Adenosine receptor activation reagent and the uses of thereof

a technology of adenosine receptor and activation reagent, which is applied in the field of new adenosine a1 receptor agonist, can solve the problems of adenosine being hindered in the use of clinical drugs

Inactive Publication Date: 2016-01-28
ZHEJIANG SUB TROPICS CROP INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes a new compound called N(6)-(2-hydroxyethyl)-adenosine (HEA) and its derivatives, which are agonists of the adenosine A1 receptor. HEA and its derivatives have strong selectivity for the A1 receptor and can produce a variety of physiological and biochemical effects. The patent also describes the use of HEA and its derivatives in the preparation of drugs and foods for the prevention and treatment of nervous system and kidney diseases. The patent also discusses the mechanism of action of HEA and its derivatives, as well as the potential applications of this new compound.

Problems solved by technology

In the early years, Jacobson K A et al. reported that adenosine was hindered to be used as clinical drug due to its metabolic unstability.

Method used

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  • Adenosine receptor activation reagent and the uses of thereof
  • Adenosine receptor activation reagent and the uses of thereof
  • Adenosine receptor activation reagent and the uses of thereof

Examples

Experimental program
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Effect test

example 1

HEA is a Selective Agonist of A1 Receptor

[0081]Preparation of Receptor Protein

[0082]Using Wistar rat, head was cut and the brain was removed, and cerebral cortex and striatum were separated, respectively weighed, added into 10 fold volume of ice-cooled Tris-HCL buffer solution (50 mM, PH7.5) according to 1:10, the tissue is homogenized, after the suspension was centrifuged the supernatant was discarded, the above-described solution wash was repeated for 3 times, centrifuged again and the supernatant was discarded, the precipitate was again mixed in 50 mM Tris-HCL buffer solution, the protein concentration in rat cerebral cortex determined by Coomassie Brilliant Blue Method (Bradford method) was 0.8 mg / ml, the protein content in rat striatum brain tissue homogenate was 1.3 mg / ml. After subpackage stored at −80□ for subsequent use (Li M, Kang R X, Shi J Liu G T, Zhang J J, 2013. Anticonvulsant Activity of B2, an Adenosine Analog, on Chemical Convulsant-Induced Seizures, PLoS One June ...

example 2

Application of HEA in Anti-Convulsion

[0090]2.1 Animal Model and Administration Method

[0091]Male ICR mouse, 18˜22 g; purchased from Animal Experiment Center of Wenzhou Medical University. Before experiment, animals were adapted to environment for at least 5 days. Kept at 25□, food and water were freely fed. Based on the weight, the healthy male ICR mice were randomly divided into control group (1% DMSO, ip), model group, CCPA group (0.1 mg·kg−1, ip), HEA group (15 mg / kg, 40 mg / kg, 60 mg / kg), DPCPX group (2 mg·kg−1, ip), ZM241385 group (1 mg·kg−1, 5 mg·kg−1, ip), DPCPX+HEA (2 mg·kg−1+40 mg / kg, ip) group and ZM241385+HEA (1 mg·kg−1+40 mg / kg, 5 mg·kg−1+40 mg / kg ip) group. Wherein, 10 min before administration, the adenosine A1R receptor antagonist DPCPX (or A2R receptor antagonist ZM241385) were peritoneal injected, after 15 min of administration pentylenetetrazole (100 mg·kg−1, ip) was given to induce mouse convulsion; in alone antagonist group, after 5 min of the antagonist pentylenet...

example 3

Application of the HEA in Cerebral Ischemia

[0096]3.1 Preparation of Tested Sample

[0097]The dried Cordyceps cicadae was precisely weighed as raw material, and extracted by using 50% ethanol as solvent, 2 h / time, filtered, the filtrate were combined, to prepare a solution containing sample with a effective dose of 1500 mg / kg for subsequent use.

[0098]3.2 Animal Model and Administration Method

[0099]Using rat middle cerebral artery distal obstruction cerebral ischemia model. (1) according to rat weight, 10% chloral hydrate (3 ml / kg) was peritoneally injected to anaesthetize. (2) the rat lie on right side and fixed, 1 cm skin incision was cut at connection of inner canthus with external canal, fascia was isolated, muscle tissue, the skull was exposed; (3) a small amount of normal saline was sucked with cotton ball to wipe the skull to ac clear view; (4) fascia was isolated under operating microscope, and the skull was exposed, a hole with diameter of 2 mm circular was drilled at a sute ⅓ ...

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Abstract

The present invention relates to application of N(6)-(2-hydroxyethyl)-adenosine (HEA) and its derivatives as an adenosine A1 receptor agonist in preparation of drug or food, the HEA and its derivatives are used in treatment of diseases relating to adenosine receptor regulator, such as insomnia, pain, convulsion, apoplexia, Parkinson's disease, opioid drug addiction and kidney ischemia reperfusion injury etc. The present invention provides a new method for treatment of the diseases relating to nervous system and kidney.

Description

RELATED APPLICATIONS[0001]The present application claims the priority from China Patent Application No. 201410360752.9 filed on Jul. 27, 2014, and China Patent Application No. 201510226745.4, filed on May 6, 2015. The entireties of these applications including all tables, diagrams and claims are incorporated hereby as reference of the present invention.TECHNICAL FIELD[0002]The present invention relates to a new adenosine A1 receptor agonist, particularly, relates to N(6)-(2-hydroxyethyl)-adenosine (HEA) and its derivatives as adenosine A1 receptor agonist; and its new application as adenosine A1 receptor agonist in preparation of drug or food for prevention and treatment of the disease relating to adenosine receptor regulator.[0003]Incorporated by reference herein in its entirety is the Sequence Listing entitled “sequence Listing.txt”, created Jul. 7, 2015, size of 2 kilobytes.BACKGROUND OF THE INVENTION[0004]Cordyceps cicadae is a Cordyceps, in which the body is full of mycelium an...

Claims

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Application Information

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IPC IPC(8): C07H19/16
CPCC07H19/16A61P25/08A61P25/16A61P25/36C07H19/167
Inventor CHAI, YIQIUZHU, BICHUNPENG, XIUXIUJIN, YIWEI
Owner ZHEJIANG SUB TROPICS CROP INST
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