LY451395

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Background

LY451395 (Mibampator) is a powerful, highly selective and biarylsulfonamide potentiator of AMPA receptors [1].LY451395 (Mibampator) has been found to be a potent, selective and centrally active positive allosteric modulators of AMPA receptor-mediated neurotransmission, which enhances ion channel flux in the presence of agonist by inhibiting desensitization and deactivation of the receptors. In addition, LY451395 has been revealed to enhance synaptic transmission. Besides, LY451395 has been reported to attenuate the response to acute ethanol administration in the rat in vivo [1]. Moreover, the in vivo metabolisms of LY451395 in mouse, rat, dog and human have produced several phase 1 oxidative metabolites [2].

[1] Jones N1, Messenger MJ, O'Neill MJ, Oldershaw A, Gilmour G, Simmons RM, Iyengar S, Libri V, Tricklebank M, Williams SC. AMPA receptor potentiation can prevent ethanol-induced intoxication. Neuropsychopharmacology. 2008 Jun;33(7):1713-23. Epub 2007 Sep 12.
[2] Zmijewski M1, Gillespie TA, Jackson DA, Schmidt DF, Yi P, Kulanthaivel P. Application of biocatalysis to drug metabolism: preparation of mammalian metabolites of a biaryl-bis-sulfonamide AMPA (alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid) receptor potentiator using Actinoplanes missouriensis. Drug Metab Dispos. 2006 Jun;34(6):925-31. Epub 2006 Feb 28.