Cocaine receptor binding ligands

Abstract

A class of binding ligands for cocaine receptors and other receptors in the brain. Specifically, a novel family of compounds shows high binding specificity and activity, and, in a radiolabeled form, can be used to bind to these receptors, for biochemical assays and imaging techniques. Such imaging is useful for determining effective doses of new drug candidates in human populations. In addition, the high specificity, slow onset and long duration of the action of these compounds at the receptors makes them particularly well suited for therapeutic uses, for example as substitute medication for psychostimulant abuse. Some of these compounds may be useful in treating Parkinson's Disease or depression, by virtue of their inhibitory properties at monoamine transporters.

1 - 42 . (canceled) 
     
     
         43 . A method of inhibiting the action of a psychostimulant, inhibiting neurotransmitter re-uptake, treating neurodegenerative disorders, treating depression, treating anorexia, treating cocaine addiction, treating nicotine addiction, treating alcohol addiction, treating bipolar disorder, treating eating disorders, treating obesity, treating attention deficit disorder, treating panic attacks, treating panic disorders, treating obsessive-compulsive disorder and/or sexual dysfunction, comprising administering to a patient in need of such treatment an effective amount of a 2β,3β-cis substituted compound having the formula: 
       
         
           
           
               
               
           
         
         or a salt thereof. 
       
     
     
         44 . The method of  claim 43 , which comprises inhibiting the action of a psychostimulant. 
     
     
         45 . The method of  claim 45 , wherein the psychostimulant is cocaine, nicotine, alcohol or amphetamine. 
     
     
         46 . The method of  claim 43 , wherein the compound is in the form an HCl salt. 
     
     
         47 . The method of  claim 43 , which comprises inhibiting neurotransmitter re-uptake. 
     
     
         48 . The method of  claim 47 , wherein the neurotransmitter is dopamine, norepinephrine, serotonin or another monomaine. 
     
     
         49 . The method of  claim 47 , wherein the compound is in the form an HCl salt. 
     
     
         50 . The method of  claim 43 , which comprises treating neurodegenerative disorders. 
     
     
         51 . The method of  claim 50 , wherein the neurodegenerative disorder is Parkinson's disease. 
     
     
         52 . The method of  claim 50 , wherein the compound is in the form an HCl salt. 
     
     
         53 . The method of  claim 43 , which comprises treating depression. 
     
     
         54 . The method of  claim 53 , wherein the compound is in the form an HCl salt. 
     
     
         55 . The method of  claim 43 , which comprises treating anorexia. 
     
     
         56 . The method of  claim 55 , wherein the compound is in the form an HCl salt. 
     
     
         57 . The method of  claim 43 , which comprises treating cocaine addiction. 
     
     
         58 . The method of  claim 57 , wherein the compound is in the form an HCl salt. 
     
     
         59 . The method of  claim 43 , which comprises treating alcohol addiction. 
     
     
         60 . The method of  claim 59 , wherein the compound is in the form an HCl salt. 
     
     
         61 . The method of  claim 43 , which comprises treating bipolar disorder. 
     
     
         62 . The method of  claim 61 , wherein the compound is in the form an HCl salt. 
     
     
         63 . The method of  claim 43 , which comprises treating eating disorders. 
     
     
         64 . The method of  claim 63 , wherein the compound is in the form an HCl salt. 
     
     
         65 . The method of  claim 43 , which comprises treating obesity. 
     
     
         66 . The method of  claim 65 , wherein the compound is in the form an HCl salt. 
     
     
         67 . The method of  claim 43 , which comprises treating attention deficit disorder. 
     
     
         68 . The method of  claim 67 , wherein the compound is in the form an HCl salt. 
     
     
         69 . The method of  claim 43 , which comprises treating panic attacks. 
     
     
         70 . The method of  claim 69 , wherein the compound is in the form an HCl salt. 
     
     
         71 . The method of  claim 43 , which comprises treating panic disorders. 
     
     
         72 . The method of  claim 71 , wherein the compound is in the form an HCl salt. 
     
     
         73 . The method of  claim 43 , which comprises treating obsessive-compulsive disorder. 
     
     
         74 . The method of  claim 73 , wherein the compound is in the form an HCl salt. 
     
     
         75 . The method of  claim 43 , which comprises treating sexual dysfunction. 
     
     
         76 . The method of  claim 75 , wherein the compound is in the form an HCl salt.