Flupirtine derivatives

To delineate requirements for selectivity, correlation analysis was conducted for the neurotoxicity data, log 1/I50(NT), of flupirtine derivatives in a similar way. Unlike the correlation with the MES data, log k 0l l is now clearly superior to the use of log Al/T2in describing the observed variance in neurotoxic effects. 

Schluter, T., Struy, H., and Schonfeld P., 2000, Protection of mitochondrial integrity from oxidative stress by the triaminopyridine derivative flupirtine. FEBS Lett., 481 42-46 Shidoji, Y., Nakamura, N., Moriwaki, H., and Muto, Y., 1997, Rapid loss in the mitochondrial membrane potential during geranygeranoic acid-induced apoptosis. 

Retigabine which is in phase II clinical trials for epilepsy, is a derivative of the analgesic flupirtine which also has anticonvulsant activity. The anticonvulsant action of retigabine is greater than that of flupirtine, however retigabine is not effective in models of acute pain. 

Anticonvulsants are supposed to act on the Na+-channel that is embedded in phospholipid membranes. In a cooperative study aiming at reducing the number of animal experiments, the interaction of flupirtine (1) derivatives with PPC vesicles was... 

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See also in sourсe #XX -- [ ]

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