Anticonvulsant profile and teratogenicity of N-methyl-tetramethylcyclopropyl carboxamide: a new antiepileptic drug

Epilepsia
Nina IsoherranenMeir Bialer

Abstract

The studies presented here represent our efforts to investigate the anticonvulsant activity of N-methyl-tetramethylcyclopropyl carboxamide (M-TMCD) and its metabolite tetramethylcyclopropyl carboxamide (TMCD) in various animal (rodent) models of human epilepsy, and to evaluate their ability to induce neural tube defects (NTDs) and neurotoxicity. The anticonvulsant activity of M-TMCD and TMCD was determined after intraperitoneal (i.p.) administration to CF#1 mice, and either oral or i.p. administration to Sprague-Dawley rats. The ability of M-TMCD and TMCD to block electrical-, chemical-, or sensory-induced seizures was examined in eight animal models of epilepsy. The plasma and brain concentrations of M-TMCD and TMCD were determined in the CF#1 mice after i.p. administration. The induction of NTDs by M-TMCD and TMCD was evaluated after a single i.p. administration at day 8.5 of gestation in a highly inbred mouse strain (SWV) that is susceptible to valproic acid-induced neural tube defects. In mice, M-TMCD afforded protection against maximal electroshock (MES)-induced, pentylenetetrazol (Metrazol)-induced, and bicuculline-induced seizures, as well as against 6-Hz "psychomotor" seizures and sound-induced seizures with ED50 values...Continue Reading

References

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Citations

Jan 3, 2007·Neurotherapeutics : the Journal of the American Society for Experimental NeuroTherapeutics·Meir Bialer, Boris Yagen
Apr 2, 2003·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Nina IsoherranenMeir Bialer
Feb 22, 2012·Journal of Medicinal Chemistry·Naama HenBoris Yagen
May 31, 2006·Expert Opinion on Investigational Drugs·Meir Bialer
Oct 16, 2009·Birth Defects Research. Part B, Developmental and Reproductive Toxicology·Akinobu OkadaMichio Fujiwara
Aug 2, 2008·Birth Defects Research. Part A, Clinical and Molecular Teratology·Akinobu OkadaMichio Fujiwara
May 31, 2006·Congenital Anomalies·Akinobu Okada, Michio Fujiwara
Dec 4, 2004·Biological Psychiatry·Galit ShaltielGalila Agam
Jun 9, 2006·Journal of Neurophysiology·Anitha B AlexKaren S Wilcox
Nov 13, 2007·Journal of Medicinal Chemistry·Jakob Avi ShimshoniBoris Yagen

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