Ro 41-1049 hydrochloride is a reversible and selective inhibitor of monoamine oxidase-A (MAO-A). An homogeneous population of high affinity binding sites for [3H]Ro 41-1049 is found in membrane preparations from human frontal cortex and placenta (Kd values of 16.5 and 64.4 nM, respectively)[1].
in vivo
Ro 41-1049 (1-50 mg/kg; intraperitoneal injection; for 3 hours; Sprague-Dawley rats) treatment inhibits dopamine metabolite formation and increases dopamine levels in a dose-dependent fashion. Pretreatment with Ro 41-1049 (20 mg/kg) significantly increases dopamine formation following L-dopa administration (100 mg/kg IP) while decreasing formation of 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA)[2].
Animal Model:
Sprague-Dawley rats (200-240 g)[2]
Dosage:
1 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, or 50 mg/kg
Administration:
Intraperitoneal injection; for 3 hours
Result:
Inhibited dopamine metabolite formation and increased dopamine levels in a dose-dependent fashion. Pretreatment with the concentration of 20 mg/kg significantly increased dopamine formation following L-dopa administration while decreasing formation of DOPAC and HVA.
References
[1] Cesura AM, et al. Characterization of the binding of [3H]Ro 41-1049 to the active site of human monoamine oxidase-A. Mol Pharmacol. 1990 Mar;37(3):358-66. PMID:2314388 [2] Brannan T, et al. Effect of a selective MAO-A inhibitor (Ro 41-1049) on striatal L-dopa and dopamine metabolism: an in vivo study. J Neural Transm Park Dis Dement Sect. 1994;8(1-2):99-105. DOI:10.1007/BF02250920
