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Application of TRPV1 channel targeting micromolecule

A technology of small molecules and channels, which is applied in the application field of TRPV1 channel targeting small molecules, can solve the problems of thermoregulation and maintenance function interference, etc., and achieve the effects of reducing the risk of side effects, significant analgesic effect, and rapid analgesic effect Effect

Active Publication Date: 2021-07-20
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Other TRPV1 channel-targeting small molecule compounds in the prior art also have side effects of interfering with animal body temperature regulation and maintenance functions while exerting an analgesic effect

Method used

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  • Application of TRPV1 channel targeting micromolecule
  • Application of TRPV1 channel targeting micromolecule
  • Application of TRPV1 channel targeting micromolecule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: The delayed effect of small molecule PSFL426 on the activation of TRPV1 channel by capsaicin

[0025] 1. Experimental materials:

[0026] Plasmid: pFROG-TRPV1;

[0027] Cell line: HEK293 (human embryonic kidney cells);

[0028] Transfection reagents: Common chemical reagents required for calcium transfection reagents were purchased from Sigma-Aldrich.

[0029] 2. Experimental equipment:

[0030] Electrode puller and polisher were from Narishige; patch clamp digital-to-analog converter Digidata1440A, amplifier Axon 200B, membrane current recording software pCLAMP10.6 and analysis software Clampfit10.6 were purchased from Axon; inverted microscope IX51 and fluorescent light source U-RFL- Both T were purchased from Olympus; Microcontroller MC1000e was purchased from Siskiyou.

[0031] 3. Experimental reagents:

[0032] (1) Capsaicin;

[0033] (2) small molecule PSFL426;

[0034] (3) extracellular fluid:

[0035]

[0036] Adjust the pH to 7.4 with tris...

Embodiment 2

[0046] Example 2: Alleviating effect of small molecule PSFL426 on capsaicin-induced pain

[0047] 1. Experimental animals: C57BL / 6 male mice.

[0048]The mice were kept in a ventilated experimental cage with a body weight of 20±2g. Breeding temperature is about 23°C; normal day and night alternation; all experimental animals drink water and eat freely; purchased experimental animals are raised in this laboratory for 3 to 5 days to adapt to the experimental environment; all animal experiments are carried out between 8:00 and 18:00.

[0049] 2. Experimental equipment:

[0050] Electronic balance, cage ventilation system, microinjectors and polyethylene laboratory cages.

[0051] 3. Experimental reagents:

[0052] Capsaicin, small molecule PSFL426, DMSO, Tween 80 and sodium chloride injection.

[0053] 4. Experimental method:

[0054] Before the start of the experiment, the mice were put into the experimental polyethylene cage to familiarize themselves with the environment f...

Embodiment 3

[0057] Example 3: Effects of small molecule PSFL426 on the maintenance and regulation of body temperature in mice

[0058] 1. Experimental animals: C57BL / 6 male mice.

[0059] The mice were kept in a ventilated experimental cage with a body weight of 20±2g. Breeding temperature is about 23°C; normal day and night alternation; all experimental animals drink water and eat freely; purchased experimental animals are raised in this laboratory for 3 to 5 days to adapt to the experimental environment; all animal experiments are carried out between 8:00 and 18:00.

[0060] 2. Experimental equipment:

[0061] Electronic balance, cage ventilation system, micro injector and thermocouple thermometer body temperature measuring instrument.

[0062] 3. Experimental reagents:

[0063] Small molecule PSFL426, AMG9810, DMSO, Tween 80 and sodium chloride injection. Among them, AMG9810 is a TRPV1 channel-targeted small molecule, which has also shown excellent analgesic effects in animal exper...

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Abstract

The invention discloses application of a targeting small molecule capable of acting on a classical pain receptor TRPV1 channel in preparation of a medicine for preventing and / or treating pain. The small molecule has a delay effect on opening of a TRPV1 channel caused by capsaicin, the pain feeling of a mouse is remarkably relieved on the premise of not interfering the body temperature maintenance and body temperature regulation functions of the mouse, the analgesic effect is rapid, remarkable and lasting, and a new development strategy is provided for a TRPV1 channel targeted analgesic drug.

Description

technical field [0001] The present invention relates to the application of TRPV1 channel targeting small molecules, in particular to the application of said small molecules in the preparation of pain prevention and / or treatment drugs. Background technique [0002] Transient receptor potential vanilloidcation channel 1 (TRPV1) is a kind of non-selective cation channel receptor protein expressed on cell membrane or organelle membrane. In mammals, such channel receptor proteins are widely expressed in the peripheral sensory nervous system and central brain nuclei, and are also expressed in some non-neuronal tissues and organs. TRPV1 can respond to a variety of internal and external stimuli and open, causing the flow of cations inside and outside the cell. It participates in the physiological processes of mammals such as nociception, heat perception, taste perception, mechanical perception and osmotic pressure perception. At the same time, it is involved in some normal physiolog...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/53A61K31/165A61P29/00
CPCA61K31/53A61K31/165A61P29/00
Inventor 于烨孙萌阳雷运涛
Owner CHINA PHARM UNIV
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