Lazabemide (Ro 19-6327)

An inhibitor of MAO-B

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10mg

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Background

Lazabemide is an inhibitor of monoamine oxidase B (MAO-B; K_i = 0.084 ?M).¹ It is selective for MAO-B over MAO-A (IC₅₀s = 0.02 and 640 ?M, 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

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 mutagenesisEur. 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 liverBr. 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 findingsJ. Neural Transm. Suppl.41321-325(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 micePharmacology50(6)357-362(1995)