左旋多巴 T0848

Product Introduction
Bioactivity


英文名: L-DOPA

描述: L-DOPA (Levodopa) 是的神经递质多巴胺的代谢前体，具有口服活性。Levodopa 能够透过血脑屏障，并在大脑中转化为多巴胺。Levodopa 具有抗痛觉过敏作用。Levodopa 还具有帕金森氏病的研究潜力。

激酶实验: Briefly, transfected HEK-293 cells, incubated in charcoal-treated Dulbecco's modified Eagle's medium for 24 h, are washed once with Hanks' solution and resuspended in a buffer containing 100 mM NaCl, 1 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 250 mMsucrose, 20 mM Tris-HCl, pH 7.4. Cells are lysed by freezing in liquid nitrogen. Dehydrogenase activity is measured in a final volume of 20 μL containing the appropriate concentration of bile acid, 30 nCi of [3H]cortisol, and unlabeled cortisol to a final concentrations of 50 nM. The reaction is started by mixing cell lysate with the reaction mixture. Alternatively, endoplasmic reticulum microsomes are prepared from transfected HEK-293 cells and incubated with reaction mixture containing various concentrations of cortisol and CDCA. Incubation proceeded for 20 min, and the conversion of cortisol to cortisone is determined by thin layer chromatography (TLC). Because of the inaccuracy of the TLC method at low conversion rates and the end-product inhibition of 11βHSD2 at conversion rates higher than 60-70%, only conversion rates between 10 and 60% are considered for calculation. The inhibitory constant IC50 is evaluated using the curve-fitting program. Results are expressed as means±S.E. and consist of at least four independent measurements.

体外活性: 在25-200 μM浓度下，L-DOPA 以剂量依赖的方式降低胎鼠中脑培养物中3H-DA的摄取。L-DOPA 减少了可存活细胞及酪氨酸羟化酶(TH)阳性神经元的数量，并破坏了整体神经突触网络。[1] 在多巴胺缺失的情况下，L-DOPA 通过过度抑制壳核-苍白球(GPe)投射的神经元以及随后的苍白球(GPi)来诱导运动障碍。L-DOPA 还导致苍白球(GPi)中细胞色素氧化酶信使RNA表达的降低。[2]

体内活性: L-DOPA 在诱导MPTP帕金森症状的猴子中引起多种异常运动的发展。L-DOPA 给药导致在6-OHDA-损伤大鼠的CdPu中多巴胺D3受体表达的异位。[3] L-DOPA （50 mg/kg）通过激活完整大鼠多巴胺D1/D2受体，增加基底节区整体的内酰胺浓度。L-DOPA 产生日益严重的口-舌自发运动，这些运动在损伤大鼠中可被大麻素激动剂R(+)-WIN55,212-2（1 mg/kg）减缓。[4] L-DOPA 给药逆转了严重损伤大鼠中观察到的D2多巴胺受体上调，提供了L-DOPA 在基底节达到生物活性浓度的证据。[5]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : Insoluble
H2O : 2.5 mM


关键字: blood-brain | precursor | Dopamine Receptor | anti-allodynic | inhibit | dopamine | L DOPA | LDOPA | L-DOPA | Orally | barrier | neurotransmitters | Parkinson | Inhibitor | Endogenous Metabolite

相关产品: (-)-Isocorypalmine | Tetrabenazine | CP-226269 | SKF-83566 | Pimozide-d4 | 2'-O-Methylisoliquiritigenin | Nuciferine | Methiothepin mesylate | Domperidone | ABT-670

相关库: Human Endogenous Metabolite Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Human Endogenous Metabolite Compound Library Plus | Anti-Cancer Approved Drug Library | Natural Product Library for HTS | Food as Medicine Compound Library | Orally Active Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途