Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Application of type-II cannabinoid receptor agonist in preparation of drugs for treating hypertensive cerebral hemorrhage

A technology of hypertensive cerebral hemorrhage and cannabinoid receptors, which is applied in the field of cerebral hemorrhage drugs to achieve the effects of inhibiting the proliferation and activation of microglia, improving secondary brain damage, and increasing therapeutic effects

Inactive Publication Date: 2016-06-15
THE FIRST AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIVERSITY OF PLA
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there is no research report on JWH133 improving neurological function after hypertensive cerebral hemorrhage

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Application of type-II cannabinoid receptor agonist in preparation of drugs for treating hypertensive cerebral hemorrhage
  • Application of type-II cannabinoid receptor agonist in preparation of drugs for treating hypertensive cerebral hemorrhage
  • Application of type-II cannabinoid receptor agonist in preparation of drugs for treating hypertensive cerebral hemorrhage

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] SD rats (250g-300g) were model animals, and the right femoral artery was dissected and separated, and 200 microliters of autologous arterial blood (without anticoagulant) was taken with a 1ml insulin needle and immediately injected into the right side of the rat through a stereotaxic instrument and a microinjection pump. In the basal ganglia area (slowly inject within 15 minutes), the needle insertion coordinates are 0.2 mm on the mouth side and 2.2 mm on the right side, and the needle tip is inserted 5 mm after breaking through the dura mater. Set up a blank control group (normal SD rats without surgery), a normal saline group (peritoneal injection of the same amount of normal saline after surgery), a JWH133 treatment group (peritoneal injection of JWH133 aqueous solution 1.5 mg / kg, twice a day, 7 days in total), 10 animals in each group.

[0043] Three days after the establishment of the model, the brain was perfused and sliced ​​for immunohistochemistry and brain tis...

Embodiment 2

[0049] Effect of Type II Cannabinoid Receptor Selective Agonist (JWH133) on Proliferation of Primary Cultured Microglial Cells Stimulated by Thrombin

[0050] Pregnant 14.5dSD rats were selected, anesthetized intraperitoneally with 5% chloral hydrate, the peritoneum was opened, the embryos were taken out, the scalp, skull and dura mater were removed, and the rat brain was peeled off. Under a dissecting microscope, the olfactory bulb was taken as the center of the sagittal longitudinal section, and the cerebral cortex was collected. Add proliferation medium (DMEM / F12, bFGF20ng / mL, EGF20ng / mL, 2% B27), filter through a 200-mesh filter, count cells after trypan blue staining, and adjust the number of cells to 1×10 6 / ml, transferred to culture flask, put into 5% CO 2 , Cultivated in a constant temperature incubator at 37°C, and passaged once every three days.

[0051] Take the logarithmic growth NSCs, digest with 0.25% EDTA trypsin for 2min, stop the digestion with 10% DMEM / F12...

Embodiment 3

[0054] Minocycline, also known as "minocycline" or "minocycline", is a broad-spectrum antibacterial tetracycline antibiotic with pharmacological properties such as long half-life and lipophilicity.

[0055] Due to the blood-brain barrier in the brain, direct administration of JWH133 is not easy to enter the brain to realize its function. After patients took it, it was found that the effect of JWH133 combined with minocycline was significantly better than that of patients who took JWH133 alone.

[0056] In view of this, the following animal experiments were carried out:

[0057] A rat cerebral hemorrhage model was constructed according to Example 1, and divided into a normal saline control group, a JWH133 alone group and a JWH133+minocycline group, and the number of microglial cells was detected after 7 days of administration. It was found that the number of microglia in the JWH133+minocycline group was 10% less than that in the JWH133 alone group. It can be seen that the com...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to the field of cerebral hemorrhage drugs, in particular to application of type-II cannabinoid receptor agonist in the preparation of drugs for inhibiting microglial cell proliferation and treating hypertensive cerebral hemorrhage after the treatment of hypertensive cerebral hemorrhage.In-vivo experiments show that the type-II cannabinoid receptor agonist is capable of inhibiting microglial cell proliferation and activation after cerebral hemorrhage, inhibiting perihematomal neurogenic inflammations and improving secondary brain injury caused by cerebral hemorrhage; in addition, in the use with the type-II cannabinoid receptor agonist, minocycline is capable of significantly increasing blood brain barrier penetration rate of the type-II cannabinoid receptor agonist and improving anti-inflammatory therapeutic effect.

Description

technical field [0001] The invention relates to the field of cerebral hemorrhage drugs, in particular to the application of type II cannabinoid receptor agonists in the preparation of drugs for inhibiting microglial cell proliferation and cerebral hemorrhage inflammation after treating hypertensive cerebral hemorrhage. Background technique [0002] Hypertensive intracerebral hemorrhage is one of the most serious complications of hypertension. It often occurs between 50 and 70 years old. It is often caused by rupture and hemorrhage of lenticular artery in the basal ganglia area, accompanied by neurological sequelae such as severe brain atrophy and neurological dysfunction. In addition to surgical removal of hematoma, cerebrospinal fluid drainage and other surgical methods, drugs are the main means to improve the sequelae of hypertensive cerebral hemorrhage. At present, there is no effective drug treatment clinically. [0003] Type II cannabinoid receptor (Cannabinoid Recepto...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K45/06A61K31/65A61P25/00A61P9/10
CPCA61K9/0019A61K9/08A61K9/19A61K9/2059A61K9/4866A61K31/352A61K31/65A61K45/06A61K47/10A61K2300/00
Inventor 陶一浩唐俊朱刚陈志陈前伟谭亮姜兵
Owner THE FIRST AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIVERSITY OF PLA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products