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Use of a phosphodiesterase 9a inhibitor for preventing and treating ischemic stroke

A technology for ischemic cerebral stroke and phosphodiesterase, applied in the field of medicine, can solve problems such as no PDE9A inhibitor, and achieve the effect of reducing behavioral damage and reducing volume

Active Publication Date: 2021-12-28
SUN YAT SEN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there is no application of PDE9A inhibitors as drugs for the treatment of ischemic stroke

Method used

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  • Use of a phosphodiesterase 9a inhibitor for preventing and treating ischemic stroke
  • Use of a phosphodiesterase 9a inhibitor for preventing and treating ischemic stroke
  • Use of a phosphodiesterase 9a inhibitor for preventing and treating ischemic stroke

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1. Effect of LW33 on Acute Cerebral Ischemia in Mice

[0025] (1) Experimental materials

[0026] Experimental animals: 60 SPF grade KM mice, male, weighing 16-20 g, purchased from the Experimental Animal Center of Sun Yat-sen University (permit number: SCXK (Guangdong) 2016-0029), free to eat and drink.

[0027] Main instruments: stopwatch (Shanghai Xingzuan Stopwatch Co., Ltd.), ACS-3H electronic balance (Zhongshan Jinli Electronic Scaling Instrument Co., Ltd.), surgical instruments (Beijing Seinong Technology Co., Ltd.).

[0028] Main reagents: LW33 (School of Pharmacy, Sun Yat-Sen University), Nimodipine Tablets (Guangdong South China Pharmaceutical Group Co., Ltd.), sodium carboxymethylcellulose (Tianjin Zhiyuan Chemical Reagent Co., Ltd.).

[0029] (2) Experimental method

[0030] 60 male KM mice were randomly divided into 5 groups according to weight balance: control group (0 mg / kg), LW33 low dose group (1 mg / kg), LW33 medium dose group (3 mg / kg), LW33 ...

experiment example 2

[0038] Experimental example 2. Effect of LW33 on model mice resistant to normal pressure and hypoxia

[0039] (1) Experimental materials

[0040] Experimental animals: 72 SPF grade KM mice, male, weighing 16-20 g, purchased from the Experimental Animal Center of Sun Yat-sen University (permit number: SCXK (Guangdong) 2016-0029), free to eat and drink.

[0041] Main instruments: stopwatch (Shanghai Xingzuan Stopwatch Co., Ltd.), ACS-3H electronic balance (Zhongshan Jinli Electronic Scaling Instrument Co., Ltd.), 1mL syringe (Jiangsu Zhengkang Medical Instrument Co., Ltd.), surgical instruments (Beijing Seinong Technology Co., Ltd.).

[0042] Main reagents: LW33 (School of Pharmacy, Sun Yat-sen University), Nimodipine Tablets (Guangdong South China Pharmaceutical Group Co., Ltd.), Sodium Carboxymethylcellulose (Tianjin Zhiyuan Chemical Reagent Co., Ltd.), Isoproterenol Hydrochloride Injection (Shanghai He Feng Pharmaceutical Co., Ltd.), soda lime (Tianjin Damao Chemical Reagent F...

Embodiment 3

[0052] Example 3. The acute phase protective effect of LW33 on MCAO model rats

[0053] (1) Experimental materials

[0054] Experimental animals: 48 SPF grade SD rats, male, weighing 200-240 g, purchased from the Experimental Animal Center of Sun Yat-sen University (permit number: SCXK (Guangdong) 2016-0029), free to eat and drink.

[0055] Main instruments: ACS-3H electronic balance (Zhongshan Jinli Electronic Weighing Apparatus Co., Ltd.), LDZ5-2 centrifuge (Beijing Medical Centrifuge Factory), HH-W600 digital display three-purpose constant temperature water tank (Jiangsu Jintan Ronghua Instrument Manufacturing Co., Ltd. Company), 1mL syringe (Jiangsu Zhengkang Medical Devices Co., Ltd.), surgical instruments (Beijing Xinong Technology Co., Ltd.).

[0056] Main reagents: LW33 (School of Pharmacy, Sun Yat-sen University), Nimodipine Tablets (Guangdong South China Pharmaceutical Group Co., Ltd.), sodium carboxymethylcellulose (Tianjin Zhiyuan Chemical Reagent Co., Ltd.), 2% s...

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Abstract

The invention relates to the use of a phosphodiesterase 9A (PDE9A) inhibitor for preventing and treating ischemic stroke. PDEs are a large multigene family, including 11 subtypes and 30 subtypes, among which phosphodiesterase 9A (PDE9A) specifically acts on cGMP. The LW33(I) of the present invention is a PDE9A inhibitor, which can be used to prevent or / and treat the related disease symptoms of ischemic cerebral apoplexy, and can be used to prepare drugs that reduce cerebral infarction in middle cerebral artery ischemia (MCAO) rats. The volume, the medicine that alleviates behavioral injury, can be used for preparing the medicine that raises the SOD content in plasma of MCAO rats, reduces IL-1β, IL-6, TNF-α, MDA content in plasma, can be used for preparing the tissue that influences MCAO rat Drugs for pathological structures.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a phosphodiesterase inhibitor for preventing and treating ischemic cerebral apoplexy and its application. Background technique [0002] Stroke is a disease in which nerve function is damaged or lost due to insufficient blood supply to the brain [1]. According to the estimates of the World Health Organization, more than 15 million people suffer from stroke every year in the world, which is equivalent to 1 person in every 400 people suffers from stroke. People of all ages are at risk of stroke, including children and infants, although people over 65 make up the majority of stroke patients. Statistics show that only about 15% of all surviving stroke patients can recover, and the remaining 75% will be left with different degrees of disabilities such as disturbance of consciousness, hemiplegia, and aphasia. [0003] At present, there are two main methods for the treatment of cereb...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/519A61P9/10
CPCA61K31/519A61P9/10
Inventor 刘培庆陈健文罗海彬刘鑫巍李卓明王权路静
Owner SUN YAT SEN UNIV
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