Estimation of the elimination half-life of the monoamine oxidase inhibitor cimoxatone in rat brain on the basis of ex vivo inhibition data.

Cimoxatone is a reversible mixed-type selective inhibitor of monoamine oxidase-A. For a mixed-type inhibitor, it can be shown that (vo-vi)/Vi is proportional to the inhibitor concentration. This relationship has been used to estimate the t 1/2 of the elimination of cimoxatone in rat brain after a single dose of inhibitor. t 1/2 values, estimated with three monoamine oxidase substrates, were in the range 3.9-4.8 h, in reasonable agreement with t 1/2 values determined from the plasma and brain concentration/time curves of cimoxatone.