Kinetic evaluation of MAO-B-activity following oral administration of selegiline and desmethyl-selegiline in the rat.

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Abstract

The monoamine oxidase (MAO) B activity of rat brain was inhibited by selegiline and its desmethyl-metabolite in vitro with IC50-values of 11.25 nmol/l and 625.00 nmol/l, respectively. When measured in an ex vivo experiment following oral treatment of rats, the large difference in potency was distinctly reduced, from factor 60 in vitro to factor 3 ex vivo. Restoration experiments of MAO-B-activity after cessation of treatment revealed a nearly identical time course for both compounds. It is concluded that desmethyl-selegiline is an irreversible blocker of MAO-B, nearly equipotent to selegiline after multiple oral administration. No pharmacologically relevant inhibition of MAO-A was found with both compounds.

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Borbe, H. O., Niebch, G., & Nickel, B. (1990). Kinetic evaluation of MAO-B-activity following oral administration of selegiline and desmethyl-selegiline in the rat. Journal of Neural Transmission. Supplementum, 32, 131–137. https://doi.org/10.1007/978-3-7091-9113-2_18

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