Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.

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McComas CC, Vu AT, Mahaney PE, Cohn ST, Fensome A, Marella MA, Nogle L, Trybulski EJ, Ye F, Zhang P, Alfinito P, Bray J, Johnston G, Koury E, Deecher DC

Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):4929-31. doi: 10.1016/j.bmcl.2008.08.060. Epub 2008 Aug 22.

PubMed ID
18771916 [ View in PubMed
]
Abstract

Norepinephrine and serotonin play an important role in a wide variety of biological processes and are implicated in a number of neurological disorders. A novel class of 1-(3-amino-1-phenylpropyl)indolin-2-ones was designed and synthesized that displays potent norepinephrine reuptake inhibition while maintaining high selectivity (>100-fold) against the human serotonin and dopamine transporters.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
AtomoxetineSodium-dependent noradrenaline transporterIC 50 (nM)3N/AN/ADetails
AtomoxetineSodium-dependent serotonin transporterIC 50 (nM)48N/AN/ADetails
DesipramineSodium-dependent noradrenaline transporterIC 50 (nM)3.9N/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)10N/AN/ADetails
ParoxetineSodium-dependent noradrenaline transporterIC 50 (nM)100N/AN/ADetails
ParoxetineSodium-dependent serotonin transporterIC 50 (nM)2N/AN/ADetails