry Quipazine - pharmacokinetics Quipazine - pharmacology Rats Serotonin Plasma Membrane Transport Proteins Serotonin Uptake Inhibitors - chemical synthesis Serotonin Uptake Inhibitors - chemistry Serotonin Uptake Inhibitors - pharmacokinetics Serotoninergic system Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00290-0