Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.

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Lee KH, Park CE, Min KH, Shin YJ, Chung CM, Kim HH, Yoon HJ, Won-Kim, Ryu EJ, Shin YJ, Nam HS, Cho JW, Lee HY

Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5567-71. doi: 10.1016/j.bmcl.2010.07.021. Epub 2010 Aug 17.

PubMed ID
20724153 [ View in PubMed
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Abstract

A series of 3-aryl-3-azolylpropan-1-amines was prepared and screened for its capability of inhibiting monoamine reuptake. Analogs with nanomolar potency, good human in vitro microsomal stability, and low drug-drug interaction potential were described. In vivo models were used to evaluate the compound 19r for antidepressive, anxiolytic, and analgesic activity.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
FluoxetineSodium-dependent serotonin transporterIC 50 (nM)3.1N/AN/ADetails
VenlafaxineSodium-dependent dopamine transporterIC 50 (nM)7340N/AN/ADetails
VenlafaxineSodium-dependent noradrenaline transporterIC 50 (nM)581N/AN/ADetails
VenlafaxineSodium-dependent serotonin transporterIC 50 (nM)35N/AN/ADetails