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@ARTICLE{Maleeva:1031972,
      author       = {Maleeva, Galyna and Nin-Hill, Alba and Wirth, Ulrike and
                      Rustler, Karin and Ranucci, Matteo and Opar, Ekin and
                      Rovira, Carme and Bregestovski, Piotr and Zeilhofer, Hanns
                      Ulrich and König, Burkhard and Alfonso-Prieto, Mercedes and
                      Gorostiza, Pau},
      title        = {{L}ight-{A}ctivated {A}gonist-{P}otentiator of {GABA} {A}
                      {R}eceptors for {R}eversible {N}euroinhibition in {W}ildtype
                      {M}ice},
      journal      = {Journal of the American Chemical Society},
      volume       = {146},
      number       = {42},
      issn         = {0002-7863},
      address      = {Washington, DC},
      publisher    = {ACS Publications},
      reportid     = {FZJ-2024-05896},
      pages        = {28822-28831},
      year         = {2024},
      abstract     = {Gamma aminobutyric acid type A receptors (GABAARs) play a
                      key role in the mammalian central nervous system (CNS) as
                      drivers of neuroinhibitory circuits, which are commonly
                      targeted for therapeutic purposes with potentiator drugs.
                      However, due to their widespread expression and strong
                      inhibitory action, systemic pharmaceutical potentiation of
                      GABAARs inevitably causes adverse effects regardless of the
                      drug selectivity. Therefore, therapeutic guidelines must
                      often limit or exclude clinically available GABAAR
                      potentiators, despite their high efficacy, good
                      biodistribution, and favorable molecular properties. One
                      solution to this problem is to use drugs with
                      light-dependent activity (photopharmacology) in combination
                      with on-demand, localized illumination. However, a suitable
                      light-activated potentiator of GABAARs has been elusive so
                      far for use in wildtype mammals. We have met this need by
                      developing azocarnil, a diffusible GABAergic
                      agonist-potentiator based on the anxiolytic drug abecarnil
                      that is inactive in the dark and activated by visible violet
                      light. Azocarnil can be rapidly deactivated with green light
                      and by thermal relaxation in the dark. We demonstrate that
                      it selectively inhibits neuronal currents in hippocampal
                      neurons in vitro and in the dorsal horns of the spinal cord
                      of mice, decreasing the mechanical sensitivity as a function
                      of illumination without displaying systemic adverse effects.
                      Azocarnil expands the in vivo photopharmacological toolkit
                      with a novel chemical scaffold and achieves a milestone
                      toward future phototherapeutic applications to safely treat
                      muscle spasms, pain, anxiety, sleep disorders, and
                      epilepsy.},
      cin          = {INM-9 / IAS-5},
      ddc          = {540},
      cid          = {I:(DE-Juel1)INM-9-20140121 / I:(DE-Juel1)IAS-5-20120330},
      pnm          = {5241 - Molecular Information Processing in Cellular Systems
                      (POF4-524) / 5251 - Multilevel Brain Organization and
                      Variability (POF4-525) / 5252 - Brain Dysfunction and
                      Plasticity (POF4-525) / DFG project G:(GEPRIS)291198853 -
                      FOR 2518: Funktionale Dynamik von Ionenkanälen und
                      Transportern - DynIon - (291198853) / DFG project
                      G:(GEPRIS)329460521 - Protonentransfer und Substraterkennung
                      in SLC17-Transportern (329460521)},
      pid          = {G:(DE-HGF)POF4-5241 / G:(DE-HGF)POF4-5251 /
                      G:(DE-HGF)POF4-5252 / G:(GEPRIS)291198853 /
                      G:(GEPRIS)329460521},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {39383450},
      UT           = {WOS:001335501100001},
      doi          = {10.1021/jacs.4c08446},
      url          = {https://juser.fz-juelich.de/record/1031972},
}