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A new application of κ-opioid receptor agonist

An opioid receptor agonizing and functional technology, applied in the field of medicine, can solve undiscovered problems, achieve good hypoglycemic effect, promote activation, and enhance the effect of adiponectin and insulin sensitivity

Inactive Publication Date: 2011-12-07
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, the research on U50, 488H has found that it has the effects of analgesia, sedation, and anti-inflammation, but it has not been found that it has the effect of lowering blood sugar and treating diabetes

Method used

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  • A new application of κ-opioid receptor agonist
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  • A new application of κ-opioid receptor agonist

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Preparation method of injection medicine for treating diabetes with κ-opioid receptor agonist U50, 488H as active ingredient:

[0032] The sterile powder of κ-opioid receptor agonist U50, 488H is directly used as injection, and each injection contains 50mg-80mg of κ-opioid receptor agonist U50, 488H.

[0033] The usage and dosage of the injection is as follows: dissolve and dilute with 1mL-2.5mL of water for injection or sterile normal saline to form an injection, and inject one intramuscularly every day.

Embodiment 2

[0035] Preparation method of capsule drug for treating diabetes with κ-opioid receptor agonist U50, 488H as active ingredient:

[0036] The κ-opioid receptor agonist U50, 488H is made into capsules according to the conventional capsule-making method, and the carrier is a conventional pharmaceutical capsule carrier, each capsule is 0.1g to 0.25g, and each capsule contains the κ-opioid receptor agonist U50 , 488H 50mg ~ 80mg.

[0037] The usage and dosage of the capsules are as follows: take after meals, 1-2 times a day, 1-2 capsules each time.

Embodiment 3

[0039] Preparation method of tablet medicine for treating diabetes with κ-opioid receptor agonist U50, 488H as active ingredient:

[0040] The kappa-opioid receptor agonist U50, 488H is made into tablets according to the conventional tablet-making method, and the auxiliary materials are conventional pharmaceutically acceptable auxiliary materials (such as starch, magnesium stearate, dextrin, etc.), 0.25g per tablet ~0.5g, each tablet contains 50mg~80mg of κ-opioid receptor agonist U50, 488H.

[0041] The usage and dosage of the tablet is as follows: take after meal, 1-2 times a day, 1-2 tablets each time.

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PUM

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Abstract

The invention discloses an application of kappa-opioid receptor agonists U50 and 488H in preparation of drugs for treating diabetes. In the invention, the good blood sugar reducing effect of kappa-opioid receptor agonists U50 and 488H is creatively discovered, and the research shows that the blood sugar reducing mechanisms of kappa-opioid receptor agonist U50 and 488H are as follows: (1) increasing the level of skeletal muscle adiponectin receptor 1 (AdipoR1) and enhancing the sensitivity of adiponectin and insulin; (2) promoting the membrane translocation of glucose transporter (GLUT4) in skeletal muscle cell and increasing the glucose transport capability of the skeletal muscle cell; and (3) promoting the activation of AMPK (adenosine-monophosphate-activated protein kinase) in the skeletal muscle cell and enhancing insulin sensitivity. In the invention, a new option is provided for the preparation of the drugs for treating diabetes.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a new application of a κ-opioid receptor agonist, in particular to a new application of a κ-opioid receptor agonist U50,488H. Background technique [0002] Diabetes is a global public health problem with rapid development and great harm to people's health. Diabetes mellitus is a chronic systemic metabolic disease characterized by persistent high blood sugar as its basic biochemical feature. Hyperglycemia is a sign of diabetes, and decreased insulin levels or insulin sensitivity are the causes of diabetes. Therefore, reducing blood glucose levels by improving insulin sensitivity is an important target for the treatment of diabetes. [0003] As an insulin hypersensitizing hormone, adiponectin can increase and promote the fatty acid oxidation and sugar absorption of skeletal muscle cells, significantly strengthen the gluconeogenesis of insulin, inhibit the glycogenesis ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P3/10A61K31/40A61P5/50
Inventor 裴建明王跃民郭海涛樊荣张淑苗李娟冯娜
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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