Structure–activity relationship of trihexyphenidyl analogs with respect to the dopamine transporter in the on going search for a cocaine inhibitor

…, P Abraham, S Kitayama, TA Kopajtic, A Gamliel…

Index: Dar; Thiruvazhi; Abraham; Kitayama; Kopajtic; Gamliel; Slusher; Carroll; Uhl European Journal of Medicinal Chemistry, 2005 , vol. 40, # 10 p. 1013 - 1021

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Citation Number: 9

Abstract

A series of trihexyphenidyl (THP) analogs were used to search for a derivative that could serve as a cocaine inhibitor. A compound that blocks binding of the cocaine analog carboxyfluorotropane (CFT), allows dopamine uptake and exhibits low side effects could serve as a good candidate for that purpose. All analogs were tested for the extent to which they inhibit CFT binding, dopamine uptake and n-methyl scopolamine (NMS) binding. ...