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Medical application of optical isomer of amine compound for treating pain

An amine compound and compound technology, which can be applied to the optical isomers of amine compounds to prepare medicines for preventing and/or treating pain, and can solve problems such as adverse reactions of central sedation, cardiotoxicity, dependence and addiction. , to achieve excellent analgesic effect, low toxicity effect

Inactive Publication Date: 2016-04-20
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Opioid analgesics have strong analgesic effects, but long-term use can easily lead to tolerance, dependence, and addiction, and have adverse reactions such as respiratory depression and central sedation. They are currently used for acute sharp pain and severe cancer pain.
Non-steroidal anti-inflammatory drugs only exert a moderate degree of analgesic effect and are suitable for mild and moderate chronic dull pain, but are ineffective for sharp pain caused by direct stimulation of sensory extremities. In addition, they also have adverse reactions such as gastrointestinal bleeding and cardiotoxicity

Method used

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  • Medical application of optical isomer of amine compound for treating pain
  • Medical application of optical isomer of amine compound for treating pain
  • Medical application of optical isomer of amine compound for treating pain

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Embodiment 1. Mouse acetic acid writhing method evaluates the analgesic effect of amoxetine

[0052] 1. Experimental animals:

[0053] KM mouse, male, SPF grade, 22-25g,

[0054] The animals were purchased from the Experimental Animal Center of the Academy of Military Medical Sciences and bred in the Experimental Animal Center of the Academy of Military Medical Sciences.

[0055] 2. Test sample:

[0056] Amoxetine, the structural formula is Prepared according to the method of Example 5 in the patent CN102850335A;

[0057] Duloxetine hydrochloride (Zhejiang Haixiang Pharmaceutical Co., Ltd.).

[0058] 3. Experimental method:

[0059] 30 minutes after the mice were orally administered the test drug amoxetine or the positive drug duloxetine, each mouse was intraperitoneally injected with 2% acetic acid aqueous solution 0.1ml / 10g, and the writhing of each mouse was observed and recorded within 5-20 minutes The number of times, that is, the body twisting or elongatin...

Embodiment 2

[0065] Embodiment 2. Mouse formalin method evaluates the analgesic effect of amoxetine

[0066] 1. Experimental animals:

[0067] KM mouse, male, SPF grade, 22-25g,

[0068] The animals were purchased from the Experimental Animal Center of the Academy of Military Medical Sciences and bred in the Experimental Animal Center of the Academy of Military Medical Sciences.

[0069] 2. Test sample:

[0070] Amoxetine, prepared according to the method of Example 5 in the patent CN102850335A;

[0071] Duloxetine hydrochloride (Zhejiang Haixiang Pharmaceutical Co., Ltd.).

[0072] 3. Experimental method:

[0073] 30 minutes after the mice were orally administered the test drug amoxetine or the positive drug duloxetine, each mouse was subcutaneously injected with 5% formalin aqueous solution 0.02ml on the right paw of each mouse, and observed and recorded for 0-5 minutes respectively (acute phase) The times of licking the feet of each mouse in the two time periods of 10-25 minutes ...

Embodiment 3

[0079] Embodiment 3. Rat sciatic nerve branch selective injury (SNI) model evaluates the effect of amoxetine Analgesic effect

[0080] 1. Experimental animals:

[0081] SD rat, male, SPF grade, 180-220g,

[0082] The animals were purchased from the Experimental Animal Center of the Academy of Military Medical Sciences and bred in the Experimental Animal Center of the Academy of Military Medical Sciences.

[0083] 2. Test sample:

[0084] Amoxetine, prepared according to the method of Example 5 in the patent CN102850335A;

[0085] Duloxetine hydrochloride (Zhejiang Haixiang Pharmaceutical Co., Ltd.).

[0086] 3. Experimental method:

[0087] Rats were anesthetized by intraperitoneal injection of pentobarbital sodium (50mg / kg), and the rats were fixed on the operating table in a lateral position. After disinfection with iodine, the skin on the upper edge of the mouse's right hind limb was cut, the muscles were separated, and the trunk of the sciatic nerve was exposed. a...

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Abstract

The invention relates to a medical application of an optical isomer of an amine compound and particularly relates to an application of the amine compound represented as the formula I or a pharmaceutically acceptable salt thereof in prevention and / or treatment on pain. A test proves that the amine compound represented as the formula I or the pharmaceutically acceptable salt thereof has excellent analgesic effect. The invention provides a novel effective medicine for the prevention and / or treatment on pain.

Description

technical field [0001] The present invention relates to the medical use of amine compounds, in particular to the use of optical isomers of amine compounds for preparing medicines for preventing and / or treating pain. Background technique [0002] Pain is a painful sensation resulting from actual or potential tissue damage, often accompanied by unpleasant emotions or cardiovascular and respiratory changes. It is not only a protective response of the body, but also a common symptom of many clinical diseases. [0003] Depending on the duration, pain can be divided into acute pain and chronic pain. Acute pain is mostly nociceptive pain caused by tissue trauma, while chronic pain is mainly neuropathic pain. Pain has a high clinical incidence and brings great suffering to patients. In addition, pain has a high comorbidity ratio with depression and other mental diseases, and most patients with depression are also accompanied by chronic pain. [0004] Traditional analgesic drugs m...

Claims

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Application Information

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IPC IPC(8): A61K31/381A61P29/00A61P25/04A61P25/06
Inventor 仲伯华张有志薛瑞董华进何新华樊士勇李云峰黄世杰袁莉
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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