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Chimeric peptide based on endomorphin-1 and neurotensin (8-13) and synthesis method and application thereof

A technology of neurotensin and endomorphin, applied in the field of chimeric peptides and their synthesis, can solve the problems of low analgesic activity, short analgesic duration, analgesic tolerance and gastrointestinal side effects, and achieve low Side effects, effects of high clinical application value

Active Publication Date: 2018-04-27
黑龙江省工研院资产经营管理有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The present invention aims to solve the problems of short analgesic duration of existing endomorphin-1, low analgesic activity of peripheral administration, analgesic tolerance and gastrointestinal side effects, and provides endomorphin-1 based Chimeric peptide of 1 and neurotensin (8-13) and its synthesis method and application

Method used

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  • Chimeric peptide based on endomorphin-1 and neurotensin (8-13) and synthesis method and application thereof
  • Chimeric peptide based on endomorphin-1 and neurotensin (8-13) and synthesis method and application thereof
  • Chimeric peptide based on endomorphin-1 and neurotensin (8-13) and synthesis method and application thereof

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specific Embodiment approach 1

[0038] Specific embodiment one: the amino acid sequence of the chimeric peptide based on endomorphin-1 and neurotensin (8-13) in this embodiment is as follows:

[0039] Tyr-Pro-Trp-Phe-Gly-Gly-Arg-Arg-Pro-Tyr-Ile-Leu.

[0040] This embodiment retains the biological activity of the two neuropeptide fragments, and solves the problem of the short analgesic duration of endomorphin-1, the low analgesic activity of peripheral administration, and the analgesic tolerance and gastrointestinal side effects The problem. Through various in vitro and in vivo biological experiments, the pharmacological activity of the chimeric peptide of this embodiment was identified. The results show that the chimeric peptide of this embodiment has higher affinity to μ-opioid receptors and opioid activity on isolated specimens, especially the activity on GPI specimens is higher than that of endomorphin-1. In addition, the chimeric peptide has high analgesic activity of central and peripheral administrat...

specific Embodiment approach 2

[0041] Specific embodiment two: the present embodiment is based on the synthetic method of the chimeric peptide of endomorphin-1 and neurotensin (8-13), comprises the following steps:

[0042] 1. Pretreatment of Wang resin protected by "Fmoc": check the air tightness of the solid phase synthesizer, put the Fmoc-Leu-Wang resin with one amino acid residue into the synthesizer, add dichloromethane and stir for 30-40min, After the resin is fully soaked and swollen, filter the solvent under reduced pressure; the mass ratio of the Fmoc-Leu-Wang resin with one amino acid residue to the volume ratio of dichloromethane is 1g: (7-12)mL;

[0043] 2. Remove the "Fmoc" protecting group: wash the swelled resin with DMF for 3 to 5 minutes, dry it, repeat 3 to 5 times, and then add 20% to 25% vol. Piperidine / DMF deprotection solution, stirred for 5-10 minutes, drained, repeated 2-3 times, then added piperidine / DMF deprotection solution with volume percentage concentration of 20%-25%, stirred ...

specific Embodiment approach 3

[0050] Specific embodiment three: the difference between this embodiment and specific embodiment two is: the molar weight of the amino acid protected by the "Fmoc" group in step three is 2.5-3 times the molar weight of the Fmoc-Arg(pbf)-Wang resin. Others are the same as in the second embodiment.

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Abstract

The invention a chimeric peptide based on endomorphin-1 and neurotensin (8-13) and a synthesis method and application thereof. The chimeric peptide solves the problem that the existing endomorphin-1 has short lasting time of easing pain, low pain-easing activity based on peripheral administration and analgesic tolerance and gastrointestinal side effects. The chimeric peptide has an amino acid sequence of Tyr-Pro-Trp-Phe-Gly-Gly-Arg-Arg-Pro-Tyr-Ile-Leu. The synthesis method comprises 1, Fmoc-protective Wang resin pretreatment, 2, removal of a Fmoc-protective gene, 3, amino acid condensation reaction, 4, peptide chain extension, 5, cutting of the peptide chain from resin, and 6, crude peptide desalting and purification. The chimeric peptide has long duration of easing pain and has the advantages of no pain easing tolerance and low side effects on the gastrointestinal tract. The chimeric peptide is used for preparation of polypeptide pain easing drugs.

Description

technical field [0001] The invention relates to a chimeric peptide and its synthesis method and application. Background technique [0002] The World Association for the Study of Pain (IASP) defines neuropathic pain as a pain syndrome caused by sensory pathway damage or dysfunction in the central or peripheral nervous system, characterized by spontaneous pain, hyperalgesia, hyperalgesia, or evoked pain. feature. Neuropathic pain lasts for a long time, recovers slowly, and its pain mechanism is not completely clear. There is a lack of satisfactory treatment methods in clinical practice, which seriously affects the quality of life of human beings. The study of neuropeptides in pain perception and modulation has always been a hot spot in neuroscience research. A variety of neuropeptides have been found to play an important role in the transmission and modulation of pain information, among which opioid peptides are the most familiar. [0003] Endomorphins are endogenous μ-opio...

Claims

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Application Information

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IPC IPC(8): C07K19/00C07K1/20C07K1/16C07K1/06C07K1/04A61K38/17A61P25/04
CPCY02P20/55C07K14/665A61K38/00C07K14/47C07K2319/00
Inventor 王长林袁碧玉杨代军
Owner 黑龙江省工研院资产经营管理有限公司
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