Adenosine receptor activation reagent and the uses of thereof

Abstract

The present invention relates to application of N(6)-(2-hydroxyethyl)-adenosine (HEA) and its derivatives as an adenosine A 1 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.

1 . An adenosine receptor agonist, wherein the agonist includes N(6)-(2-hydroxyethyl) adenosine (HEA) or its derivatives. 
     
     
         2 . The agonist according to  claim 1 , wherein said adenosine receptor is one or more of A 1 , A 2A , A 2B , A 3 . 
     
     
         3 . The agonist according to  claim 1 , wherein the adenosine receptor is A 1  receptor. 
     
     
         4 . The agonist according to  claim 1 , wherein the HEA has a structure as follow: 
       
         
           
           
               
               
           
         
       
     
     
         5 . The agonist according to  claim 1 , wherein said derivative of the HEA has the following general formula (1) 
       
         
           
           
               
               
           
         
       
       wherein R1 is a branched or linear alkyl group. 
     
     
         6 . The agonist according to  claim 5 , wherein R1 is C(CH 3 ) 2 CH 2 OH, CH(CH 3 )CH 2 OH or C(CH 3 ) 3 . 
     
     
         7 . A method for treating or preventing convulsion, pain, insomnia, apoplexia, Parkinson's disease or opioid drug addiction, renal failure or renal ischemia reperfusion injury comprising using HEA or its derivatives. 
     
     
         8 . The method according to  claim 7 , wherein the HEA and its derivatives have the following general structural formula: 
       
         
           
           
               
               
           
         
       
       wherein R1 is a branched or linear alkyl group. 
     
     
         9 . The method according to  claim 7 , wherein R1 is C(CH 3 ) 2 CH 2 OH, CH(CH 3 )CH 2 OH or C(CH 3 ) 3 . 
     
     
         10 . The method according to  claim 7 , wherein said HEA is selected from the group consisting of  Cordyceps, Cordyceps militaris, Paecilomyces cicadae  fungus and culture extract of the fungus. 
     
     
         11 . The method according to  claim 7 , wherein said HEA is selected from the group consisting of  Cordyceps cicadae, Cordyceps militaris, Cordyceps sinensis  and extract of its artificial culture. 
     
     
         12 . The method according to  claim 7 , wherein said HEA treats or prevents convulsion, pain, insomnia, apoplexia, Parkinson's disease, or opioid drug addiction via the adenosine receptor. 
     
     
         13 . The method according to  claim 12 , wherein said adenosine receptor is the A 1  receptor.