The α2,3-selective potentiator of GABAA receptors, KRM-II-81, reduces nociceptive-associated behaviors induced by formalin and spinal nerve ligation in rats

@article{Witkin2019TheP,
  title={The $\alpha$2,3-selective potentiator of GABAA receptors, KRM-II-81, reduces nociceptive-associated behaviors induced by formalin and spinal nerve ligation in rats},
  author={J. Witkin and R. Černe and P. Davis and K. Freeman and J. Carmo and J. K. Rowlett and K. R. Methuku and A. Okun and S. Gleason and X. Li and M. Krambis and M. Poe and G. Li and J. Schkeryantz and R. Jahan and L. Yang and W. Guo and L. K. Golani and W. H. Anderson and J. Catlow and T. M. Jones and F. Porreca and J. L. Smith and K. Knopp and J. Cook},
  journal={Pharmacology Biochemistry and Behavior},
  year={2019},
  volume={180},
  pages={22-31}
}
Clinical evidence indicates that positive allosteric modulators (PAMs) of GABAA receptors have analgesic benefit in addition to efficacy in anxiety disorders. However, the utility of GABAA receptor PAMs as analgesics is compromised by the central nervous system side effects of non-selective potentiators. A selective potentiator of GABAA receptors associated with α2/3 subunits, KRM-II-81(5-(8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepin-3-yl)oxazole), has demonstrated… Expand
The α2,3-selective potentiators of GABAA receptors, KRM-II-81 and MP-III-80, produce anxiolytic-like effects and block chemotherapy-induced hyperalgesia in mice without tolerance development
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  • The Journal of Pharmacology and Experimental Therapeutics
  • 2019
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