Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models.
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ABSTRACT:
SUBMITTER: Rivas FM
PROVIDER: S-EPMC2671240 | biostudies-literature | 2009 Apr
REPOSITORIES: biostudies-literature
Publications
Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models.
Rivas Felix M FM Stables James P JP Murphree Lauren L Edwankar Rahul V RV Edwankar Chitra R CR Huang Shengming S Jain Hiteshkumar D HD Zhou Hao H Majumder Samarpan S Sankar Subramanian S Roth Bryan L BL Ramerstorfer Joachim J Furtmüller Roman R Sieghart Werner W Cook James M JM
Journal of medicinal chemistry 20090401 7
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 search ...[more]
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