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      Synthesis and in vitro sodium channel blocking activity evaluation of novel homochiral mexiletine analogs.

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          Abstract

          New chiral mexiletine analogs were synthesized in their optically active forms and evaluated in vitro as use-dependent blockers of skeletal muscle sodium channels. Tests carried out on sodium currents of single muscle fibers of Rana esculenta demonstrated that all of them exerted a higher use-dependent block than mexiletine. The most potent analog, (S)-3-(2,6-dimethylphenoxy)-1-phenylpropan-1-amine (S)-(5), was six-fold more potent than (R)-Mex in producing a tonic block. As observed with mexiletine, the newly synthesized compounds exhibit modest enantioselective behavior, that is more evident in 3-(2,6-dimethylphenoxy)butan-1-amine (3).

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          Author and article information

          Journal
          Chirality
          Chirality
          Wiley
          1520-636X
          0899-0042
          Mar 2010
          : 22
          : 3
          Affiliations
          [1 ] Dipartimento Farmaco-Chimico, Facoltà di Farmacia, Università degli Studi di Bari, Bari, Italy. carocci@farmchim.uniba.it
          Article
          10.1002/chir.20741
          19544349
          8e6a7f55-6418-4357-af64-89a97ecde130
          History

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