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

A disease and drug technology, applied in drug combinations, nervous system diseases, antipyretics, etc.

Active Publication Date: 2013-11-13
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 Effect on the hot plate response of mice, the compound is referred to as IV in the following 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), each group contains 10 animals. Each group of mice were injected with vehicle or IV into the abdominal cavity 7 After 30, 60, 90 and 120 minutes hot plate reaction. The shorter the hot plate reaction time, the more severe the pain in mice.

[0025] Attached figure 1 For IV 7 The effect on the hot plate reaction of mice. mean±SD, n=10; compared with the 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 is significantly stronger than that of IV 7 25mg...

Embodiment 2

[0028] Compound IV 7 Effect on writhing response in mice

[0029] 40 mice, half male and half male, 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), each group contains 10 animals. Mice in each group were injected with vehicle or IV into the abdominal cavity 7 After 50 minutes, 1% acetic acid solution was intraperitoneally injected, and the number of writhing times of mice in each group was recorded for 10-20 minutes. Inhibition rate of writhing response = (number of writhing in the vehicle control group-IV 7 Number of writhing) / Number of writhing in the solvent control group×100%. The more writhing times, the more severe the pain in mice.

[0030] Attached figure 2 For IV 7 The effect on the writhing response of mice. Mean ± SD, n=10; compared with the model group, **p <0.01.

[0031] Attached figure 2 Show: Compared with the model group (vehicle control group), IV 7 50mg / kg, 35.4mg / kg ...

Embodiment 3

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

[0035] 60 mice, half male and half male, were randomly divided into 6 groups, namely the 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 animals in each group. Each group of mice was injected with vehicle or Clik 148 into the abdominal cavity and injected with vehicle or IV into the abdominal cavity. 7 After 50 minutes, 1% acetic acid solution was intraperitoneally injected, and the number of writhing times of mice in each group was recorded for 10-20 minutes. Inhibition rate of writhing response = (number of writhing in the vehicle control group-IV 7 The number of writhing) / the number of writhing in the solvent control group × 100%. The more writhing times, the more severe the pain in mice.

[0036] Attached image 3 For Clik 148 to compound IV 7 ...

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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 Applications(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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