The Positive Allosteric Modulator of α2/3-Containing GABA(A) Receptors, KRM-II-81, Is Active in Pharmaco-Resistant Models of Epilepsy and Reduces Hyperexcitability after Traumatic Brain Injury

The imidizodiazepine, 5-(8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepin-3-yl)oxazole (KRM-II-81), is selective for α2/3-containing GABA(A) receptors. KRM-II-81 dampens seizure activity in rodent models with enhanced efficacy and reduced motor-impairment compared with diazepam. In...

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Vydáno v:J Pharmacol Exp Ther
Hlavní autoři: Witkin, Jeffrey M., Li, Guanguan, Golani, Lalit K., Xiong, Wenhui, Smith, Jodi L., Ping, Xingjie, Rashid, Farjana, Jahan, Rajwana, Cerne, Rok, Cook, James M., Jin, Xiaoming
Médium: Artigo
Jazyk:Inglês
Vydáno: The American Society for Pharmacology and Experimental Therapeutics 2020
Témata:
Drug Discovery and Translational Medicine
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC6927408/
https://ncbi.nlm.nih.gov/pubmed/31694876
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1124/jpet.119.260968
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