Ro 41-1049 hydrochloride 是单胺氧化酶-A (MAO-A) 的可逆选择性抑制剂。
| Cas No. | 127917-66-2 |
| Canonical SMILES | O=C(C1=C(C2=CC=CC(F)=C2)SC=N1)NCCN.[H]Cl |
| 分子式 | C12H13ClFN3OS |
| 分子量 | 301.77 |
| 溶解度 | DMSO : ≥ 32 mg/mL (106.04 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Ro 41-1049 hydrochloride is a selective, reversible, orally-active MAO-A inhibitor.Target: MAOin vivo: Ro 41-1049 is an inhibitor of the enzyme monoamine oxidase type A (MAO-A) to rats and monitored extracellular catecholamine levels in the corpus striatum before and after the intraperitoneal (IP) administration of a bolus of L-dopa. Acute administration of Ro 41-1049 (1-50 mg/kg IP) produced a dose-dependent decrease in basal levels of the dopamine metabolites 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) and an increase in basal levels of dopamine. In rats treated with Ro 41-1049 (20 mg/kg IP), L-dopa administration (100 mg/kg IP) produced a greater increase in striatal levels of dopamine than it did in controls, while DOPAC and HVA formation was attenuated. We conclude that inhibition of central MAO-A activity promotes synaptic accumulation of dopamine following administration of pharmacological doses of L-dopa. 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.
[2]. Richards G, et al. Up-regulation of the isoenzymes MAO-A and MAO-B in the human basal ganglia and pons in Huntington's disease revealed by quantitative enzyme radioautography. Brain Res. 2011 Jan 25;1370:204-14.
[3]. 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. |
