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Photo-antagonism of the GABAA receptor

Author

Listed:
  • Martin Mortensen

    (Physiology and Pharmacology, University College London)

  • Favaad Iqbal

    (University College London)

  • Arun P. Pandurangan

    (Institute of Structural and Molecular Biology, Birkbeck College, University of London)

  • Saad Hannan

    (Physiology and Pharmacology, University College London)

  • Rosemary Huckvale

    (University College London)

  • Maya Topf

    (Institute of Structural and Molecular Biology, Birkbeck College, University of London)

  • James R. Baker

    (University College London)

  • Trevor G. Smart

    (Physiology and Pharmacology, University College London)

Abstract

Neurotransmitter receptor trafficking is fundamentally important for synaptic transmission and neural network activity. GABAA receptors and inhibitory synapses are vital components of brain function, yet much of our knowledge regarding receptor mobility and function at inhibitory synapses is derived indirectly from using recombinant receptors, antibody-tagged native receptors and pharmacological treatments. Here we describe the use of a set of research tools that can irreversibly bind to and affect the function of recombinant and neuronal GABAA receptors following ultraviolet photoactivation. These compounds are based on the competitive antagonist gabazine and incorporate a variety of photoactive groups. By using site-directed mutagenesis and ligand-docking studies, they reveal new areas of the GABA binding site at the interface between receptor β and α subunits. These compounds enable the selected inactivation of native GABAA receptor populations providing new insight into the function of inhibitory synapses and extrasynaptic receptors in controlling neuronal excitation.

Suggested Citation

  • Martin Mortensen & Favaad Iqbal & Arun P. Pandurangan & Saad Hannan & Rosemary Huckvale & Maya Topf & James R. Baker & Trevor G. Smart, 2014. "Photo-antagonism of the GABAA receptor," Nature Communications, Nature, vol. 5(1), pages 1-13, December.
    • Handle: RePEc:nat:natcom:v:5:y:2014:i:1:d:10.1038_ncomms5454
    DOI: 10.1038/ncomms5454
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