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Application of (E)-2-(3,5-dimethoxybenzylidene)-cyclopentanone in preparing medicines used for treating pain diseases

A drug and pain relief technology, applied in drug combinations, neurological diseases, antipyretics, etc.

Active Publication Date: 2014-12-31
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the invention of the present invention is to provide a new application of a compound to solve the above-mentioned defects in the existing analgesic drugs for painful diseases

Method used

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  • Application of (E)-2-(3,5-dimethoxybenzylidene)-cyclopentanone in preparing medicines used for treating pain diseases
  • Application of (E)-2-(3,5-dimethoxybenzylidene)-cyclopentanone in preparing medicines used for treating pain diseases
  • Application of (E)-2-(3,5-dimethoxybenzylidene)-cyclopentanone in preparing medicines used for treating pain diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] compound The effect on the hot plate response in mice, the compound is hereafter referred to as IV 7 .

[0024] 40 male mice were randomly divided into vehicle control group (model group, model) and IV 7 High, medium and low dose groups (50mg / kg, 35.4mg / kg and 25mg / kg), 10 rats in each group. Mice in each group were injected intraperitoneally with vehicle or IV 7 After 30, 60, 90 and 120 minutes hot plate reaction. The shorter the hot plate reaction time, the more severe the pain of the mice.

[0025] attached figure 1 for IV 7 Effects on hot plate responses in mice. mean±SD, n=10; compared with model group, **p 7 25mg / kg comparison, ▲ P﹤0.05, ▲▲ P﹤0.01.

[0026] figure 1 The results show that: compared with the model group (vehicle control group), IV 7 50mg / kg, 35.4mg / kg and 25mg / kg significantly prolong the hot plate reaction time of mice, and IV 7 The analgesic effect of 50mg / kg and 35.4mg / kg was significantly stronger than that of IV 7 25mg / kg, ins...

Embodiment 2

[0028] Compound IV 7 Effects on the writhing response in mice

[0029] 40 mice, half male and half male, were randomly divided into vehicle control group (model group, model) and IV 7 High, medium and low dose groups (50mg / kg, 35.4mg / kg and 25mg / kg), 10 rats in each group. Mice in each group were injected intraperitoneally with vehicle or IV 7 After 50 minutes, 1% acetic acid solution was injected intraperitoneally, and the times of writhing of mice in each group were recorded for 10-20 minutes after injection of acetic acid solution. Writhing response inhibition rate=(writhing number of times in the vehicle control group-IV 7 writhing times) / writhing times of vehicle control group×100%. The more times of writhing, the more severe the pain of the mice.

[0030] attached figure 2 for IV 7 Effects on the writhing response in mice. Mean ± SD, n=10; **p <0.01 compared with model group.

[0031] attached figure 2 Show: compare with model group (vehicle control group), I...

Embodiment 3

[0034] Cathepsin L specific inhibitor Clik 148 to compound IV 7 Analgesic effects

[0035] 60 mice, half male and half male, were randomly divided into 6 groups, respectively vehicle control group (model group, model), IV 7 50mg / kg group, Clik 148 10mg / kg group, Clik 148 20mg / kg group, IV 7 50mg / kg + Clik 148 10mg / kg group and IV 7 50mg / kg + Clik 148 20mg / kg group, 10 rats in each group. Mice in each group were injected intraperitoneally with vehicle or Clik 148 and intraperitoneally injected with vehicle or IV 7 After 50 minutes, 1% acetic acid solution was injected intraperitoneally, and the times of writhing of mice in each group were recorded for 10-20 minutes after injection of acetic acid solution. Writhing response inhibition rate=(writhing number of times in the vehicle control group-IV 7 writhing times) / writhing times of vehicle control group×100%. The more times of writhing, the more severe the pain of the mice.

[0036] attached image 3 Compound IV for C...

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Abstract

The invention discloses an application of (E)-2-(3,5-dimethoxybenzylidene)-cyclopentanone in preparing medicines used for treating pain diseases. Related studies show that the compound has a significant abirritation, and can effectively reduce pain reactions caused by thermal stimulation and chemical stimulation. The compound can be used for preparing medicines used for relieving acute pains, headache, toothache, neuralgia, tumor-type pain, and pains caused by inflammatory diseases of muscles and bone joints, wherein the acute pains are caused by severe injury, burns, etc., and the pains caused by the inflammatory diseases of the muscles and the bone joints comprise rheumatic and rheumatoid arthritis pains, dysmenorrheal and other inflammatory pains, and neuropathic pains.

Description

technical field [0001] The invention relates to the field of medicines, in particular to the application of (E)-2-(3,5-dimethoxybenzylidene)-cyclopentanone in the preparation of medicines for treating pain diseases. Background technique [0002] Pain (pain) is one of the most common clinical symptoms, which can usually be divided into several types: nociceptive pain, inflammatory pain and neuropathic pain. Nociception refers to the body's perception of noxious stimuli, while pain is the body's subjective response to noxious afferent stimuli, and protects tissues from injury through behavioral and reflex defenses. Nociceptive pain is mostly acute pain (such as extrusion, trauma, etc.). Inflammatory pain and neuropathic pain are mostly chronic pain (such as inflammation or tumors), which are caused by the activation of nociceptive pathways by noxious stimuli. [0003] Chronic pain can still occur spontaneously when tissue damage has stopped, which is often caused by damage t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/122A61P29/00A61P25/04A61P25/02A61P1/02
Inventor 敖桂珍张慧灵顾卫卫范加红荣加国朱永明
Owner SUZHOU UNIV
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