Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors.

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Vickers T, Dyck B, Tamiya J, Zhang M, Jovic F, Grey J, Fleck BA, Aparicio A, Johns M, Jin L, Tang H, Foster AC, Chen C

Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3230-5. doi: 10.1016/j.bmcl.2008.04.045. Epub 2008 Apr 25.

PubMed ID
18468895 [ View in PubMed
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Abstract

A series of milnacipran analogs containing a heteroaromatic group were synthesized and studied as monoamine transporter inhibitors. Many compounds exhibited higher potency than milnacipran at NET and NET/SERT with no significant change in lipophilicity. For example, compound R-26f was about 10-fold more potent than milnacipran with IC(50) values of 8.7 and 26nM at NET and SERT, respectively.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
LevomilnacipranSodium-dependent noradrenaline transporterIC 50 (nM)40N/AN/ADetails
LevomilnacipranSodium-dependent serotonin transporterIC 50 (nM)320N/AN/ADetails
MilnacipranSodium-dependent noradrenaline transporterIC 50 (nM)5500N/AN/ADetails
MilnacipranSodium-dependent serotonin transporterIC 50 (nM)3500N/AN/ADetails