Radiosynthesis of [18F] N-3-fluoropropyl-2-beta-carbomethoxy-3-beta-(4-iodophenyl) nortropane and the first human study with positron emission tomography.
A procedure for the routine preparation of [18F]FP-CIT has been developed. Purification of the final product was achieved by preparative HPLC using phenethyl column without decomposition or epimerization. [18F] labeled-N-fluoropropyl-2 beta-carbomethoxy-3 beta-(4-iodophenyl) nortropane was prepared and PET imaging was performed on human subjects. A high uptake into striatal regions was observed. HPLC plasma analysis using [18F]FP-CIT indicated the presence of only one metabolite. By directly comparing the behavior of these three radiotracers ([18F]DOPA, [123I]FP-CIT, and [18F]FP-CIT) in the same subjects, we can enhance our understanding of the dopaminergic system as well as the relative potential of these techniques in a clinical research setting.
Chaly
T
T
Department of Research, North Shore University Hospital/Cornell University Medical College, Manhasset, NY 11030, USA.
Dhawan
V
V
Kazumata
K
K
Antonini
A
A
Margouleff
C
C
Dahl
J R
JR
Belakhlef
A
A
Margouleff
D
D
Yee
A
A
Wang
S
S
Tamagnan
G
G
Neumeyer
J L
JL
Eidelberg
D
D
D002851:Chromatography, High Pressure Liquid; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000302:isolation & purification; D014055:Tomography, Emission-Computed; D015899:Tomography, Emission-Computed, Single-Photon; D014326:Tropanes / Q000138:chemical synthesis* / Q000302:isolation & purification
D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D014326:Tropanes; C087552:2-carbomethoxy-8-(3-fluoropropyl)-3-(4-iodophenyl)tropane