Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models.

@article{Rivas2009AntiseizureAO,
  title={Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models.},
  author={Felix M Rivas and James P. Stables and Lauren J. Murphree and Rahul V. Edwankar and Chitra R. Edwankar and Shengming Huang and Hiteshkumar D Jain and Hao Zhou and Samarpan Majumder and Subramanian Sankar and Bryan L. Roth and Joachim Ramerstorfer and Roman Furtmueller and Werner Sieghart and James M Cook},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 7},
  pages={
          1795-8
        }
}
The antiseizure activity of benzodiazepines (BDZs) 1-5 in mice and rats as animal models is described. These BDZs have selective efficacy for alpha2beta3gamma2 and alpha3beta3gamma2 GABA(A)-receptors. Significant anticonvulsant activity with little or no motor impairment and therapeutic indexes (TI) of 2.8-44 (mice, ip) were observed for compounds 2-4 in the subcutaneous metrazole seizure (scMET) test. In rats, orally (po) the TI was >5 to 105. These compounds represent novel leads in the… CONTINUE READING
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