Chimeric peptide based on endomorphins 2 and neuropeptides FF, and synthesis and application thereof

A technology of endomorphin and neuropeptide, applied in the field of biochemistry, to achieve the effect of reducing side effects such as opioid tolerance and addiction

Active Publication Date: 2011-10-05
SHANGHAI TIANCI LIFE SCI DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, while neuropeptides exert their main activity, they are often accompanied by secondary activities, and these secondary activities become its side effects

Method used

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  • Chimeric peptide based on endomorphins 2 and neuropeptides FF, and synthesis and application thereof
  • Chimeric peptide based on endomorphins 2 and neuropeptides FF, and synthesis and application thereof
  • Chimeric peptide based on endomorphins 2 and neuropeptides FF, and synthesis and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0063] The synthesis method of the chimeric peptide of the present invention will be further illustrated by specific examples below.

[0064] I material

[0065] 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, and the mechanical stirring method was replaced by the nitrogen blowing method, so as to achieve the purpose of fully mixing the reaction solution). Reagent: The resin is Rink-Amide-MBHA-Resin (1% DVB, 200 ~ 400mesh, substitution value S = 0.40 mmol / g resin), purchased from Tianji...

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Abstract

The invention provides chimeric peptide based on endomorphins 2 and neuropeptides FF, wherein the chimeric peptide is the novel chimeric peptide EN-9 which is constructed by using the characteristic that both a C end of the endomorphins 2 and an N end of the neuropeptides FF have phenylalanine residues, on the basis of reserving an N end structure of the endomorphins 2 and a C end structure of the neuropeptides FF. Through in-vivo pharmacological study, it is found that the EN-9 shows stronger and more persistent analgesic activity than the endomorphins 2, and has the advantages of no enduring action, low addiction and the like. In addition, hypodermic compound EN-9 can play obvious analgesic action, can overcome the defect that the endomorphins have no analgesic activity through injecting in peripheral regions, therefore the chimeric peptide has a potential using value of being used for clinical pain treatment.

Description

technical field [0001] The invention belongs to the field of biochemical technology, and relates to a chimeric peptide constructed based on endomorphin 2 and neuropeptide FF and a synthesis method thereof; the invention also relates to the application of the chimeric peptide in preparing analgesic drugs. Background technique [0002] In clinical practice, morphine-like opioids have been widely used in the treatment and relief of various pains. However, opioid analgesics can cause serious adverse reactions and opioid dependence, which greatly limits their use in clinical treatment. Applications. Existing studies have shown that opioid receptors exist widely in both the central and peripheral areas of mammals. In 1997, the discovery of endomorphins (endomorphins, EMs), that is, endomorphin 1 (EM-1, Tyr-Pro-Trp-Phe-NH 2 ) and 2 (EM-2, Tyr-Pro-Phe-Phe-NH 2 ) are highly efficient and selective endogenous agonists of μ opioid receptors (MOR), and their K i 360 pM and 690 pM, r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K1/20C07K1/14A61P25/04C07K1/04A61K38/17C07K19/00C07K1/06
CPCY02P20/55
Inventor 王锐方泉李宁韩政岚
Owner SHANGHAI TIANCI LIFE SCI DEV CO LTD
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