Losigamone. Dr Willmar Schwabe.
Losigamone is a potential antiepileptic under development by Schwabe, which is currently in phase III clinical trials. By August 2000, Schwabe was seeking suitable partners to collaborate in the completion of the phase III trials and further development. The exact mode of action of losigamone is unclear but it does not involve specific binding of GABA, flunitrazepam or t-butyl-bicyclophosphorothionate (TBPS) to their receptors. Data concerning the interaction of losigamone with GABA-A receptor channels, however, are inconsistent; it does not significantly modify the GABAergic inhibitory postsynaptic potentials (IPSPs) in hippocampal slices, although it potentiates GABA-induced chloride influx in primary spinal cord neuron cultures. Another suggested possible mechanism of action for losigamone is K+ channel activation.
Willmore
L J
LJ
Department of Neurology, Saint Louis University School of Medicine, MO 63104, USA. willmore@slu.edu
D000927:Anticonvulsants / Q000009:adverse effects / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D004827:Epilepsy / Q000188:drug therapy*; D005663:Furans / Q000009:adverse effects / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D006801:Humans; D013329:Structure-Activity Relationship
D000927:Anticonvulsants; D005663:Furans; C065427:losigame