HEA Adenosine Agonist Metabolic Stability
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Solution Overview
Problem
Current A1 adenosine receptor agonists face challenges due to metabolic instability and limited selectivity, and there is a lack of effective treatments for conditions such as convulsions, Parkinson's disease, and renal diseases.
Innovation Solution
N(6)-(2-hydroxyethyl)-adenosine (HEA) and its derivatives are developed as selective A1 adenosine receptor agonists, offering strong selectivity and neuroprotective and renal protective functions, which can be used in drug or food form to treat various diseases by activating the A1 receptor.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing A1 adenosine receptor agonists are used, then neuroprotective and renal protective functions are achieved, but metabolic instability and limited selectivity occur
Solution Approach 1:
The patent modifies the chemical structure of adenosine by replacing the N6-hydrogen with a 2-hydroxyethyl group, creating HEA. This structural parameter change results in a compound that maintains A1 receptor agonist activity while improving metabolic stability and selectivity compared to existing agonists like adenosine and its derivatives
2Reliability
If selective A1 receptor agonists are developed, then treatment efficacy for convulsions, Parkinson's disease and renal diseases is improved, but drug development complexity increases
Solution Approach 1:
The patent identifies and utilizes HEA as an intermediary compound that bridges the gap between adenosine and its metabolites. HEA serves as a stable intermediate that maintains therapeutic activity while avoiding the metabolic instability of parent compounds, thereby simplifying the development of effective treatments for neurological and renal conditions
Data Source
AI summary
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.