Radiosynthesis of [18F] N-(3-Fluoropropyl)-2-beta-Carbomethoxy-3-beta-(4-Bromophenyl) Nortropane and the regional brain uptake in non human primate using PET.
A synthetic procedure for the preparation of [18F]FPCBT, an imaging agent for the dopamine transporter (DAT), has been developed. The radiosynthesis was carried out in a two step procedure. Even though the yield was low, we were able to prepare 20 to 30 mCi of the product, which was enough for two or three studies. The radiochemical purity was greater than 96%. The in vivo properties of this radiotracer were evaluated using baboon and it showed highest uptake in the striatum. The studies also revealed that the maximum uptake was reached within 7 to 10 minutes post injection. Plasma metabolite analysis indicated that there is only one metabolite and it is less lipophilic than the parent compound. [18F]FPCBT displayed good brain uptake and its high target to non target ratio indicate that it is a potential candidate for DAT imaging.
Chaly
Thomas
T
Department of Medicine, North Shore University Hospital, NYU Medical College, PET Research, Manhasset, NY 11030, USA. tchaly@nshs.edu
Baldwin
R M
RM
Neumeyer
John L
JL
Hellman
Matthew J
MJ
Dhawan
Vijay
V
Garg
Pradeep K
PK
Tamagnan
Gilles
G
Staley
Julie K
JK
Al-Tikriti
Mohammed S
MS
Hou
Yankun
Y
Zoghbi
Sami S
SS
Gu
Xiao Hui
XH
Zong
R
R
Eidelberg
David
D
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D050483:Dopamine Plasma Membrane Transport Proteins; D005260:Female; D007553:Isotope Labeling / Q000379:methods; D008562:Membrane Glycoproteins / Q000378:metabolism*; D026901:Membrane Transport Proteins / Q000378:metabolism*; D008657:Metabolic Clearance Rate; D009419:Nerve Tissue Proteins / Q000378:metabolism*; D009662:Nortropanes / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D010215:Papio; D019275:Radiopharmaceuticals / Q000097:blood / Q000138:chemical synthesis / Q000493:pharmacokinetics; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed / Q000379:methods
D050483:Dopamine Plasma Membrane Transport Proteins; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; C490461:N-(3-fluoropropyl)-2-carbomethoxy-3-(4-bromophenyl)nortropane; D009419:Nerve Tissue Proteins; D009662:Nortropanes; D019275:Radiopharmaceuticals