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New application of 7-chloro sulfur kynurenic acid in preparing drugs for preventing and/or treating tristimania

A technology for kynuric acid and depression, applied in the field of 7-chlorothiokynuric acid, can solve the problems of poor curative effect and slow onset of effect

Active Publication Date: 2014-11-26
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These drugs can improve the depressive symptoms of patients to a certain extent, but there are inevitably some limitations in the treatment, such as slow onset of action, and most patients need to take the drugs continuously for several weeks or even months to make their condition better. , the efficacy of these drugs is relatively poor, only about 60% of patients can play a therapeutic role, and most of these drugs are accompanied by gastrointestinal reactions, headache, drowsiness or insomnia, sexual dysfunction and other adverse reactions

Method used

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  • New application of 7-chloro sulfur kynurenic acid in preparing drugs for preventing and/or treating tristimania
  • New application of 7-chloro sulfur kynurenic acid in preparing drugs for preventing and/or treating tristimania
  • New application of 7-chloro sulfur kynurenic acid in preparing drugs for preventing and/or treating tristimania

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment 1, investigate the influence of 7-chlorothiokynuuric acid on the spontaneous activity of rats

[0019] The experimental animals were Sprague-Dawley (SD) rats, male, purchased from Beijing Weitong Lihua Experimental Animal Technology Co., Ltd., license number: SCXK (Beijing) 2002-2003, body weight 220-240 g. The animal room is kept at constant temperature and humidity (temperature 22±2°C, humidity 50±10%), controlled by 12-hour circadian rhythm (8:00-20:00). Before the start of the experiment, the animals were acclimatized in the animal room for 5-7 days, and had free access to water and food.

[0020] 7-Chlorothiokynuric acid (purchased from Enzo Life Science Technology Company, USA, product number: 550-067-M005) was dissolved in normal saline containing 10% DMSO, and administered by intraperitoneal injection.

[0021] The rats were randomly divided into 3 groups, 8 in each group. These 3 groups of rats were injected with 0.9% normal saline, 0.1mg / kg 7-chlor...

Embodiment 2

[0024] Embodiment 2, investigate the influence of 7-chlorothiokynuuric acid on the immobility time of forced swimming test rats

[0025] The swimming device is made of transparent plexiglass (glass cylinder height 65cm, diameter 25cm, water depth 45cm, water temperature 24±1°C). The day before the experiment, the rats were placed in the plexiglass cylinder. After 15 minutes of adaptation, the rats were Dry the body and put it back in the cage. After 24 hours, 24 rats were randomly divided into 3 groups, 8 rats in each group, and these 3 groups of rats were injected with 0.9% normal saline, 0.1mg / kg 7-chlorothiokynuric acid and 1mg / kg 7 - Chlorothiokynuric acid, after 60 minutes of administration, the rats were placed in the swimming device in turn, and the time for the rats to float within 5 minutes was recorded. The floating immobility time is defined as the time when the rat curls up its body slightly and is in a floating state (the forced swimming test is a classic antidep...

Embodiment 3

[0029] Example 3. To investigate the influence of 7-chlorothiokynuuric acid on the number of evasion mistakes and the evasion latency of rats in the acquired helplessness experiment

[0030] In order to further verify the rapid antidepressant effect of 7-chlorothiokynuuric acid, we observed the effects of 7-chlorothiokynuric acid on the number of escape mistakes and escape latency in rats in the acquired helplessness experiment. The rat acquired helplessness experimental device is a rat shuttle test box, the bottom of which is equipped with a 38V stainless steel grid (50cm×20cm×16cm), with a baffle in the center to separate the shuttle into two equal parts, purchased from Shanghai Jiliang Software Technology Co., Ltd. (Model: JLBehv-STR-8).

[0031] The experiment was divided into three days. On the first day, the rats were first put into one end of the shuttle box, and the baffle was closed to allow them to adapt to the test environment for 3 minutes. Then, 60 inescapable foo...

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Abstract

The invention discloses new application of 7-chloro thiokynurenic acid. The new application is the application of 7-chloro thiokynurenic acid or a pharmaceutically acceptable salt, an ester or a solvate in preparing drugs for preventing and / or treating tristimania. Results in pharmacodynamics experiments show that 7-chloro thiokynurenic acid remarkably shortens a dead time of a rat in a forced swimming experiment, and remarkably reduces mistake escaping times and an escaping incubation period of the rat in a learned helplessness experiment, while not changing the spontaneous activity of the rat. The new application shows that 7-chloro thiokynurenic acid has the function of depression resistance and has the potential of rapidly effective depression resistance, so that 7-chloro thiokynurenic acid can be used for treating the tristimania caused by various factors.

Description

technical field [0001] The invention relates to a new application of 7-chlorothiokynuric acid. Background technique [0002] Depression is a serious emotional disorder mental disease, which is chronic and recurrent. Its clinical manifestations are diverse, such as appetite and sleep disorders, slow thinking and response, loss of interest and happiness, pessimism and world-weariness, and suicide in severe cases. thoughts and actions. According to the World Health Organization, the current global incidence of depression is about 17%. Depression will become the leading cause of human disability by 2020. With the increasing pace of life in modern society, increasing competitive pressure and mental pressure, more and more people are suffering from depression. The incidence rate in 1999 was 0.64%. By 2009, the incidence of depression in my country It is about 3%-5%, which has caused great harm to patients and society, so antidepressant treatment is urgent. [0003] At present, ...

Claims

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Application Information

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IPC IPC(8): A61K31/47A61P25/24
Inventor 陆林朱维莉王慎军刘萌萌丁增波
Owner PEKING UNIV
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