Application of compound 6-(4-chlorophenoxy)-tetrazolo [5,1-a] phthalazine to preparation of medicine for treating depression

A compound and technology for depression, applied in the field of pharmaceutical preparations for the treatment of depression, can solve the problems of poor antidepressant effect, obvious toxic and side effects, etc.

Active Publication Date: 2013-01-23
JILIN YINGLIAN SHANGDE SCI & TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, about 1/3 of the depressed patients in the world do not respond well to clinically used a

Method used

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  • Application of compound 6-(4-chlorophenoxy)-tetrazolo [5,1-a] phthalazine to preparation of medicine for treating depression
  • Application of compound 6-(4-chlorophenoxy)-tetrazolo [5,1-a] phthalazine to preparation of medicine for treating depression
  • Application of compound 6-(4-chlorophenoxy)-tetrazolo [5,1-a] phthalazine to preparation of medicine for treating depression

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The compound of formula I can significantly shorten the immobility time of mice in the forced swimming test.

[0024] 50 male mice were randomly divided into 5 groups, 10 in each group. 5 groups of mice were given vehicle (0.3% methylcellulose solution, 20mL / kg, intragastrically), three doses of formula I compounds (5, 10 and 20mg / kg, intragastrically), and imipramine ( 10mg / kg, orally), once a day for 7 consecutive days. One hour after administration on days 3 and 7, all mice were subjected to the forced swimming test (FST). The immobility time of mice was observed and recorded, and SPSS statistical analysis was performed on the data. See figure 1 .

[0025] The results show that the compound of formula I can significantly shorten the immobility time of mice in the forced swimming test in a dose-dependent manner.

Embodiment 2

[0027] The compound of formula I can significantly shorten the immobility time of mice in the tail suspension test.

[0028] 50 male mice were randomly divided into 5 groups, 10 in each group. 5 groups of mice were given vehicle (0.3% methylcellulose solution, 20mL / kg, intragastrically), three doses of formula I compounds (5, 10 and 20mg / kg, intragastrically), and imipramine ( 10mg / kg, orally), once a day for 7 consecutive days. One hour after administration on days 3 and 7, all mice were subjected to a tail suspension test (TST). The immobility time of mice was observed and recorded, and SPSS statistical analysis was performed on the data. See figure 2 .

[0029] The results show that the compound of formula I can significantly shorten the immobility time of mice in the tail suspension test in a dose-dependent manner.

Embodiment 3

[0031] The compound of formula I has no significant effect on the indicators of spontaneous activity of mice in the open-field test.

[0032] 50 male mice were randomly divided into 5 groups, 10 in each group. 5 groups of mice were given vehicle (0.3% methylcellulose solution, 20mL / kg, intragastrically), three doses of the compound of formula I (5, 10, and 20mg / kg, intragastrically), and fluoxetine (20mg / kg, intragastric administration), once a day, for 7 consecutive days. One hour after administration on day 7, open-field experiments were performed on all mice. Observe and record the number of crawling frames, upright times, and grooming times of the mice, and perform SPSS statistical analysis on the data. See image 3 .

[0033] The results show that the compound of formula I has no effect on various indicators of mouse locomotor activity, thereby excluding the possibility that the compound of formula I is a false positive result in FST and TST.

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Abstract

The invention relates to the use of a compound (shown in formula I) as a medicine for treating depression.

Description

technical field [0001] The present invention relates to the use of 6-(4-chlorophenoxy)-tetrazolo[5,1-a]phthalazine in the preparation of pharmaceutical preparations for treating depression. Background technique [0002] Depression is the main type of affective disorder (Mood Disorder), which is a syndrome characterized by significant and persistent low mood. With the fast-paced and mental and psychological pressure brought by the market economy, the incidence of depression has increased significantly. According to a survey by the World Psychiatric Association, the global incidence of depression is 4.2%, and it reaches 6.9% in China, and the number of patients with depression is increasing at an annual growth rate of 113%. According to statistics, the cost of absenteeism, loss of work ability, treatment and rehabilitation caused by patients with depression in my country reaches hundreds of billions of yuan a year. Depression has become a recognized medical and sociological ...

Claims

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Application Information

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IPC IPC(8): A61K31/5025A61P25/24
Inventor 全哲山于海玲邓先清
Owner JILIN YINGLIAN SHANGDE SCI & TECH DEV
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