A real-time fluorescence assay for measuring N-dealkylation.

A real-time fluorescence assay system using a series of 9-N-(alkylamino)acridine derivatives (methyl, ethyl, n-propyl, n-butyl, n-pentyl, and benzyl) that are N-dealkylated to 9-aminoacridine (9AA) is described. The product, 9AA, is approximately 27-fold more fluorescent than the substrates using excitation and emission wavelengths of 405 and 455 nm, respectively. Tests using expressed CYP1A1, 1A2, 3A4, 3A5, 1B1, 2C9, 2C19, and 2D6 indicated that N-dealkylase activity is specific for CYP1A1 and CYP2D6.

Stability of memantine in an extemporaneously prepared oral liquid.

Memantine, a N-methyl-D-aspartate receptor antagonist, was recently approved by the United States Food and Drug Administration for the palliative treatment of moderate to severe Alzheimer's disease. Its suggested mechanism of action in the treatment of Alzheimer's disease is binding to N-methyl-D-aspartate receptors, which results in inhibition of glutamate activity. Glutamate has been reported to contribute to the pathogenesis of Alzheimer's disease by overstimulating the N-methyl-D-aspartate receptors, resulting in brain cell damage.

Aging induces cardiac diastolic dysfunction, oxidative stress, accumulation of advanced glycation endproducts and protein modification.

Evidence suggests that aging, per se, is a major risk factor for cardiac dysfunction. Oxidative modification of cardiac proteins by non-enzymatic glycation, i.e.