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Application of cdn1163 in the preparation of drugs for alleviating or treating neuropathic pain

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

Active Publication Date: 2022-03-08
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 the preparation of drugs for alleviating or treating neuropathic pain
  • Application of cdn1163 in the preparation of drugs for alleviating or treating neuropathic pain
  • Application of cdn1163 in the preparation of drugs for alleviating or treating neuropathic pain

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] This example is used to illustrate the application of CDN1163 provided by the present invention in reducing the mechanical pain threshold and thermal pain threshold of chronic sciatic nerve compression injury (chronic constriction injury, CCI) rats in the preparation of drugs for relieving or treating neuropathic pain.

[0036] 1. Experimental animals

[0037] 50 male SD rats were purchased from the Qinglongshan Animal Breeding Farm in Jiangning District, Nanjing. Before the experiment, the rats were placed in a quiet environment avoiding strong light and raised for one week to adapt to the environment. The ratio of light to dark time was 1:1. The room temperature was controlled at 22-25° C., the humidity was 55%, and the rats could eat and drink freely.

[0038] 2. Experimental drugs and consumables

[0039]

[0040] 3. Experimental equipment and equipment

[0041]

[0042] Glass minute needle, sterile gauze, hand towel, cotton swab, micro syringe.

[0043] 4....

Embodiment 2

[0056] This embodiment is used to illustrate that CDN1163 provided by the present invention improves L 5 Application of the DRG morphology in the preparation of drugs for relieving or treating neuropathic pain.

[0057] 1. Experimental drugs and consumables

[0058]

[0059] 2. Experimental equipment and equipment

[0060]

[0061] 3. Experimental method

[0062] 3.1 Material collection and fixation

[0063] Rats were killed by decapitation, and L 4-6 Segment of spinal cord, choose L on ice 5 DRG was rinsed in pre-cooled saline, immediately put into 4% paraformaldehyde, and fixed overnight.

[0064] 3.2 Dehydration and transparency

[0065] Put the tissue into 75%, 85%, 95%, 100%, 100% ethanol for dehydration. Place the dehydrated tissue in twice pure xylene for clearing.

[0066] 3.3 Wax dipping and embedding

[0067] Put the tissues placed in xylene into a 40°C oven and bake for 40 minutes, and then add new paraffin wax twice, each time for 0.5 hours. Pour ...

Embodiment 3

[0081] This embodiment is used to illustrate that CDN1163 provided by the present invention inhibits L 4-6 Application of DRG neuron excitability in preparation of medicine for relieving or treating neuropathic pain.

[0082] 1. Experimental drugs and consumables

[0083]

[0084]

[0085] 2. Experimental equipment and equipment

[0086]

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

[0088] 3.1 Action potential AP intracellular fluid

[0089] The formula is 140mM KCl, 0.5mM EGTA, 3mM Mg-ATP, 5mM HEPES, adjust the pH to 7.4 with KOH. That is, weigh 521.85mg KCl, 9.51mg EGTA, 76.08mg Mg-ATP, 59.58mg HEPES, add sterile water to 40mL, use KOH to adjust the pH to 7.3-7.4, dilute to 50mL, filter through a 0.22μm membrane, and store at 4°C .

[0090] 3.2 Action potential AP extracellular fluid

[0091] The formula is 140mM NaCl, 3mM KCl, 2mM CaCl 2 , 2mM MgCl 2 , 10 mM HEPES, pH 7.4. Namely weigh 4090.8mg NaCl, 111.83m...

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Abstract

The invention discloses the application of CDN1163 in preparing a medicine for relieving or treating neuropathic pain. The CDN1163 can act on neuropathic pain including one or more of central neuropathic pain and peripheral neuropathic pain, and improve chronic sciatic nerve compression in rats. Mechanical pain sensitivity and thermal pain sensitivity caused by sexual injury, improve neuronal shrinkage and astrocyte activation in lumbar intervertebral foramen 5 dorsal root ganglia, inhibit neuronal excitation in lumbar intervertebral foramina 4-6 dorsal root ganglia It can effectively reduce the symptoms of neuropathic pain, and repeated injections can significantly reverse mechanical hyperalgesia and thermal hyperalgesia, and there is no sign of tolerance, and the therapeutic effect can be maintained after drug withdrawal. and difficult-to-treat neuropathic pain medications.

Description

technical field [0001] The invention belongs to the technical field of nerve drugs, and in particular relates to the application of CDN1163 in the preparation of drugs for alleviating or treating neuropathic pain. Background technique [0002] Neuropathic pain is mostly caused by peripheral or central nervous system damage or dysfunction caused by mechanical damage, viral infection, neurotoxin, inflammation and tumor infiltration. According to the survey, the incidence of neuropathic pain is about 7-10%, and it has a tendency to increase year by year. During the onset, spontaneous pain such as tingling pain and burning pain, as well as stimulus-induced pain such as hyperalgesia and hyperalgesia will occur. affect the work and life of patients. Decision Resources, the world's leading pharmaceutical and healthcare consulting company, predicted in a report that the market value of pain treatment in the world's seven major markets (the United States, Japan, France, Germany, Ita...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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