Supercharge Your Innovation With Domain-Expert AI Agents!

C end modification endomorphin 2

An endomorphin and structural feature technology, applied in the field of physiological activity research, can solve the problems of difficult to break through the blood-brain barrier, unfavorable for oral administration and injection, etc., and achieve the effects of low cost, high yield and reduced workload

Inactive Publication Date: 2008-03-12
LANZHOU UNIVERSITY
View PDF1 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Third, it is not easy to break through the blood-brain barrier (Brainblood barrier, BBB), which is not conducive to oral administration and injection

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
  • C end modification endomorphin 2
  • C end modification endomorphin 2
  • C end modification endomorphin 2

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0036] Example of Synthesis: Synthesis of Compound 1e (Tyr-Pro-Trp-D-Ala-NH-Bn)

[0037] Reaction i: Synthesis of benzyloxycarbonyl-tyrosine-proline (c): Compound a 0.946g (3mmol), Hosu 0.346g (3.3mmol) were dissolved in anhydrous tetrahydrofuran (THF), stirred in ice bath for 10 minutes 0.619 g (3.6 mmol) of DCC were added afterwards. After reacting in ice bath for 30 minutes, remove the ice bath, react at room temperature for 3 to 5 hours, filter with Buchner funnel, remove the DCU (cyclodihexyl urea) generated by the reaction to obtain the activated ester THF solution of compound a. 0.414g (3.6mmol) of compound b was dissolved in equimolar sodium hydroxide aqueous solution, and the pH value was adjusted to 9-10. After stirring in an ice bath for 10 minutes, THF solution of the activated ester of compound a was added. After reacting in an ice bath for 30 minutes, remove the ice bath, and react overnight at room temperature. Drain THF, dissolve in ethyl acetate, wash with 5...

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 novel analogue of Endomorphin1(Endomorphin1, EM1) and endomorphin 2 (Endomorphin2, EM2)with the structure formula of (I) and (II) as well as the preparation method for the analogues. And through isolated biological activity identification: GPI(Mu receptor affinity identification) , the MVD (Delta receptor affinity identification) test and SAP, HR experiments used in the biological activity identification to demonstrate that C- terminal modified EM1 and EM2 analogues have strong receptor binding ability and good analgesic effect. The analogues overcome the side effects of morphine in terms of slow cardiac. The present invention provides vary board prospects for morphine substitutes in deep-seated pain adjustment.

Description

[0001] The present invention is a divisional application of "C-terminal modified endomorphin 1, endomorphin 2", the original filing date is September 30, 2004; application number: 200410073159.2. Technical field: [0002] The present invention relates to a class of new compounds, specifically a class of new analogues of endomorphin 1 (Endomorphin 1, EM1) and endomorphin 2 (Endomorphin 2, EM2), and the preparation method and physiological activity research of these compounds. Background technique: [0003] Opioid receptors are mainly divided into three types: μ, δ, κ, which are distributed in the central nervous system and various peripheral organs of mammals, and the corresponding endogenous ligands are endomorphins [see Zadina, J.E.; Hackler, L. .; Ge, L.J.; Kastin, A.J.A potent and selective endogenous agonist for the μ-opiatereceptor. Nature. 1997, 386(6624): 499-502] (Endomorphins, EMs), enkephalin (Enkephalin) [see Hughes, J ., Smith, T.W., Kosterlitz, H.W., Forthergill...

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 Applications(China)
IPC IPC(8): C07K5/107C07K7/06C07K14/665
Inventor 王锐于烨刘红美
Owner LANZHOU UNIVERSITY
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com