Synthesis and biological evaluation of novel compounds within a class of 3-aminochroman derivatives with dual 5-HT1A receptor and serotonin transporter affinity.

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Hatzenbuhler NT, Evrard DA, Harrison BL, Huryn D, Inghrim J, Kraml C, Mattes JF, Mewshaw RE, Zhou D, Hornby G, Lin Q, Smith DL, Sullivan KM, Schechter LE, Beyer CE, Andree TH

Synthesis and biological evaluation of novel compounds within a class of 3-aminochroman derivatives with dual 5-HT1A receptor and serotonin transporter affinity.

J Med Chem. 2006 Jul 27;49(15):4785-9.

PubMed ID
16854086 [ View in PubMed
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Abstract

Compounds containing a 5-carbamoyl-8-fluoro-3-amino-3,4-dihydro-2H-1-benzopyran and a 3-alkylindole moiety linked through a common basic nitrogen were prepared and evaluated for 5-HT1A affinity, serotonin rat transporter affinity, and functional antagonist activity in vitro. 26a was found to be the most potent and selective compound in this series and was shown to possess neurochemical activity in vivo by producing acute and rapid increases in 5-HT in the rat frontal cortex.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
FluoxetineSodium-dependent serotonin transporterIC 50 (nM)39.4N/AN/ADetails