High impact information on MD 780515

• This may reflect the dose of cimoxatone used, the activity of monoamine oxidase form B (MAO-B) in the gut and liver or displacement of the predominantly reversible and predominantly competitive inhibitor, cimoxatone, from the enzyme by a high local tyramine concentration [1].
• The Ki values of the inhibition of MAO-A by cimoxatone and MD770222 (the principal plasma metabolite of cimoxatone) were independent of the substrate used to assay for activity, but were lower than the Ki values for the inhibition of MAO-B by these compounds [2].
• Rhesus monkey cerebrospinal fluid amine metabolite changes following treatment with the reversible monoamine oxidase type-A inhibitor cimoxatone [3].
• MD 770222, the O-demethyl metabolite, appeared to be bound to HSA at the same binding sites as cimoxatone [4].
• Plasma protein binding of the reversible type A MAO inhibitor cimoxatone (MD 780515) [4].

Biological context of MD 780515

• Pharmacokinetic and relative bioavailability studies of cimoxatone in humans [5].
• The pharmacokinetics of the reversible MAO-A inhibitor, cimoxatone, and its O-demethyl metabolite MD 770222 were investigated in eight healthy adult volunteers following single doses of 20- and 40-mg tablets, and 40-mg aqueous suspension [5].

Associations of MD 780515 with other chemical compounds

• In vitro, SR 95191 selectively inhibited MAO-A and was less potent than cimoxatone, clorgyline and harmaline, but was more potent than moclobemide [6].
• The effects of cimoxatone, a reversible inhibitor of monoamine oxidase type A (MAO-A), on the deaminated metabolites of norepinephrine, dopamine, and serotonin were examined in continuously collected rhesus monkey cerebrospinal fluid (CSF) [3].
• The preferential or specific inhibitors of MAO A, amiflamine, cimoxatone, CGP 11305 A, moclobemide and toloxatone did not alter rat brain PEA even at high doses [7].
• If in vitro findings are considered, the most potent MAO-A inhibitor seems to be cimoxatone and the least potent toloxatone [8].
• Here again moclobemide preferentially inhibited MAO-A; it was equipotent to clorgyline and brofaromine in these tests, and 2-4 times as potent as cimoxatone and harmaline [9].

Gene context of MD 780515

• Effect of a reversible and selective MAO-A inhibitor (cimoxatone) on diurnal variation in plasma prolactin level in man [10].

Analytical, diagnostic and therapeutic context of MD 780515

• Single simultaneous time point determinations revealed 10-to 20-fold lower concentrations of cimoxatone and its metabolite in CSF compared to plasma 2 h after treatment [3].

References