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Sigma receptor stimulant polypeptide and application

A receptor agonist and sequence technology, applied in the direction of peptides, depsipeptides, specific peptides, etc., can solve the problems of no Sigma-1 receptor activators, reduce forced swimming time, improve depression symptoms, and reduce tail suspension the effect of time

Inactive Publication Date: 2017-02-01
SUZHOU PULUODA BIOLOGICAL SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At this stage, no Sigma-1 receptor activators are available

Method used

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  • Sigma receptor stimulant polypeptide and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Effects of Sigma receptor agonist peptides on BDNF content in brain tissue of chronic unpredictable stress model rats.

[0017] SD rats were used as test animals, and 60 rats, half male and half male, with a body weight of 180-220 g, were randomly divided into 6 groups, high-dose group, middle-dose group, low-dose group, positive control group, model group, Blank group, 10 rats in each group. Establish a rat chronic unpredictable stress model: the stress content is: restraint for 4 hours; wet bedding overnight; shaking for 1 hour (160r / min); fasting for 12 hours; Clamp the tail for 1 min; crowd overnight (8 / cage). Two stresses were used during the day, and one stress was used at night, and the stress was continued for 4 weeks. Administer after the last stimulation. Dosing regimen: the treatment group was subcutaneously injected with the polypeptide of the present invention at doses of 20, 10, 5, and 2.5 mg / Kg, the control group was given fluoxetine at a dose of 10 mg...

Embodiment 2

[0023] Effects of sigma receptor agonist peptides in a mouse forced-swim stress hopelessness model.

[0024] Using ICR mice as the test animals, 50 mice, half male and half male, weighing 18-22g, were randomly divided into 5 groups: high-dose group, middle-dose group, low-dose group, positive control group, blank group, Each group l0. The treatment group was subcutaneously injected with the polypeptide of the present invention at doses of 20, 10, 5, and 2.5 mg / Kg, the control group was given fluoxetine at a dose of 10 mg / Kg, and the blank group was given normal saline for 7 consecutive days. One hour after administration on the seventh day, the mice were subjected to a forced swimming test. The mice were forced to swim in water at 20-25°C for 6 minutes, and the immobility time within 4 minutes after recording was recorded. The time spent floating with the head out of the water is used to evaluate the effect of the polypeptide of the present invention on the model of mouse for...

Embodiment 3

[0030] Effects of sigma receptor agonist peptides on a mouse tail-suspension stress hopelessness model.

[0031] Using ICR mice as the test animals, 50 mice, half male and half male, weighing 18-22g, were randomly divided into 5 groups: high-dose group, middle-dose group, low-dose group, positive control group, blank group, Each group l0. The treatment group was subcutaneously injected with the polypeptide of the present invention at doses of 20, 10, 5, and 2.5 mg / Kg, the control group was given fluoxetine at a dose of 10 mg / Kg, and the blank group was given normal saline for 7 consecutive days. 1h after administration on the 7th day, the mice were subjected to a tail-suspension test, and the mice were fixed with adhesive tape at a place about 1 cm from the end of their tails, and the mice were kept in a suspended state for 6 minutes, and the immobility time of 4 minutes after recording was used to evaluate this product. Effects of Invention Peptides on a Mouse Tail Suspensio...

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Abstract

The invention relates to the field of medicine, in particular to polypeptide with the effects of stimulating a Sigma-1 receptor, up-regulating the brain-derived neurotrophic factor level and relieving the depressive symptom. The sequence of the polypeptide is a brand-new sequence, and the polypeptide has the advantage of being capable of increasing the BDNF content in chronic unpredictable stress model rat brain tissue. The pharmacological result shows that the polypeptide can relieve the depressive symptom of acute and chronic depression model animals. The polypeptide can serve as an effective candidate treatment method for clinical depression and has potential new medicine development value.

Description

technical field [0001] The invention relates to a Sigma receptor agonist polypeptide and its application, in particular to a polypeptide capable of stimulating Sigma-1 receptors, up-regulating the level of brain-derived neurotrophic factors, and alleviating depression symptoms. Background technique [0002] Depression, also known as depressive disorder, is the main type of mood disorder with significant and persistent low mood as the main clinical feature. It can be seen clinically that the mood is not commensurate with the situation. The depression of mood can range from gloomy to distraught, low self-esteem and depression, even pessimistic world-weariness, and there may be suicide attempts or behaviors; even stupor; some cases have obvious anxiety and motor agitation; In severe cases, psychotic symptoms such as hallucinations and delusions may appear. Each attack lasts for at least 2 weeks, or even several years in the elderly. Most cases have a tendency to recur. Most of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/00A61K38/16A61P25/24
CPCA61K38/00C07K14/001
Inventor 罗瑞雪
Owner SUZHOU PULUODA BIOLOGICAL SCI & TECH
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