Nonsedating Alpha-2 Agonists

Abstract

The present invention provides an α-2A/α-1A selective agonist that includes a compound represented by Structure 1 or a pharmaceutically acceptable salt, ester, amide, stereoisomer or racemic mixture thereof. The present invention further provides a pharmaceutical composition that contains a pharmaceutical carrier and a therapeutically effective amount of an α-2A/α-1A selective agonist that includes a compound represented by Structure 1 or a pharmaceutically acceptable salt, ester, amide, stereoisomer or racemic mixture thereof.

1 . An α-2A/α-1A selective agonist, comprising a compound represented by 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt, ester, amide, stereoisomer or racemic mixture thereof. 
     
     
         2 . The α-2A/α-1A selective agonist of  claim 1 , wherein said selective agonist has an α-1A efficacy less than that of brimonidine or a ratio of α-1A/α-2A potency greater than that of brimonidine. 
     
     
         3 . The α-2A/α-1A selective agonist of  claim 1 , comprising a compound represented by 
       
         
           
           
               
               
           
         
       
     
     
         4 . A pharmaceutical composition, comprising a pharmaceutical carrier and a therapeutically effective amount of an α-2A/α-1A selective agonist that comprises a compound represented by 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt, ester, amide, stereoisomer or racemic mixture thereof. 
     
     
         5 . The pharmaceutical composition of  claim 4 , said selective agonist having an α-1A efficacy less than that of brimonidine or a ratio of α-1A/α-2A potency greater than that of brimonidine. 
     
     
         6 . The pharmaceutical composition of  claim 4 , said selective agonist comprising a compound represented by