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Compound for preventing and treating pain and application thereof

A technology of compound and composition, applied in the field of pain treatment and prevention, can solve problems such as unsatisfactory treatment effect, and achieve good analgesic effect

Pending Publication Date: 2022-05-06
EAST CHINA NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pregabalin is a drug for neuropathic pain and herpes zoster. However, the treatment effect is not satisfactory, and only half of the patients who take the drug achieve partial relief

Method used

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  • Compound for preventing and treating pain and application thereof
  • Compound for preventing and treating pain and application thereof
  • Compound for preventing and treating pain and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] Whole-cell electrophysiological assays

[0088] The cDNA of human TREK-1 was subcloned into pEGFP-N1 expression vector. The constructed plasmid was transfected into CHO-K1 cells with Lipofectamine 3000. The cell culture medium used in the experiments was DMEM / F12 containing 10% FBS and 1% penicillin-streptomycin. Culture conditions were constant temperature at 37°C, 5% CO 2 gas environment.

[0089] Cells cultured 16-36 hours after transfection can be used for electrophysiological experiments. The detection adopts Whole-CellRecording whole-cell patch clamp recording mode. The experiments used a HEKA EPC10 amplifier, a Sutter Instrument MP-225 micromanipulator, a Nikon fluorescence microscope, and a Bio-Logic RSC-200 drug delivery system. The glass electrode is pulled by SutterInstrument P-97 electrode puller, and the resistance of the liquid is 3-7MΩ. TREK-1 intracellular fluid components include: 140mM KCl, 2mM MgCl 2 , 10mM EGTA, 1mM CaCl 2 , 10mM HEPES, and a...

Embodiment 2

[0093] Animal pharmacology and drug efficacy experiment

[0094] The test drug used in this embodiment includes:

[0095] YET01 was synthesized by conventional methods, and pregabalin was commercially available.

[0096] In the embodiment of YET01, two doses are set, which are 20mg / kg and 50mg / kg respectively. The way of administration is oral gavage, 10ml / kg.

[0097] Compound Dissolution:

[0098] YET01 was dissolved according to the following steps: (1) 20% injection volume of DMSO was completely dissolved; (2) 20% injection volume polyethylene glycol 400 was added and mixed evenly; (3) 60% injection volume was diluted with sterile normal saline to the final volume. According to the sequence of operations, mediate for 30 seconds in each step, and then ultrasound for 1 minute, and configure it for use on the same day.

[0099] Solvent control group: DMSO: polyethylene glycol 400: normal saline = 1:1:2

[0100] Positive control drug:

[0101] Pregabalin: The solvent is...

Embodiment 21

[0106] Embodiment 2.1 mouse thermal stimulation tail flick experiment (tail immersion)

[0107] In the mouse tail flick experiment, the mouse tail was immersed in 52°C water, and the mouse raised its tail because it felt the pain caused by the noxious heat stimulus, and the pain tolerance of the mouse was judged by timing the tail-raising time latency. Such as Figure 4 As shown, the results of this experiment show that YET01 can effectively relieve the pain caused by noxious heat stimulation in mice.

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PUM

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Abstract

The invention discloses a TREK-1 potassium channel agonist and an application of the TREK-1 potassium channel agonist in analgesic treatment. Specifically, the invention discloses a compound capable of activating a TREK-1 potassium ion channel, and the compound has a remarkable analgesic effect and can be used for preparing pharmaceutical compositions and preparations for preventing and / or treating chronic pain (muscle and soft tissue pain, bone joint pain, headache, visceral pain and pathological neuralgia), acute pain and cancer pain.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a compound for preventing and treating pain and its application. Background technique [0002] Pain makes patients suffer for a long time, and even produce malignant emotional reactions such as anxiety and depression. Currently, clinical medications for pain treatment are mainly opioid analgesics, non-steroidal anti-inflammatory drugs, anticonvulsants, and depressants. Opioids have good analgesic effects, but these drugs have toxic side effects such as addiction and respiratory depression, which bring great harm. Non-steroidal anti-inflammatory drugs are weak and poor in efficacy, and have strong gastrointestinal and cardiovascular side effects. Pregabalin is a drug for the treatment of neuropathic pain and herpes zoster. However, the treatment effect is not satisfactory, and only half of the patients who take the drug get partial relief. Therefore, the developme...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61P29/00A61P25/04A61P21/00A61P35/00A61P19/02A61P35/02
CPCA61K31/519A61P29/00A61P25/04A61P21/00A61P35/00A61P19/02A61P35/02
Inventor 阳怀宇任娟傅杰张洋刘诗洁莫奕青张乾森
Owner EAST CHINA NORMAL UNIV
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