Lazabemide

Lazabemide is an inhibitor of monoamine oxidase B (MAO-B; K_i = 0.084 µM).¹ It is selective for MAO-B over MAO-A (IC₅₀s = 0.02 and 640 µM, respectively).² Lazabemide inhibits rat liver MAO-B ex vivo with an ED₅₀ value of 53 nmol/kg.³ It inhibits ischemia-reperfusion injury-induced hydroxyl radical formation in mouse cerebral ventricles when administered at a dose of 3 mg/kg.⁴

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1. Cesura, A.M., Gottowik, J., Lahm, H.W., et al. Investigation on the structure of the active site of monoamine oxidase-B by affinity labeling with the selective inhibitor lazabemide and by site-directed mutagenesis. Eur. J. Biochem. 236(3), 996-1002 (1996).

2. Ozaita, A., Olmos, G., Boronat, M.A., et al. Inhibition of monoamine oxidase A and B activities by imidazol(ine)/guanidine drugs, nature of the interaction and distinction from I₂-imidazoline receptors in rat liver. Br. J. Pharmacol. 121(5), 901-912 (1997).

3. Henriot, S., Kuhn, C., Kettler, C., et al. Lazabemide (Ro 19-6327), a reversible and highly sensitive MAO-B inhibitor: Preclinical and clinical findings. J. Neural Transm. Suppl. 41, 321-325 (1994).

4. Suzuki, T., Akaike, N., Ueno, K., et al. MAO inhibitors, clorgyline and lazabemide, prevent hydroxyl radical generation caused by brain ischemia/reperfusion in mice. Pharmacology 50(6), 357-362 (1995).