hat
Sèvi ak yon konplo dekouvèt dwòg pou maladi alzayme a (AD) ki baze sou patoloji miltip nan laj fin vye granmoun, nou idantifye yon konpoze ki pisan ak efikasite nan memwa wonjè ak AD bèt modèl. Depi sa a konpoze, J-147 poud, se yon hydrazide phenyl, te gen enkyetid ke li ka metabolize nan amine aromat / idrazin ki potansyèlman kanserojèn. Pou eksplore sa a posibilite, nou egzamine metabolit yo nan J 147 poud nan imen ak sourit mikrosom ak plasma sourit. Yo montre ke J-147 (1146963-51-0) poud pa metabolize nan amine aromat oswa idrazin, ke echafodaj la se eksepsyonèlman ki estab, e ke metabolit yo oksidatif yo tou neuroprotective. Li konkli ke metabolit pi gwo nan J 147 (1146963-51-0) poud ka kontribye nan aktivite byolojik li yo nan bèt yo.
eng
Using a drug discovery scheme for Alzheimer’s disease (AD) that is based upon multiple pathologies of old age, we identified a potent compound with efficacy in rodent memory and AD animal models. Since this compound, J-147 powder, is a phenyl hydrazide, there was concern that it can be metabolized to aromatic amines/hydrazines that are potentially carcinogenic. To explore this possibility, we examined the metabolites of J 147 powder in human and mouse microsomes and mouse plasma. It is shown that J-147(1146963-51-0) powder is not metabolized to aromatic amines or hydrazines, that the scaffold is exceptionally stable, and that the oxidative metabolites are also neuroprotective. It is concluded that the major metabolites of J 147(1146963-51-0) powder may contribute to its biological activity in animals.