Serotonin transporter inhibitors: synthesis and binding potency of 2′-methyl- and 3′-methyl-6-nitroquipazine

Racemic 2′-methyl- and 3′-methyl-6-nitroquipazine ligands were selected as targets, synthesized and evaluated at the serotonin transporter employing an in vitro competitive inhibition assay with [ 3H]paroxetine and rat cortical membrane. The 2′-methyl-6-nitroquipazine was found to be 50 times more p...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-12, Vol.10 (23), p.2643-2646
Main Authors: Gerdes, John M, DeFina, Steven C, Wilson, Paul A, Taylor, Scott E
Format: Article
Language:English
Subjects:
Animals
Binding, Competitive
Biological and medical sciences
Carrier Proteins - antagonists & inhibitors
Carrier Proteins - metabolism
Cerebral Cortex - metabolism
Medical sciences
Membrane Glycoproteins - antagonists & inhibitors
Membrane Glycoproteins - metabolism
Membrane Transport Proteins
Nerve Tissue Proteins
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Paroxetine - metabolism
Pharmacology. Drug treatments
Quipazine - analogs & derivatives
Quipazine - chemical synthesis
Quipazine - metabolism
Rats
Serotonin Plasma Membrane Transport Proteins
Serotonin Uptake Inhibitors - metabolism
Serotoninergic system
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Summary:Racemic 2′-methyl- and 3′-methyl-6-nitroquipazine ligands were selected as targets, synthesized and evaluated at the serotonin transporter employing an in vitro competitive inhibition assay with [ 3H]paroxetine and rat cortical membrane. The 2′-methyl-6-nitroquipazine was found to be 50 times more potent than the 3′-methyl-substituted counterpart and of comparable potency to the known high affinity agent 5-iodo-6-nitroquipazine.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00546-1