Anti-addiction medical application of L-corydalmine (L-CDL)

A technology of Corydalis damming and addiction, which is applied in the field of anti-addiction medicine of Corydalis damming, and can solve problems such as clinical application limitations

Active Publication Date: 2016-12-07
杨征
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, l-THP has obvious sedative eff...

Method used

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  • Anti-addiction medical application of L-corydalmine (L-CDL)
  • Anti-addiction medical application of L-corydalmine (L-CDL)
  • Anti-addiction medical application of L-corydalmine (L-CDL)

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Experimental program
Comparison scheme
Effect test

Embodiment

[0047] Corydalis chinensis (l-CDL) is an isoquinoline alkaloid originally isolated from the traditional Chinese medicine Corydalis Corydalis [1-2] . Through the research on the metabolism of l-THP, it is found that the product with the highest content in human plasma is 10-desmethyl sulfate conjugate, that is, the sulfate conjugate of Corydalamine, the concentration of which is equivalent to or higher than that of rotundine. The other product is the 3-desmethylsulfate conjugate. In human urine, the product with the highest content is also 10-desmethyl sulfate conjugate, followed by 3-desmethyl sulfate conjugate. It shows that rotundine works mainly through metabolism into corydalis damamine in the body. We have opened up and optimized the chemical synthesis route, and preclinical studies have confirmed that l-CDL has a dopamine receptor D 1 、D 2 、D 3 Antagonism and serotonin receptors (5-HT 1A ) agonistic effect.

[0048] Materials and methods

[0049] Experimental ani...

Embodiment 2

[0060] Embodiment 2, the impact of l-CDL on mouse methamphetamine (MA) induced behavioral sensitization acquisition

[0061] Kunming mice were administered with solvent or l-CDL for 7 consecutive days and then injected with MA intraperitoneally for 25 minutes. On the 12th day, after intraperitoneal injection of 2 mg / kg MA challenge, the activity of animals in each group was measured. The 1-h activity count of animals in MA group was significantly higher than that in solvent group (P figure 2

Embodiment 3

[0062] Embodiment 3, the influence of l-CDL on methamphetamine self-administration

[0063] Self-administration SA (self-administration SA) is an operational behavioral experiment, which uses the drug reinforcement effect to change the behavior of animals before and after exposure to drugs, simulating the process of drug addiction, withdrawal and relapse in humans . It is the most direct method to study the mechanism of drug addiction and evaluate the anti-addiction efficacy of drugs. It is the most ideal animal behavior model in the field of addiction research.

[0064] Materials and Methods

[0065] Long Evans rats, male, weighing 250-300g. Room temperature (22 ± 1) ℃, light time 8:00-20:00, free to drink and eat.

[0066] ①Venous cannulation: anesthetized with pentobarbital 40mg / kg, ligated the distal end, made a V-shaped incision at the proximal end, slowly inserted the silicone tube from the incision into the right internal jugular vein, at the entrance of the right a...

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Abstract

The invention relates to an application of a lead compound namely L-corydalmine (L-CDL) of isoquinoline compounds on treating diseases related with addiction. The diseases comprise drug addiction (heroin, opium, methyl amphetamine, morphine, marihuana, cocaine, and the like), nicotine addiction, and alcohol addiction, and also comprise novel drug addiction (stimulant type novel drugs) and brain damage caused by novel drugs.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to the medical use of isoquinoline alkaloid Corydalamine, which can be used to prepare medicines for treating diseases related to addiction damage, and to prevent and treat human new drug addiction and new drug addiction. Brain tissue damage caused by drugs, the addiction-related diseases include heroin, opium, methamphetamine (ice), morphine, marijuana, cocaine and other drug addictions and nicotine, alcohol and other substance addiction-related diseases, especially excitement Addiction to novel drugs and the brain damage they cause. Background technique [0002] The growing drug problem has become a global catastrophe. It directly endangers the physical and mental health of the people and poses a huge threat to economic development and social progress. According to statistics from the United Nations, the annual drug trade volume in the world has reached more than 500 billion US...

Claims

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Application Information

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IPC IPC(8): A61K31/4375A61P25/30
CPCA61K31/4375
Inventor 杨征杨红菊柳红米桂芸周宇
Owner 杨征
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