| abstract |
The present invention provides a family of tropane analogs. More particularly, the present invention provides a family of 4' and 4',4''-substituted-3 alpha -(diphenylmethoxy)tropane analogs having the formula <IMAGE> (I) in which R is a functional group including, but not limited to, hydrogen, alkyl, alkoxy, arylalkyl, aryloxyalkyl, cinnamyl and acyl; and R1 and R2 are independently selected and are functional groups including, but not limited to, hydrogen, alkyl, alkoxy, hydroxy, halogen, cyano, amino and nitro. The benztropine analogs of the present invention have a high affinity for the dopamine transporter and inhibit dopamine uptake, but they do not exhibit a cocaine-like behavioral profile. Moreover, the present invention provides methods of using such benztropine analogs to treat cocaine abuse, to image dopamine transporter/cocaine binding sites, and to diagnose and/or monitor neurodegenerative disorders (e.g., Parkinson's disease). In addition, the present invention provides pharmaceutical compositions comprising a benztropine analog of the present invention and a pharmaceutically acceptable carrier or excipient. |