Protective agent for retinal neuronal cell containing prostaglandin f2alpha derivative as active ingredient

Abstract

An object of the present invention is to find a new pharmaceutical application of a prostaglandin F2α derivative. It was found that the prostaglandin F2α derivative inhibits glutamate-induced retinal neuronal cell death in a concentration-dependent manner in rat fetal retinal neuronal cells, in other words, the prostaglandin F2α derivative acts directly on the retinal neuronal cells and exhibits a protective effect. Accordingly, the prostaglandin F2α derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage.

1 . A protective agent for a retinal neuronal cell comprising a prostaglandin F2α derivative as an active ingredient. 
   
   
       2 . The protective agent for a retinal neuronal cell according to  claim 1 , wherein the prostaglandin F2α derivative is a fluorine-containing prostaglandin F2α derivative. 
   
   
       3 . The protective agent for a retinal neuronal cell according to  claim 2 , wherein the fluorine-containing prostaglandin F2α derivative is a 15,15-difluoroprostaglandin F2α derivative. 
   
   
       4 . The protective agent for a retinal neuronal cell according to  claim 3 , wherein the 15,15-difluoroprostaglandin F2α derivative is a compound represented by the following general formula (I) or a salt thereof: 
     
       
         
         
             
             
         
       
     
     wherein R represents a hydroxyalkyl group, a formyl group, a carboxy group, an alkoxycarbonyl group, an aryloxycarbonyl group, an aminocarbonyl group, an alkylaminocarbonyl group or an arylaminocarbonyl group, and when R is an aryloxycarbonyl group or an arylaminocarbonyl group, the aryl moiety thereof may have a substituent. 
   
   
       5 . The protective agent for a retinal neuronal cell according to  claim 4 , wherein in the general formula (I), R represents a carboxy group or a salt group thereof or an alkoxycarbonyl group. 
   
   
       6 . The protective agent for a retinal neuronal cell according to  claim 2 , wherein the fluorine-containing prostaglandin F2α derivative is a 15-monofluoroprostaglandin F2α derivative. 
   
   
       7 . The protective agent for a retinal neuronal cell according to  claim 1 , wherein the retinal neuronal cell is a photoreceptor cell, a bipolar cell, an optic ganglion cell, a horizontal cell or an amacrine cell. 
   
   
       8 . The protective agent for a retinal neuronal cell according to  claim 1 , which is used for the prevention or treatment of an eye disease. 
   
   
       9 . A method of protecting a retinal neuronal cell comprising administering an effective amount of a prostaglandin F2α derivative to a patient. 
   
   
       10 . The protection method according to  claim 9 , wherein the prostaglandin F2α derivative is a fluorine-containing prostaglandin F2α derivative. 
   
   
       11 . The protection method according to  claim 10 , wherein the fluorine-containing prostaglandin F2α derivative is a 15,15-difluoroprostaglandin F2α derivative. 
   
   
       12 . The protection method according to  claim 11 , wherein the 15,15-difluoroprostaglandin F2α derivative is a compound represented by the following general formula (I) or a salt thereof: 
     
       
         
         
             
             
         
       
     
     wherein R represents a hydroxyalkyl group, a formyl group, a carboxy group, an alkoxycarbonyl group, an aryloxycarbonyl group, an aminocarbonyl group, an alkylaminocarbonyl group or an arylaminocarbonyl group, and when R is an aryloxycarbonyl group or an arylaminocarbonyl group, the aryl moiety thereof may have a substituent. 
   
   
       13 . The protection method according to  claim 12 , wherein in the general formula (I), R represents a carboxy group or a salt group thereof or an alkoxycarbonyl group. 
   
   
       14 . The protection method according to  claim 10 , wherein the fluorine-containing prostaglandin F2α derivative is a 15-monofluoroprostaglandin F2α derivative. 
   
   
       15 . The protection method according to  claim 13 , wherein the retinal neuronal cell is a photoreceptor cell, a bipolar cell, an optic ganglion cell, a horizontal cell or an amacrine cell. 
   
   
       16 . A method of preventing or treating an eye disease associated with retinal neuronal cell damage comprising administering a therapeutically effective amount of a prostaglandin F2α derivative to a patient. 
   
   
       17 . The prevention or treatment method according to  claim 16 , wherein the prostaglandin F2α derivative is a fluorine-containing prostaglandin F2α derivative. 
   
   
       18 . The prevention or treatment method according to  claim 17 , wherein the fluorine-containing prostaglandin F2α derivative is a 15,15-difluoroprostaglandin F2α derivative. 
   
   
       19 . The prevention or treatment method according to  claim 18 , wherein the 15,15-difluoroprostaglandin F2α derivative is a compound represented by the following general formula (I) or a salt thereof: 
     
       
         
         
             
             
         
       
     
     wherein R represents a hydroxyalkyl group, a formyl group, a carboxy group, an alkoxycarbonyl group, an aryloxycarbonyl group, an aminocarbonyl group, an alkylaminocarbonyl group or an arylaminocarbonyl group, and when R is an aryloxycarbonyl group or an arylaminocarbonyl group, the aryl moiety thereof may have a substituent. 
   
   
       20 . The prevention or treatment method according to  claim 19 , wherein in the general formula (I), R represents a carboxy group or a salt group thereof or an alkoxycarbonyl group. 
   
   
       21 . The prevention or treatment method according to  claim 17 , wherein the fluorine-containing prostaglandin F2α derivative is a 15-monofluoroprostaglandin F2α derivative. 
   
   
       22 . The prevention or treatment method according to  claim 16 , wherein the retinal neuronal cell is a photoreceptor cell, a bipolar cell, an optic ganglion cell, a horizontal cell or an amacrine cell. 
   
   
       23 - 30 . (canceled)