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Application of endogenic marihuana peptide agonist (m) VD-Hp alpha in preparing analgesics

An agonist, endogenous technology, applied in the field of biochemistry

Active Publication Date: 2013-06-12
SHANGHAI TIANCI LIFE SCI DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004]The most important function of cannabis in the nervous system is analgesia (CNS Neurol Disord Drug Targets. 2009, 8: 403), but research results have found that the currently used Cannabis-based pain relievers limit widespread use due to their side effects
For example, when cannabis is used to treat pain, it is easy to produce analgesic tolerance. In addition, it is also prone to side effects such as decreased movement, ataxia and limb stiffness, constipation and addiction (Pharmacol. Rev. 2006, 58: 389)

Method used

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  • Application of endogenic marihuana peptide agonist (m) VD-Hp alpha in preparing analgesics
  • Application of endogenic marihuana peptide agonist (m) VD-Hp alpha in preparing analgesics
  • Application of endogenic marihuana peptide agonist (m) VD-Hp alpha in preparing analgesics

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Embodiment 1, the synthesis of cannabinoid peptide agonist (m) VD-Hpα

[0065] I material

[0066] Instrument: High performance liquid chromatography (HPLC) is Delta 600 from Waters; analytical column: DELTA PAK 5μC18 300?? 3.9×150mm; preparative column: DELTA PAK 15μC18 300??7.8×300mm. The mass spectrometer was PE Biosystems, Mariner System 5074. Manual solid-phase peptide synthesizer, designed by our laboratory and made by a glassworker (for the design principle of the synthesizer, please refer to page 14 of "Fmoc solid phase peptide synthesis" edited by Chen WC and White PD Figure 4 , and some improvements were made on the basis of it, that is, the method of blowing nitrogen gas was replaced by mechanical stirring, so as to achieve the purpose of fully mixing the reaction solution). Reagent: The resin is Fmoc-His(Trt)-Wang-Resin (1% DVB, 200 ~ 400 mesh, substitution value S = 0.57 mmol / g resin), purchased from Tianjin Nankai Hecheng Company. N - α-Fmoc protected ...

Embodiment 2

[0079] Example 2. Preparation of cannabinoid agonist (m)VD-Hpα injection preparation.

[0080] Dissolve 30mg of sterile (m)VD-Hpα freeze-dried powder in cillin bottles in 5ml of sterile physiological isotonic saline. After fully dissolving, it becomes a colorless, transparent and clear aqueous solution. Use it directly according to the amount required for the experiment. Or use after further diluting with isotonic saline.

Embodiment 3

[0081] Embodiment three, the preparation of freeze-dried powder preparation

[0082] Under aseptic conditions, 100 mg of high-purity (m)VD-Hpα freeze-dried powder was operated according to the powder injection preparation process procedure, and divided into 10 vials, stoppered, capped and sealed to obtain the present invention. (m)VD-Hpα powder preparation for injection.

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Abstract

The invention discloses application of endogenic marihuana peptide agonist (m) VD-Hp alpha in preparing analgesics, which means that an injection preparation or lyophilized powder preparation is prepared from the endogenic marihuana peptide agonist (m) VD-Hp alpha serving as an active ingredient and auxiliary materials according to a conventional process of pharmaceutics. A series of in-vivo activity detections indicate that marihuana endogenous peptide ligand (m) VD-Hp alpha has strong central analgesia activity, and has an advantage of low central side effect, which means that the marihuana endogenous peptide ligand (m) VD-Hp alpha seldom has the side effects of constipation and hypokinesia in an effective analgesic dose range, has a small influence on body temperature, and is slow in the analgesic tolerance process. Therefore, the endogenic marihuana peptide agonist (m) VD-Hp alpha has a good application prospect in preparing high-efficiency low-side-effect analgesics.

Description

technical field [0001] The invention belongs to the technical field of biochemistry, and relates to the application of an endogenous cannabinoid agonist (m) VD-Hpα in the preparation of analgesic drugs with high efficiency and low side effects. Background technique [0002] The management of chronic and severe pain has always been an urgent medical problem to be solved. A variety of agents are currently used to treat a variety of pathological conditions, including opioids, NSAIDs, anticonvulsants, antidepressants, ketamine, and others (Drugs 2007, 2121: 2133). However, the side effects of these drugs limit their clinical dosage and reduce their therapeutic effect. In addition to further research on the pathological mechanism of chronic pain and the identification of the analgesic mechanism of the drug itself, what is more clinically needed is a new drug for the treatment of chronic pain that is effective, non-toxic and has no central side effects. [0003] Cannabis has a ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61P29/02
Inventor 王锐方泉韩政岚王子龙李宁李旭辉
Owner SHANGHAI TIANCI LIFE SCI DEV CO LTD
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