Serotonergic agents with long-acting in vivo effects

Abstract

Compounds of the formula have a long duration of action and are useful for the treatment of chronic diseases resulting from the dysfunction of the serotonergic 5-HT 1A system, such as schizophrenia and other psychotic disorders such as paranoia and mano-depressive illness.

1 . A method of testing the effects of long term 5-HT 1A  receptor occupancy in a population of cells comprising contacting said cells with a labeled compound of Formula I  
       
         
           
           
               
               
           
         
       
       wherein 
 R 1 ═H or lower alkyl of 1-4 carbon atoms,  
 R 2 ═H or lower alkyl or 1-4 carbon atoms;  
 R 3  is I and p is 0 or 1, and pharmaceutical salts thereof.  
 
     
     
         2 . The method of  claim 1  wherein the compound of Formula I is radiolabelled.  
     
     
         3 . The method of  claim 1  wherein the label is  2 H,  3 H,  11 C,  13 C,  14 C,  125 I, or  131 I.  
     
     
         4 . The method of  claim 1  wherein the label is  3 H.  
     
     
         5 . The method of  claim 1  wherein the label is  11 C.  
     
     
         6 . The method of  claim 1  wherein the label is  14 C.  
     
     
         7 . The method of  claim 1  wherein the cells are in vivo.  
     
     
         8 . The method of  claim 1  wherein the cells are in vitro.