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Use of kappa-opioid receptor agonist u50,488h in the preparation of medicines for treating vascular calcification

A technology of opioid receptor stimulation and vascular calcification, which is applied in the field of medicine to achieve the effect of inhibiting calcification, inhibiting vascular calcification, and good vascular calcification

Active Publication Date: 2021-09-03
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The previous studies of the present invention have confirmed that κ-OR activation has a protective effect on large and medium vascular endothelial cells, but whether κ-OR activation can improve vascular remodeling during vascular calcification, and reverse the osteogenic transformation and apoptosis of VSMCs, improve Local calcium-phosphorus ratio and glycolysis level have not been reported at home and abroad so far

Method used

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  • Use of kappa-opioid receptor agonist u50,488h in the preparation of medicines for treating vascular calcification
  • Use of kappa-opioid receptor agonist u50,488h in the preparation of medicines for treating vascular calcification
  • Use of kappa-opioid receptor agonist u50,488h in the preparation of medicines for treating vascular calcification

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Effect test

Embodiment 1

[0021] The following experiments will illustrate the inhibitory effect and mechanism of κ-opioid receptor agonist U50,488H on calcification of rat vascular smooth muscle cells

[0022] 1. Establishment and grouping of rat vascular smooth muscle cell calcification model

[0023] Separate the rat thoracic aorta on ice, remove the adventitia and adipose tissue, cut the blood vessel longitudinally, scrape gently to remove the intimal cells, and cut the medial tissue into 1mm 3 Tissue blocks, spread evenly on 25cm 2 At the bottom of the culture flask, after 6 hours, the tissue adheres firmly to the wall, and then add sufficient medium. After the smooth muscle cells climb out, they are cultured and passaged. Cells of passage 6-8 are used in the experiment. The experiment was divided into control (Con) group: normal culture in normoxia incubator, serum concentration 10%; control+U50,488H (Con+U) group: given U50,488H (40 μmol / L) on the basis of control group Culture; high phosphoru...

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Abstract

The present invention belongs to the technical field of medicine, and relates to the new application of κ-opioid receptor agonist U50,488H, and more specifically, relates to the application of κ-opioid receptor agonist U50,488H in the preparation of drugs for treating vascular calcification. Experiments have proved that its mechanism of inhibiting vascular calcification is: by reducing the expression of PFKFB3, and then inhibiting the level of glycolysis, thereby inhibiting the calcification of VSMCs induced by high phosphorus. The research results provide a potential drug target for the clinical treatment of vascular calcification and treatment strategies.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the new application of κ-opioid receptor agonist U50,488H, and more specifically, the application of κ-opioid receptor agonist U50,488H in preparing medicine for treating vascular calcification. Background technique [0002] Vascular Calcification (VC) is the transformation of arterial wall mesenchymal cells, especially smooth muscle cells (VSMCs) into an osteoblast phenotype under the action of various pathological factors, resulting in abnormal deposition of calcium salts on the vessel wall the process of. Vascular calcification reduces the compliance of blood vessels, causes local hypoxia of blood vessels, increases the risk of vascular rupture and aneurysm formation, and easily leads to cardiovascular events such as myocardial ischemia, left ventricular hypertrophy, heart failure and stroke. Despite extensive research and enormous healthcare costs, vascular calcification curr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/40A61P9/04A61P9/10A61P9/14
CPCA61K31/40A61P9/04A61P9/10A61P9/14
Inventor 裴建明李娟牛津张淑苗樊荣付锋李军杨璐刘亚莉冯娜顾晓明贾敏刘银姬张敏
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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