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Application of adenosine receptor A1 antagonist in preparing medicine

An adenosine receptor and antagonist technology, which is applied in the application field of preparing a drug for treating or preventing cholestatic liver disease, can solve the problems of failing to show the survival rate of ursodeoxycholic acid patients, and reduce the degree of necrosis of liver cells. , Enhance the ability of urinary excretion of bile acids and bilirubin, and prevent cholestatic liver disease

Inactive Publication Date: 2013-03-27
NANJING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Unfortunately, numerous clinical trials have also failed to show that ursodeoxycholic acid treatment can improve the survival rate of patients

Method used

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  • Application of adenosine receptor A1 antagonist in preparing medicine
  • Application of adenosine receptor A1 antagonist in preparing medicine
  • Application of adenosine receptor A1 antagonist in preparing medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0142] adenosine receptor A 1 Effect of antagonist (DPCPX) on cholestatic liver injury.

[0143] 1. Establishment of animal models:

[0144] Experimental animals were C57BL / 6 (WT) mice and A 1 AR - / - mice. Raised under standard experimental conditions: 12-hour light-12-hour dark cycle, free access to water and food. ANIT is used to establish the model of drug-induced cholestasis liver disease, and it is administered by intragastric administration (75mg / kg). WT mice and A 1 AR - / - The mice were randomly divided into three groups. The first group was the control group (veh / veh), which was treated with the corresponding drug solvent during the experiment; the second group was the ANIT group (veh / ANIT), which was given the corresponding solvent of DPCPX and gavage ANIT; the third group is the DPCPX treatment group (DPCPX / ANIT), DPCPX (0.1mg / kg) is given by intraperitoneal injection 15 minutes before ANIT gavage, twice a day, once every 12 hours. After 48 hours of intragast...

Embodiment 2

[0153] adenosine receptor A 1 Effect of antagonist (DPCPX) on bile acid metabolism.

[0154] 1. Establishment of animal models:

[0155] The experimental animals were WT mice. Raised under standard experimental conditions: 12-hour light-12-hour dark cycle, free access to water and food. ANIT is used to establish the model of drug-induced cholestasis liver disease, and it is administered by intragastric administration (75mg / kg). WT mice were randomly divided into three groups. The first group was the control group (veh / veh), which was treated with the corresponding drug solvent during the experiment; the second group was the ANIT group (veh / ANIT), which was given the corresponding solvent of DPCPX and gavage ANIT; the third group is the DPCPX treatment group (DPCPX / ANIT), DPCPX (0.1mg / kg) is given by intraperitoneal injection 15 minutes before ANIT gavage, twice a day, once every 12 hours. After 48 hours of intragastric administration of ANIT, all mice in the experimental ...

Embodiment 3

[0164] other adenosine receptor A 1 Effect of antagonists on cholestatic liver injury.

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PUM

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Abstract

The invention relates to a new use of an adenosine receptor A1 antagonist in the pharmaceutical field. The substance has the abilities in reducing cholestasis degree in organisms, relieving cholestatic liver damage, promoting secretion of bile acid and strengthening excretion of bile acid and bilirubin via urine and can be used for treating or preventing cholestatic liver disease.

Description

technical field [0001] The present invention relates to an adenosine receptor A 1 Use of antagonists, especially adenosine receptor A 1 Application of antagonist in preparation of medicine for treating or preventing cholestatic liver disease. Background technique [0002] Cholestasis is a disorder in the secretion or flow of bile caused by various causes. Cholestasis is generally divided into intrahepatic cholestasis and extrahepatic cholestasis. Extrahepatic cholestasis is caused by obstruction of bile flow outside the liver, and is more common in biliary stones and cholangitis. Intrahepatic cholestasis is due to hepatic bile secretion disorder, resulting in intrahepatic cholestasis and increased bile components in the blood without biliary obstruction. Can be caused by hepatitis, pregnancy, primary biliary cirrhosis, etc. [0003] The liver is the largest gland in mammals. It plays a very important role in metabolism, bile production, detoxification, blood coagulation...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/522A61K31/519A61P35/00A61P1/16A61P1/18
Inventor 张建法杨萍詹亦贝
Owner NANJING UNIV OF SCI & TECH
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