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Application of 1,2-diphenylethylene derivative in pharmacy

A technology of stilbene and derivatives, applied in 1 field, can solve problems such as loss of pain sensation, burning sensation of capsaicin, loss of response to harmful stimuli, etc., and achieve the effect of relieving pain

Inactive Publication Date: 2011-06-15
HEBEI MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, studies have shown that large doses of capsaicin can produce some adverse reactions, such as local use of capsaicin will cause burning sensation, loss of pain sensation and loss of response to various harmful stimuli after a few days to a few weeks, which may be related to the deactivation of TRPV1. sensitive phenomenon

Method used

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  • Application of 1,2-diphenylethylene derivative in pharmacy
  • Application of 1,2-diphenylethylene derivative in pharmacy
  • Application of 1,2-diphenylethylene derivative in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 The synergistic effect of DIDS on capsaicin (CAP for short) was determined by electrophysiological patch clamp.

[0031] (1) Test compound DIDS: commercially available DIDS CAS: 207233-90-7 (Sigma batch number: 068K1116)

[0032] (2) Test method: the culture of dorsal root neurons (DRG) of adult SD rats (200~250g): get the whole dorsal root ganglia of adult SD rats, digest with collagenase and trypsin, and prepare them in 10% fetal bovine serum , 100U / ml penicillin and streptomycin in DMEM culture solution blown, the cells spread on a 12mm round coverslip, cultured in a 24-well plate.

[0033] Patch clamp technique to record cell membrane current: Axon 700B was used as a patch clamp amplifier. Amphotericin B (final concentration: 0.1-0.2 mg / ml) was used in the electrode for punching patch-clamp recording. After the microelectrode is polished, fill the inner liquid of the electrode, and control the resistance value at 1.5-2.5MΩ. The electrode inner solution ...

Embodiment 2

[0035] Example 2 Electrophysiological Patch Clamp Assay (Sensitization of DIDS to Low pH Cell Solution Activated TRPV1 Channel)

[0036] (1) Test compound: DIDS

[0037] (2) test method: with the method used in embodiment 1

[0038] (3) Test results: if image 3 As shown, using the -60mV continuous recording mode to record the activation of the TRPV1 channel by repeatedly administering the extracellular fluid with pH=5, there is an obvious rapid desensitization phenomenon of the TRPV1 current. Combined application of 100 micromol DIDS on the basis of extracellular fluid at pH=5 can increase TRPV1 current and block the rapid desensitization of TRPV1 current. The combined application of DIDS and low pH cell fluid can cause the current to increase by 4.48±0.69 times (see Figure 4 ).

Embodiment 3

[0039] Example 3 Electrophysiological Patch Clamp Assay: Sensitization of SITS on Low pH Cell Solution Activation of TRPV1 Channel

[0040] The sources of the compounds described in the present invention can be obtained from commercial sources, and the specific source of the compounds described in the example of the determination of the biological activity of the compounds is DIDS CAS: 207233-90-7 (Sigma batch number: 068K1116);

[0041] (1) Test compound SITS, commercially available (SITS CAS: 51023-76-8 (Sigma batch number: 107K1065))

[0042] (2) test method: with the method used in embodiment 1

[0043] (3) Test results: The -60mV continuous recording mode was used to record the TRPV1 channel activated by the extracellular fluid at pH=5 for many times, and the TRPV1 current had obvious rapid desensitization phenomenon; the application of SITS alone could not trigger the TRPV1 current; Combined application of 100 micromolar SITS on the basis of external fluid can increase TR...

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Abstract

The invention discloses novel application of a 1,2-diphenylethylene derivative, i.e. the 1,2-diphenylethylene derivative is used as a capsaicin receptor activated synergist. The 1,2-diphenylethylene derivative in the invention and a TRPV1 (Transient Receptor Potential Vanilloid) activator have a synergistic effect. The 1,2-diphenylethylene derivative can be used as the TRVP1 activated synergist and can be applied to the preparation of a pain-easing medicine preparation.

Description

technical field [0001] The present invention relates to the application of compounds in pharmacy, in particular to the application of 1,2-stilbene derivatives in pharmacy. Background technique [0002] Capsaicin receptor (transient receptor potential vanilloid receptor subtype 1, referred to as TRPV1) is a non-selective cation channel with high permeability to calcium ions, and is selectively highly expressed in nociceptive sensory neurons[ 1]. This receptor can be activated by capsaicin, hydrogen ions (pH<5.8), high temperature (>43°C) and some endogenous ligands such as some inflammatory factors produced when inflammation occurs. This theory is considered to mediate pain One of the main molecular mechanisms [2]. The main topology of TRPV1 is similar to that of Shaker-related voltage-gated potassium channels, including intracellular N-terminal and C-terminal and six transmembrane structures, in which there is a shorter pore between the fifth and sixth transmembrane ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/26A61K31/165A61P29/02
Inventor 张海林张璇杜肖娜祁金龙
Owner HEBEI MEDICAL UNIVERSITY
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