2Beta-carbomethoxy-3beta-(4- and 2-[18F]fluoromethylphenyl)tropanes: specific probes for in vivo quantification of central dopamine transporter sites.
Dopamine reuptake transporter binding kinetics of 2beta-carbomethoxy-3beta-(4-[18F]fluoromethylphenyl)tropane (p-FWIN) and 2beta-carbomethoxy-3beta-(2-[18F]fluoromethylphenyl)tropane (o-FWIN) were determined in vervet monkeys using positron emission tomography (PET). Ligand localization was rapid and specific to the striatum with kinetic estimates comparable with those of 11C-labeled WIN 35,428 (CWIN). Binding was more specific with p-FWIN than with CWIN or o-FWIN. The relatively longer half-life of the 18F radiolabel enabled longer acquisition times with p-FWIN, resulting in less variability in the kinetic estimates.
Stout
D
D
Department of Molecular and Medical Pharmacology, UCLA School of Medicine, Los Angeles, California 90095-6948, USA.
Petric
A
A
Satyamurthy
N
N
Nguyen
Q
Q
Huang
S C
SC
Namavari
M
M
Barrio
J R
JR
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging; D001923:Brain Chemistry; D002352:Carrier Proteins / Q000378:metabolism*; D002522:Chlorocebus aethiops; D003042:Cocaine / Q000031:analogs & derivatives / Q000493:pharmacokinetics; D050483:Dopamine Plasma Membrane Transport Proteins; D018765:Dopamine Uptake Inhibitors / Q000493:pharmacokinetics; D007091:Image Processing, Computer-Assisted; D008024:Ligands; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D009638:Norepinephrine / Q000378:metabolism; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D011954:Receptors, Dopamine / Q000378:metabolism*; D012701:Serotonin / Q000378:metabolism; D014055:Tomography, Emission-Computed; D014326:Tropanes / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology
C406246:2-carbomethoxy-3-(2-fluoromethylphenyl)tropane; C406245:2-carbomethoxy-3-(4-fluoromethylphenyl)tropane; D002352:Carrier Proteins; D050483:Dopamine Plasma Membrane Transport Proteins; D018765:Dopamine Uptake Inhibitors; D008024:Ligands; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D019275:Radiopharmaceuticals; D011954:Receptors, Dopamine; D014326:Tropanes; D012701:Serotonin; C021279:(1R-(exo,exo))-3-(4-fluorophenyl)-8-methyl-8- azabicyclo(3.2.1)octane-2-carboxylic acid, methyl ester; D003042:Cocaine; D009638:Norepinephrine