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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    References

    SHOWING 1-10 OF 79 REFERENCES
    A kinetic account for amphetamine-induced monoamine release
    • 9
    • PDF
    Nonclassical Pharmacology of the Dopamine Transporter: Atypical Inhibitors, Allosteric Modulators, and Partial Substrates
    • 75
    • PDF
    Serotonin-transporter mediated efflux: A pharmacological analysis of amphetamines and non-amphetamines
    • 85
    • PDF
    Amphetamines take two to tango: an oligomer-based counter-transport model of neurotransmitter transport explores the amphetamine action.
    • 110
    • PDF
    Amphetamine actions at the serotonin transporter rely on the availability of phosphatidylinositol-4,5-bisphosphate
    • 52
    • Highly Influential
    • PDF
    The N Terminus of Monoamine Transporters Is a Lever Required for the Action of Amphetamines*
    • 114
    • PDF
    Studies of the Biogenic Amine Transporters. 14. Identification of Low-Efficacy “Partial” Substrates for the Biogenic Amine Transporters
    • 21
    • Highly Influential
    • PDF
    Amphetamine Action at the Cocaine- and Antidepressant-Sensitive Serotonin Transporter Is Modulated by αCaMKII
    • 20
    • PDF
    In Vivo Amphetamine Action is Contingent on αCaMKII
    • 35
    Conformational state interactions provide clues to the pharmacochaperone potential of serotonin transporter partial substrates
    • 21
    • PDF