Substance for curing or relieving pain

A compound, aminobutyric acid technology, applied in the biological field, can solve problems such as lack of in-depth research and increased expression

Active Publication Date: 2013-08-14
SHANGHAI SIMR BIOTECHNOLOGY CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Found to contain α5-GABA A The receptor is mainly expressed in small neurons, and its expression is elevated in the neurotomy model (Xiao HS et al., Identification of gene expression profile of dorsal root ganglion in the rat peripheral axotomy model of neuropathic pain.”Proc Natl Acad Sci U S A.2002Jun 11;99(12):8360-5.), but whether it is closely related to injury or pain has not been deeply studied in this field

Method used

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  • Substance for curing or relieving pain
  • Substance for curing or relieving pain
  • Substance for curing or relieving pain

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preparation example Construction

[0173] Methods for the preparation of the compounds of the invention are known to those skilled in the art. For example, literature (Chambers MS et al., An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABA A alpha5receptors with cognition enhancing properties.J Med Chem.2004 Nov18;47(24):5829-32.) and patent US6355638 (Pyrazolo[1,5-d][1,2,4]triazines for enhancing cognition) disclosed MRK The chemical synthesis method of -016. Literature (Jones P et al., Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5 -ylmethoxy)pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA A alpha5 inverse agonist for cognitive dysfunction. Bioorg Med Chem Lett. 2006 Feb 15;16(4):872-5.) discloses the chemical synthesis method of MRK016-M3. Literature (Sternfeld F et al., Selective, orally active gamma-aminobutyric acid A α5receptor inverse agonists as cognition enhancers. J Me...

Embodiment 1

[0224] Embodiment 1, GABA A Expression of the α5 subunit of the receptor is elevated under SNI model conditions

[0225] In the SNI model, GABA was measured by immunohistochemistry and western blotting A The expression of the α5 subunit protein of the receptor, the results are as follows figure 1 shown.

[0226] Immunohistochemical experiments show that the SNI model can induce GABA A The receptor's α5 subunit protein expression was increased. In immunohistochemical experiments, 14 days after SNI model preparation, GABA A The α5 subunit protein expression of the receptor increased, and the control was the dorsal root ganglion slice (normal) of normal rats, such as figure 1 As shown in A. The results show: GABA A The α5 subunit of the receptor has elevated cellular expression in dorsal root ganglia and, more interestingly, in small cells, GABA A The fluorescence signal intensity of receptor α5 subunit protein increased significantly.

[0227] Western blot experiments s...

Embodiment 2

[0228] Embodiment 2, GABA A The expression of α5 subunit protein of the receptor is increased in the model of inflammatory pain

[0229] GABA was measured by immunohistochemistry and western blotting in a CFA-induced inflammatory pain model A The expression of the α5 subunit protein of the receptor, the results are as follows figure 2 shown.

[0230] Immunohistochemical experiments showed that CFA-induced inflammatory pain model can promote GABA in dorsal root ganglia 2 days after CFA injection A Increased expression of receptor α5 subunit protein, as in figure 2 As shown in A.

[0231] In immunohistochemical experiments, GABA was found A The expression of receptor α5 subunit protein was increased in minicells in dorsal root ganglia. Statistics show GABA A The expression ratio of receptor α5 subunit in dorsal root ganglia was increased. Western blot experiments showed that GABA A The protein content of the receptor α5 subunit was significantly increased in the infla...

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Abstract

The invention relates to a substance for curing or relieving pain, and provides application of a gamma-aminobutyric acid A receptor inverse agonist containing alpha 5 subunits in preparing a drug for preventing and improving or curing the pain and also provides a drug composition containing the substance for curing or relieving the pain.

Description

technical field [0001] The invention belongs to the field of biotechnology; more specifically, the invention relates to substances for treating or relieving pain. Background technique [0002] Pain is a sensory expression distinct from touch, pressure, heat, or cold. Patients often describe pain in terms such as sharp, dull, aching, stabbing, cutting, or burning. Pain caused by nociceptive nerves and manifested as hyperalgesia is generally called "neurogenic" pain; pain caused by stimulation of nociceptors is called "nociceptive" pain. [0003] Clinically speaking, pain can be divided into two categories: acute pain and chronic pain. Acute pain results from injury to the skin, body structure, or internal organs and / or from noxious stimuli produced by disease, or from abnormal function of muscles or internal organs that do not produce actual tissue damage; whereas chronic pain can be defined as persisting beyond the usual course of acute disease Chronic pain is considered ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/53A61K31/5025A61K31/5517G01N33/15G01N33/53A61P25/04A61P29/02
CPCA61K31/5025A61K31/50A61K31/551G01N33/9426G01N2800/2842A61K31/53A61K31/5517G01N2500/02A61P25/02A61P25/04A61P29/00A61P29/02G01N33/566G01N2500/10
Inventor 张旭李帅鲍岚叶阳姚胜
Owner SHANGHAI SIMR BIOTECHNOLOGY CO LTD
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