Biodistribution of [18F] SR144385 and [18F] SR147963: selective radioligands for positron emission tomographic studies of brain cannabinoid receptors.
ABSTRACT. [(18)F] SR144385 and [(18)F] SR147963 were synthesized in a multistep reaction in which fluorine-18 was introduced by nucleophilic halogen displacement on a bromo precursor. The fluorine-18-labeled intermediate was deprotected and coupled with the appropriate alkyl amine to give the final products. Both radioligands had appropriate regional brain distribution for cannabinoid receptors with a target to nontarget ratio of 1.7 for [(18)F] SR147963 and 2.5 for [(18)F] SR144385 at 60 and 90 min postinjection, respectively. The uptake of both tracers was blocked with a 1 mg/kg dose of SR141716A.
Mathews
W B
WB
Department of Radiology, Johns Hopkins University, Baltimore, Maryland 21287, USA. bmathews@petscan.nm.jhu.edu
Scheffel
U
U
Finley
P
P
Ravert
H T
HT
Frank
R A
RA
Rinaldi-Carmona
M
M
Barth
F
F
Dannals
R F
RF
D000280:Administration, Inhalation; D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D002186:Cannabinoids / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D005462:Fluorine Radioisotopes; D007553:Isotope Labeling; D008024:Ligands; D008297:Male; D051379:Mice; D009025:Morpholines / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D010880:Piperidines / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D011720:Pyrazoles / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D019275:Radiopharmaceuticals / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug / Q000378:metabolism*; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed
D002186:Cannabinoids; D005462:Fluorine Radioisotopes; D008024:Ligands; D009025:Morpholines; D010880:Piperidines; D011720:Pyrazoles; D019275:Radiopharmaceuticals; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug; C422188:SR 144385; C422189:SR 147963