Radiosynthesis of [11C]Lu 29-024: a potential radiotracer for 5HT2 receptors PET studies.
For mapping 5-HT2 receptors in the central nervous system with positron emission tomography (PET), 2,5-dimethyl-3-(4-fluorophenyl)-1-(1-[11C]methyl-4-piperidinyl)-1H-indol e ([11C]Lu29-024) has been prepared. The precursor for the radiosynthesis of [11C]Lu29-024 was obtained in an overall yield of 53% by a convenient five-step synthesis; its reaction with [11C]methyl iodide afforded [11C]Lu29-024 in 35-50% radiochemical yield (decay corrected) in 45 to 50 min with a specific radioactivity ranging from 11 to 15 GBq/micromol. Following i.v. injections into rats, the analysis of plasma samples showed that the metabolism of [11C]Lu29-024 was rapid and extensive (60% of the original tracer was metabolized at 40 min). In contrast, only unmetabolized [11C]Lu29-024 could be detected in brain tissue. These biological results suggest that labeled metabolites have no access to brain tissue and further propose [11C]Lu29-024 as an interesting tool for PET studies of brain 5HT2 receptors.
Amokhtari
M
M
CEA-DSV/DRM-GDM-TEP, Universite de Caen, France.
Andersen
K
K
Ibazizene
M
M
Dhilly
M
M
Dauphin
F
F
Barre
L
L
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism; D002250:Carbon Radioisotopes / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D006847:Hydrocarbons, Iodinated / Q000737:chemistry; D007211:Indoles / Q000097:blood / Q000138:chemical synthesis*; D007553:Isotope Labeling; D008297:Male; D010880:Piperidines / Q000097:blood / Q000138:chemical synthesis*; D019275:Radiopharmaceuticals / Q000097:blood / Q000138:chemical synthesis*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011985:Receptors, Serotonin / Q000032:analysis*; D014055:Tomography, Emission-Computed
D002250:Carbon Radioisotopes; D006847:Hydrocarbons, Iodinated; D007211:Indoles; C115517:Lu29-024; D010880:Piperidines; D019275:Radiopharmaceuticals; D011985:Receptors, Serotonin; C014055:methyl iodide