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

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.
Troy Vickers 1,  Brian Dyck,  Junko Tamiya,  Mingzhu Zhang,  Florence Jovic,  Jonathan Grey,  Beth A Fleck,  Anna Aparicio,  Michael Johns,  Liping Jin,  Hui Tang,  Alan C Foster,  Chen Chen
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Neurocrine Bioscience, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
PMID: 18468895 DOI: 10.1016/j.bmcl.2008.04.045
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.

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