Chalcone compound having function of improving sleep

A technology to improve sleep and compounds, applied in organic chemistry, drug combination, nervous system diseases, etc.

Active Publication Date: 2014-09-03
WENZHOU MEDICAL UNIV
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  • Abstract
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  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there is no research report on chalcone drugs that play a role in improving sleep from multiple levels. The inventors have designed and synthesized a series of chalcone compounds through long-term and arduous research experiments, and finally obtained a series of chalcone compounds, which were tested for pharmacological activity. They were found to have good sleep-improving activity

Method used

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  • Chalcone compound having function of improving sleep
  • Chalcone compound having function of improving sleep
  • Chalcone compound having function of improving sleep

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 Compound A172 sedative research

[0023] 40 male mice were selected and randomly divided into 4 groups, 10 in each group. The vehicle group was intraperitoneally injected with normal saline, and the drug intervention group was intraperitoneally injected with compound A172 at doses of 10mg / kg and 40mg / kg respectively; the volume was 0.1ml / 10g , The administration time is at 9:00. After 30 minutes of administration, the mice were first placed in the mouse autonomic activity counter for 5 minutes to adapt, and after 5 minutes, the instrument was turned on to measure the number of autonomic activities of the mice in each group within 5 minutes.

[0024] The experimental results are shown in Tab.1. Compared with the blank group, compound A172 at doses of 10 mg / kg and 40 mg / kg can significantly reduce the number of autonomous activities of mice per unit time (P figure 2 ).

[0025] Tab.1 compound A172 on the autonomous activity of mice

[0026]

[0027] Compa...

Embodiment 2

[0028] The effect of embodiment 2 compound A172 on the sleep time of mice caused by sodium pentobarbital

[0029] Experimental animals KM mice were fed for one week under the experimental conditions to adapt to the environment. After 7 days, 75 KM mice were randomly divided into 5 groups according to the regionalization of body weight, which were blank group, vehicle group, high and low dose of drug intervention group and positive drug group, 15 in each group. Compound A172 intervention high-dose and low-dose groups were given 10 mg / kg and 40 mg / kg drug solutions by intraperitoneal injection respectively. The positive drug group was intraperitoneally injected with 50 mg / kg of promethazine, and the vehicle group was intraperitoneally injected with an equal volume of normal saline for 4 consecutive days. Except for the positive drug group, the experimental animals in the other groups were administered at 9:00 am 30 minutes after the last administration. Pentobarbital sodium 50 mg...

Embodiment 3

[0034] Example 3 Effect of compound A172 on 5-HT content in hippocampus and hypothalamus of mouse brain

[0035] Experimental animals KM mice were fed for one week under the experimental conditions to adapt to the environment. After 7 days, 30 KM mice were randomly divided into two groups according to the regionalization of body weight, namely the blank control group and the 40mg / kg compound A172 administration group , 15 mice in each group, and the blank group was injected with the same volume of normal saline for 4 consecutive days. The last administration was carried out at 8:30 in the morning. 30 minutes after the administration, the brain was decapitated and the hypothalamus of the mouse brain was isolated on an ice board. and the hippocampus, after precise weighing with an analytical balance, add 9 times the mass of normal saline, homogenize in an ice bath for 3 minutes, collect all the homogenate, and centrifuge in a centrifuge at 3000r / min for 10 minutes, then take the ...

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Abstract

The invention provides a chalcone compound having a function of improving sleep. The chalcone compound is used as a bulk drug for preparing various dosage types of medicines for calming and soothing the nerves or the medicines related to improvement of the sleep, and has medical application in treatment and improvement on diseases related to the sleep.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, in particular, the invention relates to the chemical structure of a novel chalcone compound with the function of improving sleep. In addition, the present invention also relates to the sleep-improving mechanism and application of the compound. Background technique [0002] The significance of sleep is to regulate the circadian changes of the human body and the environment so that they can be coordinated and unified, so as to ensure the relative stability of human physiological and ecological activities. Sleep accounts for a third of the life cycle and is almost as vital as food. However, with the acceleration of the pace of society and the increasing pressure of life, sleep disorders caused by various reasons are on the rise year by year. According to statistics, about 27% of people in the world suffer from sleep disorders, and in my country alone there are about 300 million adults suffering ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C49/84A61P25/20
CPCC07C49/84
Inventor 刘志国金利泰丛维涛玄元虎于擎朱忠欣
Owner WENZHOU MEDICAL UNIV
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