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GLP-1 acceptor agonists used for treating pains

A GLP-1, receptor agonist technology, applied in the direction of anti-inflammatory agents, non-central analgesics, medical preparations containing active ingredients, etc., can solve the problem of inability to produce analgesic effect, reduce glucagon secretion, The molecular mechanism is not clear, etc.

Inactive Publication Date: 2012-08-01
王永祥
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

4) Reduce glucagon secretion, the specific molecular mechanism is still unclear
The third study on the influence of GLP-1 receptors and pain comes from Dr. Matwyshyn of Midwestern University at the AAPS Annual Meeting and Exposition meeting in 2009 and the subsequent meeting report at the 2010 World Pharmacology Congress (WorldPharm2010), but he reported The conclusion is that continuous intraperitoneal injection of GLP-1 receptor agonist exendin-4 cannot produce analgesic effect, and has no effect on morphine analgesic effect and tolerance (Matwyshyn et al., AAPS-002278, 2009)

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  • GLP-1 acceptor agonists used for treating pains
  • GLP-1 acceptor agonists used for treating pains
  • GLP-1 acceptor agonists used for treating pains

Examples

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Embodiment Embodiment 1

[0066] The present invention will be further illustrated by the following examples, which should not be interpreted as limiting the protection scope of the present invention in any way. The entire contents of all cited references in this application, including article references, issued patents, published patent applications, and co-pending patent applications, are expressly incorporated herein by reference. In the following examples, unless otherwise specified, the reagents and materials used are commercially available at least analytically pure or equivalent products. EXAMPLES Example 1 Expression of rat spinal cord GLP-1 receptor (GLP-1 receptor) mRNA

[0067] Male Wistar rats (Shanghai Slack Experimental Animal Co., Ltd.) were anesthetized with sodium pentobarbital (60 mg / kg) (Sigma, Shanghai, China), exposed their chest cavity, and perfused the heart with normal saline until the blood flowed out of the whole body. Afterwards, rat pancreas, skeletal muscle, ganglion, spin...

Embodiment 2

[0068] GLP-1 receptor gene expression According to 100 mg of tissue, 1 ml of Trizol reagent (Invitrogen, Shanghai, China) was added, and a corresponding volume of Trizol reagent was added. The quality of the extracted RNA was determined according to OD260 / OD280 and nucleic acid electrophoresis. Using reverse transcriptase (Toyobo, Toyobo (Shanghai) Biotechnology Co., Ltd.), according to the manufacturer's instructions, 1 μg of total RNA was reverse-transcribed into cDNA under the corresponding reverse transcription conditions. Using the cDNA produced by reverse transcription as a template and GAPDH as an internal reference, the expression of the target gene GLP-1 receptor in various parts of the rat was detected by fluorescent quantitative PCR (Mastercycler ep realplex real-time PCR system, Eppendorf, Hamburg, Germany). -ΔΔCt method to analyze the expression changes of the target gene GLP-1 receptor. The experimental results of 3 rats are as follows: figure 1 As shown, the p...

Embodiment 4

[0071] Behavioral observations showed that administration of GLP-1 receptor agonists such as GLP-1(7-36), exenatide, geniposide, geniposide, and genipin had no obvious behavioral changes such as sedation, shaking, paralysis, and irritation , increased activity, indicating that the analgesic effect of GLP-1 receptor agonists on pain is not due to its non-specific sedative effect or impairment of motor coordination. Example 4 Inhibitory effect of spinal cord injection of GLP-1 receptor peptide agonist exenatide on bone cancer pain model and neurogenic pain model in rats

[0072] Female Sprague Dawley rats (150-180g, Shanghai Slack Experimental Animal Co., Ltd.) were anesthetized with sodium pentobarbital (50mg / kg, i.p.), drilled a hole 0.5cm below the tibial head, and injected 5μl rat Walker 256 cell suspension (1×10 7 cells / ml, Cell Resource Center, Shanghai Institute of Biological Sciences, Chinese Academy of Sciences) into the bone marrow cavity. On the 14th day after the o...

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Abstract

The invention relates to glucagon-like peptide-1 (GLP-1) acceptor agonists (comprising: macromolecular agonists, such as GLP-1 and derivatives thereof, and exendins and derivatives thereof; and micromolecular agonists, such as geniposides) used for treating diseases, such as pains, especially chronic pains, comprising neuropathic pains, cancer pains, diabetic pains, immune inflammation pains, pains in back and loin, and the like which can be treated through activating a central nervous system comprising a spinal cord GLP-1 acceptor.

Description

technical field [0001] The present invention relates to the stimulating effect of glucagon-like peptide-1 (glucogan-like peptide-1, GLP-1) receptor agonist on the GLP-1 receptor in the nervous system, in particular for the treatment of pain, especially Chronic pain; also relates to methods of using the GLP-1 receptor to identify agents. Background technique [0002] Pain is one of the most common clinical symptoms. Many diseases or diseases will cause pain symptoms and seriously affect the quality of life of patients. Pain treatment has become one of the most considered factors in health care and disease treatment. Therefore, pain has received more and more attention from the medical field, and 2000-2010 has been called the era of pain. Pain is an unpleasant sensory and emotional experience associated with acute or potential tissue damage that prompts people to avoid or said destructive situation in order to protect the body and avoid further damage. Most pain disappears s...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K45/06A61K38/26A61K38/22A61K31/7048G01N33/68A61P25/04A61P25/06A61P29/00
CPCA61K38/22A61K38/26A61P1/18A61P25/04A61P25/06A61P29/00
Inventor 王永祥龚念
Owner 王永祥
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