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Small-molecular antagonist for A3 adenosine receptor

A technology of adenosine receptors and antagonists, applied in the field of small molecule antagonists

Active Publication Date: 2018-05-11
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Adenosine A 3 Receptor antagonists can block myocardial preconditioning, and APNEA(A 1 / A 3 Selective) can prevent ischemia, but R-PIA (A 1 optional) has no such effect

Method used

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  • Small-molecular antagonist for A3 adenosine receptor
  • Small-molecular antagonist for A3 adenosine receptor
  • Small-molecular antagonist for A3 adenosine receptor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0019] In order to enable those skilled in the art to better understand the technical solutions of the present invention, the following examples further illustrate the present invention.

[0020] 1. Materials and consumables

[0021]

[0022] 2. Experimental steps

[0023] 2.1 Culture cells

[0024] 2.1.1 At 37°C, 5% CO 2 Culturing stable cells expressing human adenosine receptors under high concentration conditions

[0025] 2.1.2 Prepare the buffer for the experiment

[0026] Reagent

volume

Final concentration

Hank’s Balanced Salt Solution

14ml

-

HEPES buffer (1M)

75μl

5mM

7.5% BSA stabilizer (pH 7.4)

200μl

0.1％

20mM Rolipram

7.5μl

10μM

[0027] 2.1.3 Use ethylenediaminetetraacetic acid solution to separate cells, collect 200g cells and centrifuge for 5min at room temperature, then use assay buffer to suspend the cells, and then Countess (Invitrogen#C10281) to calculate the density and activity of the cells. Only cells with cell viability greater than 85% are used for e...

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Abstract

The invention discloses a small-molecular antagonist for an A3 adenosine receptor, and an application thereof in medicine synthesis, and concretely relates to a use of the small-molecular antagonist for the A3 adenosine receptor and pharmacologically available salts of the small-molecular antagonist for the A3 adenosine receptor as medicines for treating or preventing A3 adenosine receptor-mediated related diseases or symptoms.

Description

Technical field [0001] Description of the invention A 3 Small molecule antagonists of adenosine receptors and their applications in drug synthesis. Background technique [0002] Adenosine is the precursor and metabolite of adenine nucleotides. Many physiological effects of adenosine are mediated by its receptor. Adenosine and four types of G protein coupled receptor A 1 , A 2A , A 2B And A 3 Interaction, and then regulate the activity of adenylate cyclase, ion channels and phospholipase. In the study of cardiovascular disease and kidney disease, it is found that adenosine has a regulatory effect on the potassium channels of cardiomyocytes and renal basement membrane cells. At the same time, adenosine receptor agonists and antagonists are useful for the treatment of central nervous system neurodegenerative diseases. (Such as Parkinson's disease and Alzheimer's disease, etc.) research also shows good prospects. Activate A 3 Adenosine receptors have the effects of protecting the he...

Claims

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Application Information

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IPC IPC(8): C07D231/12A61K31/415A61P9/10A61P19/02A61P29/00A61P25/28A61P11/06A61P3/10A61P27/06
CPCC07D231/12
Inventor 林建平魏宇赵骁勇
Owner NANKAI UNIV
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