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).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Chromatography, Thin Layer
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In Vitro Techniques
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Indicators and Reagents
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Male
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Mass Spectrometry
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Piperazine
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Piperazines / chemistry
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Quipazine / analogs & derivatives*
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Quipazine / chemical synthesis
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Quipazine / pharmacology
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Rats
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Rats, Sprague-Dawley
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Serotonin Plasma Membrane Transport Proteins / drug effects
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Serotonin Plasma Membrane Transport Proteins / metabolism*
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Structure-Activity Relationship
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Synaptic Membranes / drug effects
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Synaptic Membranes / metabolism
Substances
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Indicators and Reagents
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Piperazines
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Serotonin Plasma Membrane Transport Proteins
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Piperazine
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Quipazine
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6-nitroquipazine