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Novel use of bisbenzylisoquinoline compounds or pharmaceutically acceptable salts thereof in treating or improving depressive symptom

A technology of bisbenzylisoquinoline and compounds, applied in the field of new applications of bisbenzylisoquinoline compounds or their pharmaceutically acceptable salts in the treatment and improvement of depressive symptoms, capable of solving problems such as no reports

Inactive Publication Date: 2013-10-23
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The application of the structural compound of formula (I) in the treatment and improvement of depression and its symptoms has not been reported so far

Method used

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  • Novel use of bisbenzylisoquinoline compounds or pharmaceutically acceptable salts thereof in treating or improving depressive symptom
  • Novel use of bisbenzylisoquinoline compounds or pharmaceutically acceptable salts thereof in treating or improving depressive symptom
  • Novel use of bisbenzylisoquinoline compounds or pharmaceutically acceptable salts thereof in treating or improving depressive symptom

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0012] Experimental example 1, the effect of bisbenzylisoquinoline (BBI) derivatives represented by formula (I) on the immobility time of mice forced to swim.

[0013] The immobility of mice in the forced-swim model mirrors the animal's desperation behavior and mimics the depressive state in humans. Put the mice into a cylindrical glass jar with a height of 20 cm and a diameter of 10 cm, with a water depth of 15 cm and a water temperature of 25±1°C. The mice were pre-swimmed for 15 minutes before the experiment, then taken out, dried in a warm place, and then put back into the cage. Within 24 hours, the mice were administered intragastrically, and 60 minutes later, the mice were placed in the above-mentioned environment, and the cumulative immobility time of the mice in the last 5 minutes after swimming in the tank for 6 minutes was measured. The shortening of immobility time was used as an index to judge the antidepressant effect of drugs.

[0014] Experimental grouping: mi...

experiment example 2

[0018] Experimental example 2, the effect of bisbenzylisoquinoline (BBI) derivatives represented by formula (I) on the tail suspension time of mice.

[0019] Same as Experiment 1, the immobility state of mice in the forced swimming model reflects the desperate behavior of animals, which can simulate the depressive state of humans. Mouse tail suspension test: 60 minutes after intragastric administration of mice, stick the mouse tail on a sling with glue strips at a distance of 2 cm from the tail tip of the mouse and hang it for 1 minute, and record the immobility time for 5 minutes.

[0020] Experimental grouping: mice were randomly divided into solvent control group (distilled water gavage), derivative (low: 15mg / kg; middle: 30mg / kg; high: 60mg / kg, gavage) group, and imipramine was a positive control ( 40mg / kg, gavage) group.

[0021] Table 2. Effect of derivatives on tail suspension time of rats (means±SEM, n=7).

[0022]

[0023] *P<0.05, **P<0.01 vs. control group (Stu...

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Abstract

Disclosed is a new application of a bisbenzylisoquinoline derivative shown in formula (I) in the specification or pharmaceutically acceptable salt thereof. The application is an application of the bisbenzylisoquinoline derivative shown in formula (I) or the pharmaceutically acceptable salt thereof in preparing medicines or health care products for curing depression and easing depression symptom. The bisbenzylisoquinoline derivative shown in formula (I) or the pharmaceutically acceptable salt thereof can be taken as an effective component to prepare a drug type of any form. A result of an animal experiment shows that, the bisbenzylisoquinoline compound shown in formula (I) or the pharmaceutically acceptable salt thereof can obviously shorten immobility time of a mouse in a forced swimming test and immobility time of the mouse in a tail suspending test, which shows an anti-depression function. The present invention is applicable to various types of depression.

Description

technical field [0001] The present invention relates to the preparation of bisbenzyl isoquinoline compounds or pharmaceutically acceptable salts thereof with the general structural formula shown in the figure except tetrandrine and fangchinoline for the treatment of depression The application in drugs or health care products for depression and depression symptoms. Background technique [0002] The structural formula of bisbenzylisoquinolines, as shown in formula (I): [0003] [0004] Among them, R 1 Is hydrogen, or a straight chain or branched chain alkyl group containing 1-10 carbon atoms; R 2 , R 3 , R 4 and R 5 Respectively one of the following groups: hydrogen, substituted acyl, linear or branched alkyl, and the alkyl can be interrupted by heteroatoms selected from O, N, S; R 2 , R 3 , R 4 and R 5 It can also be O or S together. x 1 , X 2 , X 3 and x 4 may be the same or different, and each independently is a halogen atom, nitro, hydroxyl, or a linear o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4748A61P25/24
CPCA61K31/4748A61P25/24C07D498/16
Inventor 张永鹤盛兆福张雪琼
Owner PEKING UNIV
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