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Application of PT2385 in preparation of medicine for preventing and treating pulmonary hypertension

A technology of 1.PT2385 and 3.PT2385, applied in the field of biomedicine, can solve the problems of ineffective inhibition and reversal of pulmonary vascular remodeling, lack of inhibition or reversal, etc.

Inactive Publication Date: 2021-05-07
ARMY MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the treatment of pulmonary hypertension mainly includes oxygen therapy, vasodilators (such as prostaglandins, endothelin receptor antagonists, etc.), which have improved the survival rate of patients to a certain extent, but none of them can effectively inhibit and reverse the pulmonary hypertension. The occurrence of vascular remodeling
At the same time, there is also a lack of drugs that target the inflammatory response of pulmonary vessels to inhibit or reverse pulmonary vascular remodeling

Method used

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  • Application of PT2385 in preparation of medicine for preventing and treating pulmonary hypertension
  • Application of PT2385 in preparation of medicine for preventing and treating pulmonary hypertension
  • Application of PT2385 in preparation of medicine for preventing and treating pulmonary hypertension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Observation on the protective effect of PT2385 on hypoxia-induced pulmonary hypertension model

[0040] PT2385 was purchased from MCE, item number: HY-12867.

[0041] Preparation method: PT2385 is dissolved in 0.5% (mass percentage) of sodium carboxymethyl cellulose, 2.5% (volume percentage) of Tween 80, 2.5% (volume percentage) of dimethyl sulfoxide In saline, C57BL / 6 mice were orally administered (20 mg / kg), once every 2 days.

[0042] experimental method

[0043] SPF grade male C57BL / 6 mice (purchased from Hunan Slack Jingda Experimental Animal Co., Ltd., the same below) were selected and randomly divided into three groups for 6-8 weeks: normoxia group (C) 7 mice, hypoxia group ( H) 6 rats, 8 rats in hypoxia+PT group (H+PT-2385, 20mg / kg / 2d, gavage). The mouse model of hypoxic pulmonary hypertension (HPH) was replicated by the continuous hypobaric hypoxia method, that is, the mice in the hypoxic group were placed in a hypobaric hypoxic chamber at a simulated altitu...

Embodiment 2

[0055] Regulatory effect of PT2385 on endothelial cell adhesion under chronic hypoxia

[0056] PT2385 was purchased from MCE, item number: HY-12867.

[0057] Preparation method: PT2385 dimethyl sulfoxide was prepared as a 1mM stock solution, and diluted with endothelial cell culture medium before use to a final concentration of 10μM.

[0058] experimental method:

[0059] Human pulmonary arterial endothelial cells (HPAEC) were purchased from ScienCell Company, cultured with HPAEC special culture medium, and the cells were placed at 37°C, 5% CO 2 cultured in a cell culture incubator. THP-1 cells were purchased from ATCC, and passaged when the cells grew to 90% confluence, and the cells in the logarithmic growth phase were selected for experiments. When the cells are subjected to hypoxic treatment, place the inoculated cells in a 2 and CO 2 in the tri-gas incubator, and the O 2 The concentration was set at 1% (5% CO 2 , 94%N 2 ), and removed after culturing for a corresp...

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Abstract

The invention relates to application of PT2385 in preparation of a medicine for preventing and treating pulmonary hypertension, and belongs to the technical field of biomedicine. The invention provides a new medicinal application of PT2385, namely application of PT2385 in preparation of a medicine for preventing and treating pulmonary hypertension. The medicine prepared from PT2385 can be used for well preventing and treating pulmonary hypertension without obvious adverse reaction.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to the application of PT2385 in the preparation of medicines for preventing and treating pulmonary hypertension. Background technique [0002] Pulmonary arterial hypertension (PAH) refers to a hemodynamic and pathophysiological state in which pulmonary artery pressure rises beyond the normal range. It can be an independent disease, a complication, or a syndrome. The main manifestations of pulmonary hypertension are shortness of breath, fatigue, dizziness, chest pain, palpitations, syncope, and lower extremity edema after exercise. The hemodynamic diagnostic standard is that the mean pulmonary artery pressure measured by right heart catheterization is greater than 25mmHg at resting state at sea level. Its main features are persistent pulmonary vasoconstriction and pulmonary vascular remodeling, manifested as pulmonary vascular wall thickening, pulmonary vascular stenosis, occlus...

Claims

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Application Information

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IPC IPC(8): A61K31/277A61P11/00A61P9/12A61P9/00A61P9/04
CPCA61K31/277A61P9/00A61P9/04A61P9/12A61P11/00
Inventor 高钰琪陈德伟王授衔徐刚
Owner ARMY MEDICAL UNIV
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