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Application of CDN1163 in preparation of medicine for relieving or treating neuropathic pain

A CDN1163, neurological technology, applied in the field of neurological drugs, can solve problems such as inability to infer, and achieve the effects of inhibiting the increase in neuronal excitability, improving activation, and improving mechanical pain sensitivity

Active Publication Date: 2021-04-30
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] So far, there is no report about the drug containing the SERCA2 agonist CDN1163 for the treatment of neuropathic pain, and it is impossible to infer from the known properties of CDN1163 whether it plays a role in relieving neuropathic pain in drugs by stimulating SERCA2

Method used

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  • Application of CDN1163 in preparation of medicine for relieving or treating neuropathic pain
  • Application of CDN1163 in preparation of medicine for relieving or treating neuropathic pain
  • Application of CDN1163 in preparation of medicine for relieving or treating neuropathic pain

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035]This example is intended to illustrate the use of CDN1163 by CDN1163 to reduce chronic sciatic injury, CCI) rat mechanical pain threshold and heat pain in the preparation of mitigation or therapeutic neuropathic pain drug.

[0036]Experimental animal

[0037]Purchased from 50 male SD rats in Qinglong Mountain, Nanjing, Jiangning District, where the rats were placed in a quiet and removal of strong light, and the light and dark time ratio were 1: 1, Room temperature was controlled at 22-25 ° C, humidity, and rats were free to eat and drink water.

[0038]2. Experimental drugs and consumables

[0039]

[0040]3. Experimental equipment and equipment

[0041]

[0042]Glass separation, sterilization gauze, tissue, cotton swab, trace syringe.

[0043]4. Experimental method

[0044]4.1 Random Group

[0045]Take 10 cages with marker pen, the animal temporary number is the first cage 1 ~ 5, the second cage 6 ~ 10, sequentially to the 10th cage 46 ~ 50, randomly crawled the rat weighing, each cage Placed 5, and use ...

Embodiment 2

[0056]This example is used to illustrate the improved L of the CDN1163 provided by the present invention.5 Application of DRG form in the preparation of mitigation or treatment of neuropathic pain drugs.

[0057]Experimental drugs and consumables

[0058]

[0059]2. Experimental equipment and equipment

[0060]

[0061]3. Experimental method

[0062]3.1 Application materials and fixation

[0063]Dead rats at the broken head intercept L4-6Section of the spine, choose L5 DRG is rinsed in a pre-cooled saline, and it is immediately invested in 4% polyfethaldehyde to secure overnight.

[0064]3.2 Dehydration and transparency

[0065]The tissue was placed in 75%, 85%, 95%, 100%, 100% of the dehydration. The dehydrated tissue was placed in two pure xylenes to be transparent.

[0066]3.3 Diffility and embedding

[0067]The tissue placed in xylene was placed in an oven at a 40 ° C for 40 min, then placed in two new paraffin, 0.5 h each time. Pour the dissolved paraffin into the first prepared container, quickly clip the tis...

Embodiment 3

[0081]This example is used to illustrate the CDN1163 inhibition of the present invention.4-6 The use of DRG neuronal excitability in the preparation of mitigation or treatment of neuropathic pain drugs.

[0082]Experimental drugs and consumables

[0083]

[0084]

[0085]2. Experimental equipment and equipment

[0086]

[0087]3. Experimental solution formulation (reagents were purchased from Sigma, USA)

[0088]3.1 Action potential AP cell fluid

[0089]The formulation is 140 mm KCl, 0.5 mM EGTA, 3mm Mg-ATP, 5MM HEPES, using KOH to adjust pH to 7.4. That is, 521.85 mg KCl, 9.51 mg EGTA, 76.08 mg mg-ATP, 59.58 mg HEPES were added to 40 ml, using KOH to adjust pH to 7.3-7.4, to 50 mL, 0.22 μm filter filtration, 4 ° C Preservation .

[0090]3.2 Action potential AP extracellular fluid

[0091]Formula 140mm NaCl, 3mm KCl, 2mm CaCl22mm mgcl2, 10mm HEPES, PH 7.4. That is, 4090.8 mg NaCl, 111.83mg KCl, 110.98mg CaCl295.21mg MGCL21191.55 mg HEPES was added to 400 mL, and NaOH was used to adjust pH to 7.3-7.4, and the fi...

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PUM

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Abstract

The invention discloses an application of CDN1163 in preparation of a medicine for relieving or treating neuropathic pain, and the CDN1163 can act on neuropathic pain including one or more of central nervous pain and peripheral neuropathic pain, improves mechanical pain sensitivity and heat pain sensitivity caused by chronic sciatic nerve compression injury of rats, improves meuron shrinkage and astrocyte activation of lumbar intervertebral foramen 5 dorsal root ganglion, inhibits neuron excitability increase of lumbar intervertebral foramen 4-6 dorsal root ganglions, effectively relieves neuropathic pain symptoms, can remarkably reverse mechanical hyperalgesia and thermal hyperalgesia through repeated injection; no tolerance sign exists, after the medicine is stopped, the treatment effect can be maintained, and the CDN1163 is applied to preparation of medicines for relieving or treating neuropathic pain which is long in lasting time and difficult to treat.

Description

Technical field[0001]The present invention belongs to the field of neuroplastic technology, and more particularly to the application of CDN1163 in the preparation of mitigation or treatment of neuropathic pain.Background technique[0002]Neuropic pain is mostly due to machinery, viral infection, neurotoxin, inflammation, and tumor infiltration such as periphery or central nervous system damage or dysfunction caused. According to the survey, the incidence of neuropathic pain is about 7-10%, and there is a trend year by year. There will be spontaneous pain such as stinging, burning pain and hypersensitivity, and painful hypersensitivity. The work and life affecting the patient. The world's leading pharmaceutical and health care consultant Decision Resources predicted in a report in 2028, the world's 7 major markets (Mei, Japanese, Method, Germany, Italy, British and Spain) pain treatment market value is around $ 38 billion, of which 200 Billion or above for the treatment of neuropathic ...

Claims

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Application Information

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IPC IPC(8): A61K31/4706A61P25/04
CPCA61K31/4706A61P25/04
Inventor 曹征宇李少恒赵芳
Owner CHINA PHARM UNIV
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