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Registration Number

0208U002201, 0105U002251 , R & D reports

Title

A study of the antiepileptic activity of new carbamate derivatives - potential antiepileptic drugs

Head

Gromov L.,

Registration Date

18-01-2008

Organization

Institute of Pharmacology and Toxicology Academy of Medical sciences of Ykraine

Description

The anticonvulsive activity of 32 new carmamate derivatives was studied. 10 compaunds of 32 studied have been found to be active in the maximal electroshock (MES) and the pentylenetetrazole (PTZ) seizure test. The test LD50 (median lethal dose), ED50 (median effective dose), TD50 (median neurotoxic dose), TI (therapeutik index - LD50/ED50), PI (protective index - TD50/ED50) of studied compounds for mice and rats on acute seizure models, showed that the compaund AGB31 is optimal for the next investigation as the potential antiepileptic drug, because of it's the most large therapeutic index and the less neurotoxicity as compared with ofher derivatives. The AGB31 compaund prevents the development of pentylentetrazole kindling in rats. The duration (for 14 days) of administration of AGB31 develops no tolerance to its antisconvulsive action. It is shown that the mechanism of action of the AGB31 is mediated by it'sinfluence on GABA-ergic and the glycinergic inhibitory mediator systems.

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