Levodopa Powder CAS 59-92-7

Levodopa powder, core component of levodopa, molecular formula C9H11NO2, CAS 59-92-7, molecular weight 165.19, is a synthesized amino acid. White or grayish white crystalline powder. Melting point 285.5 ℃ (decomposition). It has a bitter taste and poor solubility, only slightly soluble in water, soluble in hot water, dilute acids and alkalis, and insoluble in ethanol, ether, and chloroform. Odorless, odorless, turning black in the air. When it is damp, it is easy to oxidize in the air and the color will darken. Easily soluble in dilute hydrochloric acid and formic acid, soluble in water (66mg/ml), almost insoluble in ethanol, benzene, chloroform, and ethyl acetate. It is an important drug precursor that can be converted into levodopa by the human body, which is an amino acid with pharmacological activity. 

Levodopa powder, as a precursor drug of dopamine, has become a core drug for treating Parkinson's disease since its discovery in the 1960s. Its unique pharmacological mechanism and wide clinical applications make it occupy an important position in fields such as neuroscience, geriatrics, ophthalmology, etc.

Core indication: The 'gold standard' treatment for Parkinson's disease and syndrome

 

1. Improvement of motor symptoms in Parkinson's disease
After passing through the blood-brain barrier, levodopa is converted into dopamine by dopa decarboxylase in the brain, directly supplementing the neurotransmitter deficiency caused by the degeneration of dopaminergic neurons in the substantia nigra striatum pathway. The core therapeutic effects include:

Slow movement: Clinical studies have shown that levodopa can increase patients' walking speed by 30% -50%, increase finger tapping frequency by 40%, and significantly improve their daily activity ability.
Muscle rigidity: By activating dopamine D2 receptors and reducing excessive activation of indirect pathways in the basal ganglia, muscle tone is restored to normal. In animal experiments, levodopa reduced the rotational behavior of Parkinson's model rats by 70%.

 

2. Extended application of Parkinson's syndrome
In addition to primary Parkinson's disease, levodopa is also effective for the following secondary or hereditary Parkinson's syndrome:

Vascular Parkinson's syndrome: Improving gait freezing caused by stroke, combined with rehabilitation training, can increase the patient's walking distance by 50%.
Multi system atrophy (MSA): For MSA-P type (Parkinson's type) patients, levodopa can temporarily improve motor symptoms, but the duration of efficacy is relatively short (usually<2 years).
Progressive supranuclear palsy (PSP): It is ineffective against vertical ophthalmoplegia, but can partially alleviate axial muscle rigidity and gait disorders.

 

3. Long term management strategy
End of use phenomenon: By switching to controlled release formulations (such as levodopa controlled-release tablets) or in combination with catechol-O-methyltransferase (COMT) inhibitors (such as entecavine), the "open period" time can be extended to 4-6 hours.
Dyskinesia: Low dose, high-frequency dosing regimen or combination with dopamine receptor agonists (such as pramipexole) is used to reduce dose fluctuations.
Cognitive impairment: High doses of levodopa may exacerbate cognitive fluctuations and require regular evaluation of MMSE scores and adjustment of dosage.

Special application scenario: Cross border exploration from hepatic encephalopathy to ophthalmic diseases

 

1. Neurotransmitter regulation in hepatic encephalopathy
Levodopa improves consciousness disorders in hepatic encephalopathy through the following mechanisms:

Dopamine replacement: In patients with cirrhosis, dopamine levels in the brain decrease by 50%, but levodopa can restore them to 70% of normal levels.
Improvement of ammonia tolerance: Animal experiments have shown that levodopa increases the tolerance dose of rats to ammonia poisoning by three times, which may be related to the enhancement of glutamine synthetase activity.
Clinical efficacy: A randomized controlled trial involving 200 patients showed that the combination of levodopa and lactulose can reduce the recurrence rate of hepatic encephalopathy by 40%.

 

2. Neuroplasticity regulation in amblyopia treatment
Levodopa powder promotes visual cortex remodeling through the following pathways:

Dopamine receptor activation: enhances the response threshold of neurons in the fourth layer of the visual cortex to visual stimuli, increasing contrast sensitivity by 20% -30%.
Synaptic plasticity enhancement: In children with anisometropic amblyopia, the combination of levodopa and occlusion therapy can improve visual acuity by 0.2-0.3 LogMAR units, significantly better than the occlusion group alone.
Treatment window: The best therapeutic effect occurs 3 months before treatment, and it is recommended that the course of treatment should not exceed 6 months to avoid side effects.

 

3. Exploratory applications of rare diseases
Dopa responsive dystonia (DRD): For patients with GTP cyclohydrolase-1 (GCH1) gene mutations, low-dose levodopa (100-300mg/d) can completely alleviate symptoms and does not require lifelong treatment.
Restless Leg Syndrome (RLS): A refractory RLS that is ineffective against iron deficiency, levodopa can shorten nighttime awakening time by 50%, but caution should be taken to avoid the risk of worsening symptoms.
Congenital muscle stiffness: For patients with CLCN1 gene mutations, levodopa can temporarily improve muscle stiffness, but the duration of efficacy is only 2-4 hours.

We are the supplier of levodopa natural.

After 106 years of research and development, it has become simpler, efficient, and high yield, and the overall process of raw materials have also become economical. In recent years, there have been few studies on the chemical synthesis of levodopa, mainly including the copper-catalyzed hydroxylation reaction and the synthesis of levodopa through a series of responses with resveratrol and hydantoin. The synthesis route of the copper-catalyzed hydroxylation reaction is shown in the figure below:

The main advantages of chemical synthesis are that the synthetic target is accurate and available, the yield is large, the purity is high levodopa powder, and the types of related substances such as by-products are few, and most of them can be predicted; The main disadvantages are high cost, relatively complex production process, harsh reaction conditions, and difficult separation of intermediates and by-products from target compounds.

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Another method for synthesizing levodopa: there are two enzymes commonly used in microbial enzyme conversion synthesis, and three have been reported, which are tyrosine phenol lyase, hydroxylase, and transaminase, which are relatively less used in levodopa synthesis. With L-Tyrosine as the substrate, the expression vector of the LMB B2 target gene was constructed and transformed into E. coli, and finally, levodopa was synthesized. This process is complex, and the substrate and ascorbic acid were added, which increased the cost and made it more difficult to control. Krishnaveni et al. Used tyrosine as a substrate to synthesize levodopa through fungal transformation, packed enzymatic bed method, and improved sealed enzymatic bed method (electric automatic synthesis method). Among them, Mina's electric automatic synthesis method had the highest yield of 95.9%.

The method of synthesizing Levodopa in the laboratory usually uses phenylalanine as the starting material and is prepared through a series of chemical reaction steps. The following are the detailed synthesis steps and corresponding chemical equations:

Through the above steps, Levodopa can be synthesized in the laboratory. It should be noted that during the synthesis process, it is necessary to pay attention to safety, avoid contact with toxic and harmful substances, and properly dispose of waste.

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