Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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: 2013-02-13
SHANGHAI TIANCI LIFE SCI DEV CO LTD
View PDF3 Cites 0 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The present invention provides a chimeric peptide based on endomorphin 2 and neuropeptide FF, which utilizes the C-terminus of endomorphin 2 on the basis of retaining the N-terminal structure of endomorphin 2 and the C-terminal structure of neuropeptide FF A new chimeric peptide EN-9 was constructed based on the characteristics of phenylalanine residues present in the N-terminus of neuropeptide FF. Pharmacological studies in vivo have found that EN-9 exhibits stronger and more sustained analgesic activity than endomorphin 2, and has the advantages of no tolerance and low addiction. In addition, compound EN-9 subcutaneous EN-9 can cause significant analgesic effect, and can overcome the defect of no analgesic activity of endomorphin peripheral injection, so it has potential application value 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07K19/00C07K1/20C07K1/14C07K1/06C07K1/04A61K38/17A61P25/04
CPCY02P20/55
Inventor 王锐方泉李宁韩政岚
Owner SHANGHAI TIANCI LIFE SCI DEV CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com