Synthesis, biodistribution, and primate imaging of fluorine-18 labeled 2β-carbo-1'-fluoro-2-propoxy-3β-(4-chlorophenyl) tropanes. Ligands for the imaging of dopamine …

…, JM Hoffman, RAE BaKay, T Subramanian…

Index: Xing, Dongxia; Chen, Ping; Keil, Robert; Kilts, Clinton D.; Shi, Bing; Camp, Vernon M.; Malveaux, Gene; Ely, Timothy; Owens, Michael J.; Votaw, John; Davis, Margaret; Hoffman, John M.; BaKay, Roy A. E.; Subramanian, Thygarajan; Watts, Ray L.; Goodman, Mark M. Journal of Medicinal Chemistry, 2000 , vol. 43, # 4 p. 639 - 648

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Citation Number: 36

Abstract

2β-(R)-Carbo-1-fluoro-2-propoxy-3β-(4-chlorophenyl) tropane ((R)-FIPCT, R-6) and 2β-(S)- carbo-1-fluoro-2-propoxy-3β-(4-chlorophenyl) tropane ((S)-FIPCT, S-6) were prepared and evaluated in vitro and in vivo for dopamine transporter (DAT) selectivity and specificity. High specific activity [18F](R)-FIPCT and [18F](S)-FIPCT were synthesized in 5% radiochemical yield (decay-corrected to end of bombardment (EOB)) by preparation of the precursors 2β- ...