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Application of P2X7 receptor inhibitor

A receptor inhibitor, 1. P2X7 technology, applied in the field of P2X7 receptor inhibitors to achieve the effect of protecting neurons

Inactive Publication Date: 2015-11-25
SUN YAT SEN MEMORIAL HOSPITAL SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no literature report whether P2X7 receptor can mediate the inflammatory response caused by radiation encephalopathy

Method used

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  • Application of P2X7 receptor inhibitor
  • Application of P2X7 receptor inhibitor
  • Application of P2X7 receptor inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: In vitro, the role of P2X7 receptors in the process of radiation activation of microglial cells and release of pro-inflammatory factors.

[0033] (1) Cell culture and preparation: subculture microglial cell line BV2 in DMEM medium containing 10% fetal bovine serum by volume and 1% double-antibody (penicillin, streptomycin) by mass cultured in 5% CO by volume 2 , Under the condition of 37°C, use a culture bottle to culture in an incubator, and change the medium once every two days. Each subculture was digested with 0.25% trypsin (containing 0.02% EDTA by mass percentage concentration) and inoculated in a new culture bottle at a uniform density. Cells were divided into 2×10 5 / ml density was inoculated in 6-well plate, and the inoculation density of 24-well plate was 1×10 4 / ml, at 37°C, volume percent concentration is 5% CO 2 Under the above conditions, after culturing in the incubator for 24 hours, replace with serum-free medium and cultivate for 4 hours....

Embodiment 2

[0063] Example 2: In animal experiments, the role of P2X7 receptors in the activation of microglial cells by radiation and the release of pro-inflammatory factors.

[0064] (1) Experimental grouping: 63 healthy adult male C57BL / 6J mice were randomly divided into three groups: control group, irradiation group, irradiation + drug pretreatment group. The irradiation group and drug intervention group were further divided into four subgroups, 3 days and 7 days after irradiation. There were 10 rats in the control group, 10 rats in each of the two irradiation subgroups, and 10 rats in each of the two drug pretreatment subgroups.

[0065] (2) Animal irradiation: Anesthetized by intraperitoneal injection of 10% chloral hydrate (200mg / kg) before irradiation, and then the mice were fixed on a horizontal plank in a prone position, and the two mice were placed on each other. The head of each mouse was kept in a straight line at an interval of 5 cm. Then the mice were placed on the radiot...

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Abstract

The invention discloses application of a P2X7 receptor inhibitor in the preparation of drugs for treating radiation brain injuries. Through experimental deep research on pathogenesis of radiation brain injuries and effect of a P2X7 receptor upon occurrence and development of the radiation brain injuries, discovered is that radioactive rays activating microglial cells by the P2X7 receptor cause following inflammatory response, the P2X7 receptor specific inhibitor BBG is effective in inhibiting this response, and nerve cells are thereby protected; the inhibitor is applicable to the treatment of radiation brain injuries.

Description

technical field [0001] The present invention relates to the use of P2X7 receptor inhibitors, in particular to the use of P2X7 receptor inhibitors in the preparation of medicines for treating radiation-induced brain injury. Background technique [0002] Radiation brain injury refers to the central nervous system disease caused by radiation exposure of brain tissue and the degeneration and necrosis of neurons under the combined action of various factors. It is common in primary or secondary head and neck benign and malignant lesions after radiotherapy, and also in radiation injuries in industrial production. According to statistics, the incidence of brain tissue necrosis after radiotherapy can be as high as 28.5%. Once the brain tissue necrosis forms after radiation, the course of the disease is irreversible, which not only seriously affects the quality of life of patients, but also brings heavy burdens and great harm to patients' families and society. The current research on...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/145A61P25/00A61P25/28
Inventor 唐亚梅徐永腾许鹏飞容小明林佛财
Owner SUN YAT SEN MEMORIAL HOSPITAL SUN YAT SEN UNIV
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