Application of LIM kinase inhibitor LIMKi3 to preparation of drug for treating pains

A kinase inhibitor and drug technology, which can be used in drug combinations, antipyretics, anti-inflammatory agents, etc., can solve the problem of unmet needs for pain control, and achieve the effect of delaying pain phenotype and treating pain.

Active Publication Date: 2017-05-31
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Whether Acute Pain or Chronic Pain, there is a clinically unmet need for pain control

Method used

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  • Application of LIM kinase inhibitor LIMKi3 to preparation of drug for treating pains
  • Application of LIM kinase inhibitor LIMKi3 to preparation of drug for treating pains
  • Application of LIM kinase inhibitor LIMKi3 to preparation of drug for treating pains

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1. Intrathecal administration of LIMKi3 can significantly inhibit the phosphorylation level of proteins downstream of LIM kinase

[0024] a) Test animals: healthy adult C57bl / 6 mice, clean grade, weighing 20-25 g. The experimental animals were raised in an independent environment with 12h-12h alternation of day and night, the room temperature was maintained at 24±2°C, water and food were free to drink, and the experiment was carried out after 1 week of adaptation to the environment. All handling of animals followed the requirements of the Ethics Committee of the International Association for the Study of Pain.

[0025] b) Experimental drug: the drug LIMKi3, with a purity >98%, is commercially available (purchased from Calbiochem). Dimethylsulfoxide (DMSO), commercially available. Tris, TEMED, Bovine Serum Albumin, β-Mercaptoethanol, glycine, glycerol, Tween-20, bromophenol blue, SDS, Triton 100, Marker were purchased from Sunshine; 30% Acrylamide / Bis, Ammonium...

Embodiment 2

[0033] Example 2. Intrathecal administration of LIMKi3 can significantly inhibit the inflammatory pain phenotype

[0034] a) Test animals:

[0035] Healthy C57bl / 6 mice, clean grade, weighing 20-25g. The experimental animals were raised in an independent environment with 12h-12h alternation of day and night, the room temperature was maintained at 24±2°C, water and food were free to drink, and the experiment was carried out after 1 week of adaptation to the environment. All handling of animals followed the requirements of the Ethics Committee of the International Association for the Study of Pain.

[0036] b) Test drugs and reagents:

[0037] The drug LIMKi3, with a purity >98%, is commercially available (purchased from Calbiochem). Dimethylsulfoxide (DMSO), commercially available.

[0038] c) Test method:

[0039] Inflammatory pain model: After the mice were preserved, inject 20 microliters of a 1:1 mixture of complete Freund's adjuvant and saline into the soles of the mice...

Embodiment 3

[0046] Example 3. The effect of intrathecal administration of LIMKi3 on the pain phenotype of preserved nerve injury

[0047] a) Test animals:

[0048] Healthy C57bl / 6 mice, clean grade, weighing 20-25g. The experimental animals were raised in an independent environment with 12h-12h alternation of day and night, the room temperature was maintained at 24±2°C, water and food were free to drink, and the experiment was carried out after 1 week of adaptation to the environment. All handling of animals followed the requirements of the Ethics Committee of the International Association for the Study of Pain.

[0049] b) Test drugs and reagents:

[0050] The drug LIMKi3, with a purity >98%, is commercially available (purchased from Calbiochem). Dimethylsulfoxide (DMSO), commercially available.

[0051] c) Test method:

[0052] Preserved nerve injury model: After mice are anesthetized, cut the skin and bluntly separate the muscles to see the main trunk of the sciatic nerve and its ...

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PUM

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Abstract

The invention discloses application of a LIM kinase inhibitor LIMKi3 to preparation of a drug for treating pains. Compared with the prior art, the LIM kinase inhibitor LIMKi3 has the advantages that generation of pains can be affected obviously, pain phenotype can be relieved or delayed, and pains can be effectively treated by using the LIM kinase inhibitor LIMKi3 alone or together with other analgesic drugs.

Description

technical field [0001] The invention belongs to the technical field of new application of drugs, and relates to the new application of LIM kinase inhibitor (LIMKi3) in the field of analgesic drugs. Background technique [0002] Pain (after breathing, pulse, blood pressure, and body temperature can be listed as the fifth major vital sign of a person. It refers to an unpleasant sensory and emotional experience caused by various stimuli that are actually damaged or have potential tissue damage risks. Pain can be divided into three categories according to its characteristics: nociceptive pain, inflammatory pain and neuropathic pain. Nociceptive pain is caused by noxious stimuli and is a self-protection mechanism of the human body. Stimulation, to avoid further damage to the body caused by stimulation, so as to protect the health of the body. Inflammatory pain involves tissue damage and infiltration of immune cell products. Inflammatory factors will induce and maintain nociceptor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/427A61P29/00A61P25/02A61P25/04
CPCA61K31/427
Inventor 周子凯杨翔宇刘文涛吴俊华谢维
Owner SOUTHEAST UNIV
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