Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.

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Sabatucci JP, Mahaney PE, Leiter J, Johnston G, Burroughs K, Cosmi S, Zhang Y, Ho D, Deecher DC, Trybulski E

Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.

Bioorg Med Chem Lett. 2010 May 1;20(9):2809-12. doi: 10.1016/j.bmcl.2010.03.059. Epub 2010 Mar 15.

PubMed ID
20378347 [ View in PubMed
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Abstract

A series of heterocyclic cycloalkanol ethylamines have been prepared to expand our norepinephrine reuptake inhibitor (NRI) program. Synthesis of a variety of heterocycles identified (+)-S-21, a potent NRI efficacious in an animal model for thermoregulatory dysfunction.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DesipramineSodium-dependent noradrenaline transporterIC 50 (nM)3.4N/AN/ADetails
DuloxetineSodium-dependent dopamine transporterIC 50 (nM)>1000N/AN/ADetails
DuloxetineSodium-dependent noradrenaline transporterIC 50 (nM)4N/AN/ADetails
DuloxetineSodium-dependent serotonin transporterIC 50 (nM)3N/AN/ADetails
FluoxetineSodium-dependent serotonin transporterIC 50 (nM)9.4N/AN/ADetails
MazindolSodium-dependent dopamine transporterIC 50 (nM)22.1N/AN/ADetails
VenlafaxineSodium-dependent dopamine transporterIC 50 (nM)>10000N/AN/ADetails
VenlafaxineSodium-dependent noradrenaline transporterIC 50 (nM)535N/AN/ADetails
VenlafaxineSodium-dependent serotonin transporterIC 50 (nM)27N/AN/ADetails