J M Witkin, R Cerne, P G Davis, K B Freeman, J M do Carmo, J K Rowlett, K R Methuku, A Okun, S D Gleason, X Li, M J Krambis, M Poe, G Li, J M Schkeryantz, R Jahan, L Yang, W Guo, L K Golani, W H Anderson, J T Catlow, T M Jones, F Porreca, J L Smith, K L Knopp, J M Cook
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 anxiolytic, anticonvulsant, and antinociceptive effects in rodents with reduced motoric side effects...
February 27, 2019: Pharmacology, Biochemistry, and Behavior