产品描述: | 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) |
靶点: |
MAO-A;MAO |
体内研究: |
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). Animal Model: Sprague-Dawley rats (200-240 g) 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. |
参考文献: |
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. 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. |
溶解性: |
Soluble in DMSO、H2O |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.314 ml |
16.569 ml |
33.138 ml |
5 mM |
0.663 ml |
3.314 ml |
6.628 ml |
10 mM |
0.331 ml |
1.657 ml |
3.314 ml |
50 mM |
0.066 ml |
0.331 ml |
0.663 ml |
|
注意: |
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