Functional Selectivity and Partial Efficacy at the Monoamine Transporters: A Unified Model of Allosteric Modulation and Amphetamine-Induced Substrate Release

@article{Hasenhuetl2019FunctionalSA,
  title={Functional Selectivity and Partial Efficacy at the Monoamine Transporters: A Unified Model of Allosteric Modulation and Amphetamine-Induced Substrate Release},
  author={Peter S Hasenhuetl and Shreyas P Bhat and M. Freissmuth and W. Sandtner},
  journal={Molecular Pharmacology},
  year={2019},
  volume={95},
  pages={303 - 312}
}
  • Peter S Hasenhuetl, Shreyas P Bhat, +1 author W. Sandtner
  • Published 2019
  • Chemistry, Medicine
  • Molecular Pharmacology
    • All clinically approved drugs targeting the plasmalemmal transporters for dopamine, norepinephrine, and serotonin act either as competitive uptake inhibitors or as amphetamine-like releasers. Monoamine transporter (MAT) ligands that allosterically affect MAT-mediated substrate uptake, release, or both were recently discovered. Their modes of action have not yet been explained in a unified framework. Here, we go beyond competitive inhibitors and classic amphetamines and introduce concepts for… CONTINUE READING
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