Application of PF429242 in preparation of depression treatment medicine

Abstract

The invention discloses an application of PF429242 in preparation of a depression treatment medicine. Through detection of three models including a chronic unpredictable stress (CMS) model, a social failure model (CSDS) and an LPS intraperitoneal injection induced depression model, it is found that the appropriate dosage of PF429242 has an obvious improvement effect on depressive symptoms; meanwhile, an immunofluorescence staining experiment finds that the damage of 5-hydroxytryptamine neurons can be effectively improved by using a proper amount of PF429242, so that the depression-like behavior is inhibited; moreover, according to electrophysiological experiments, the improvement of the depression symptom by the PF429242 is that the treatment effect of the PF429242 is achieved through an IL-1R1 target spot. Therefore, the PF429242 has a good clinical application prospect when being applied to the medicine for treating the depression.

Description

technical field [0001] The present invention relates to the use of compound PF429242 as a medicine, in particular to the use of PF429242 in preparing medicines for treating depression, and belongs to the field of medical technology. Background technique [0002] Depression is the most common mood disorder, and as of January 2021, there are more than 500 million depressed patients worldwide. Epidemiological statistics show that the incidence of depression is increasing year by year. Statistics in 2017 show that at least 800,000 depression patients commit suicide every year. Some statisticians have calculated that the incidence of depression in each person's life is 12%-17%. [0003] At present, there are three common depression models in the field of depression research, namely chronic unpredictable stress (Chronic mild stress, CMS) model, social failure model (chronic social defeat stress, CSDS) model, LPS intraperitoneal injection induced model of depression. [0004] CM...

AI Technical Summary

Problems solved by technology

[0008] The disorder of 5-HT system function is mainly divided into decreased 5-HT neurotransmitter synthesis and 5-HT reuptake disorder. Paroxetine is a representative drug of selective 5-HT reuptake inhibitor (Selective Serotonin Reuptake Inhibitor, SSRI) The clinical effect is not good, and the problem of drug tolerance has plagued many doctors and patients

Other antidepressant targets, such as selective serotonin and norepinephrine reuptake inhibitors (SSNRIs), such as venlafaxine; tricyclic antidepressants (TCAs), such as amitriptyline, have clinical effects even Can't compare to paroxetine

Therefore, combination drugs are generally used clinically, and excessive use of drugs will inevitably cause organ toxicity. Therefore, finding a new therapeutic target and alternative drugs has become a top priority for the treatment of depression.

However, so far, no drugs that have a good therapeutic effect on depression have been found

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