Differential Pharmacologies of Mecamylamine Enantiomers: Positive Allosteric Modulation and Noncompetitive Inhibition

  title={Differential Pharmacologies of Mecamylamine Enantiomers: Positive Allosteric Modulation and Noncompetitive Inhibition},
  author={N. Fedorov and L. Benson and J. Graef and P. Lippiello and M. Bencherif},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={525 - 532}
  • N. Fedorov, L. Benson, +2 authors M. Bencherif
  • Published 2009
  • Medicine, Chemistry
  • Journal of Pharmacology and Experimental Therapeutics
  • (±)-Mecamylamine is a racemic mixture of a widely used brain-permeant noncompetitive inhibitor of muscle-type and neuronal nicotinic receptors (NNRs). The present studies evaluated whether the stereoisomers of this drug show different profiles for inhibition of the high-sensitivity (HS) and low-sensitivity (LS) isoforms of the human α4β2 NNR subtype expressed in subclonal human epithelial 1 cells. We found that at low concentrations (micromolar range), TC-5214 [S-(+)-mecamylamine] was more… CONTINUE READING
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