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New kappa-opiate receptor stimulant having protection function on ischemia heart

An opioid receptor stimulant and cardiac technology, applied in cardiovascular system diseases, drug combination, organic chemistry, etc., can solve problems such as low water solubility, small molecular weight, and limited clinical application

Inactive Publication Date: 2013-03-27
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Previous experimental studies also found that due to the low water solubility and small molecular weight of U50488H, it can pass through the blood-brain barrier after entering the blood circulation. Therefore, while improving ischemic myocardium, it may cause addiction and dependence in the body, thus severely limiting its use. Clinical application

Method used

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  • New kappa-opiate receptor stimulant having protection function on ischemia heart
  • New kappa-opiate receptor stimulant having protection function on ischemia heart
  • New kappa-opiate receptor stimulant having protection function on ischemia heart

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Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0051] 1. The quaternization modification of U50488H:

[0052] (1) Preparation of U50488 free base

[0053]

[0054] Take U50488H powder, gradually add distilled water until completely dissolved, add saturated Na 2 CO 3 When the pH of the solution was 10, it was extracted with ethyl acetate and detected as a pure product by thin layer chromatography (Thin Layer Chromatography, TLC) (developing solvent: ethyl acetate:methanol=5:2), and then dried with anhydrous magnesium sulfate, The solvent was removed under reduced pressure to obtain a pale yellow oil which was U50488 free base with a yield of 97.3%.

[0055] (2) preparation of methyl iodide quaternary ammonium salt

[0056]

[0057] in N 2 Under protection, put U50488 in a three-necked bottle, add freshly distilled CH 3 I (molecular weight: 142, density: 2.28g / ml), reflux (42°C), after about 5 hours, the raw material almost disappeared by TLC detection, stop the reaction, evaporate CH 3 1, the crude product (pale...

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Abstract

The invention discloses a new kappa-opiate receptor stimulant (quaternized U50488H) having protection function on ischemia heart. Quaternized U50488H is produced by reaction of kappa-opiate receptor stimulant U50488H and CH3I under the conditions of a polar solvent and a catalyst. Like U50488H, the quaternized product can obviously improve the function of ischemia / reperfused heart, obviously reduce the area of myocardial infarction, reduce leakage of myocardial enzyme and obviously reduce apoptosis number of myocardial cells. The new compound has the remarkable characteristic of avoiding passing blood brain barrier, thereby avoiding addiction and dependence caused by the situation that U50488H enters the brain tissue via blood circulation. The new kappa-opiate receptor stimulant having protection function on ischemia heart can be used for academic research and can also provide a possible new drug for clinical application to prevent and treat ischemic heart disease, thereby having good scientific research value and clinical application prospect.

Description

technical field [0001] The invention relates to the fields of basic research and clinical research of treating ischemic heart diseases with new opioids without dependence. Background technique [0002] Ischemic heart disease is the number one enemy threatening human health in today's world. With the wide application of intracoronary thrombolysis and coronary artery bypass grafting and other medical and surgical treatments, cardiologists pay more and more attention to the subsequent cardiomyocyte reperfusion injury. [0003] Studies have shown that κ-opioid receptors exist widely in the body (such as the mouth, heart, brain and other tissues and organs), and the dominant κ-opioid receptors in the heart play an important role in the process of myocardial ischemia / ischemia-reperfusion. important regulatory role. A large amount of evidence from animal experiments shows that exogenous κ-opioid receptor selective agonist U50488H can significantly reduce the number of myocardial ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/135A61P9/10
Inventor 裴建明王跃民王倩梅郭海涛樊荣张淑苗李娟冯娜
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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