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Application of glucagon-like peptde-1 receptor agonist to preparation of pulmonary hypertension treating medicine

A technology of glucagon and receptor agonist is applied in the application field of preparing pulmonary arterial hypertension treatment medicine, and can solve the problem that GLP-1 receptor agonist is not seen.

Active Publication Date: 2016-10-12
FUWAI HOSPITAL CHINESE ACAD OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are no research reports on the use of GLP-1 receptor agonists in the treatment of pulmonary hypertension.

Method used

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  • Application of glucagon-like peptde-1 receptor agonist to preparation of pulmonary hypertension treating medicine
  • Application of glucagon-like peptde-1 receptor agonist to preparation of pulmonary hypertension treating medicine
  • Application of glucagon-like peptde-1 receptor agonist to preparation of pulmonary hypertension treating medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Therapeutic Effect of GLP-1 Receptor Agonist Liraglutide on Animals with Pulmonary Hypertension

[0036] 1. Purpose of the experiment

[0037] By establishing an animal model of pulmonary hypertension and using the GLP-1 receptor agonist liraglutide for treatment, the curative effect of liraglutide was observed by detecting pulmonary artery hemodynamics and right heart hypertrophy indicators in rats.

[0038] 2. Experimental animals and experimental methods

[0039]Male SD rats with a body weight of 220-230 g were randomly divided into three groups, namely the healthy control group, the pulmonary hypertension model non-medication group and the drug treatment group, with 6 rats in each group. The healthy control group was injected with normal saline only subcutaneously. Both the non-drug group and the drug treatment group were subcutaneously injected with monocrotaline (Sigma Company) to induce pulmonary hypertension, and monocrotaline was injected once, and ...

Embodiment 2

[0052] Example 2 Therapeutic Effect of GLP-1 Receptor Agonist Exenatide on Animals with Pulmonary Hypertension

[0053] 1. Purpose of the experiment

[0054] By establishing an animal model of pulmonary hypertension and treating it with GLP-1 receptor agonist exenatide, the efficacy of exenatide was observed by detecting pulmonary artery hemodynamics and right heart hypertrophy indexes in rats.

[0055] 2. Experimental animals and experimental methods

[0056] Male SD rats with a body weight of 220-230 g were randomly divided into three groups, namely the healthy control group, the pulmonary hypertension model non-medication group and the drug treatment group, with 6 rats in each group. The healthy control group was injected with normal saline only subcutaneously. Both the non-drug group and the drug treatment group were subcutaneously injected with monocrotaline (Sigma Company) to induce pulmonary hypertension, and monocrotaline was injected once, and the injection dose was...

Embodiment 3

[0068] Example 3 Effect of GLP-1 receptor agonists on pulmonary vascular remodeling

[0069] 1. Purpose of the experiment

[0070] In vitro tissue assays to evaluate the effect of liraglutide treatment on pulmonary vascular remodeling.

[0071] 2. Experimental method

[0072] After the above-mentioned groups of rats were killed, fresh lung tissues were taken out and soaked in 10% formalin solution overnight, then stored in 70% ethanol, embedded in paraffin, and sectioned for elastic fiber EVG staining to measure the degree of pulmonary vascular muscularization and CD68 staining Measure the degree of inflammatory cell infiltration.

[0073] 3. Experimental results

[0074] The degrees of pulmonary vascular muscularization in the non-drug group and the drug-treated group of the pulmonary hypertension model were 66.96±6.28% and 49.78±4.83%, respectively, and the degree of pulmonary vascular muscularization was significantly reduced after liraglutide treatment, with significant...

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Abstract

The invention discovers novel application of glucagon-like peptde-1 receptor agonist to preparation of a pulmonary hypertension treating medicine for the first time. It is proved through various experiments that the medicine can effectively reduce the cell glycolysis level, restrain the abnormal proliferation of pulmonary vascular cells and remarkably relieve pulmonary vascular reconstruction, thereby reducing pulmonary vascular resistance and pulmonary artery pressure and treating pulmonary hypertension.

Description

[0001] This application is for application number 201510428001.0 The filing date is July 20, 2015 The Chinese patent application on date filed a priority claim. Technical field: [0002] The invention relates to a new application of the glucagon-like peptide-1 receptor agonist, in particular to its application in the preparation of drugs for the treatment of pulmonary arterial hypertension. Background technique: [0003] Glucagon-like peptide-1 (hereinafter referred to as GLP-1) is an endogenous hormone secreted by small intestinal L-cells under the stimulation of nutrients in the intestinal lumen. [0004] In the reports in the prior art, GLP-1 mainly has the effect on glucose metabolism, including stimulating insulin release, preventing glucagon secretion, slowing down gastric emptying, and increasing satiety, etc. These effects are produced through Achieved by the GLP-1 receptor. GLP-1 receptors belong to G protein-coupled receptors and are distributed in tissues or or...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K38/26A61K38/22A61P9/12A61P11/00
CPCA61K38/22A61K38/26A61K45/00
Inventor 汪蕾方纬
Owner FUWAI HOSPITAL CHINESE ACAD OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE
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