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Synthesis and Biodistribution of (R,S)-[O-Methyl-11C]-1-[3-(5-Methoxy-1,2,3,4-tetrahydro-1-naphtalenyl)propyl]-4-Phenylpiperazine (PNU-157760), A Putative Radioligand for 5-HT1AReceptors

✍ Scribed by Mario Matarrese; Dmitrij V. Soloviev; Rosa M. Moresco; Valentino Ferri; Pasquale Simonelli; Fulvio Magni; Diego Colombo; Sergio Todde; Assunta Carpinelli; Ferruccio Fazio; Marzia Galli Kienle

Publisher
Elsevier Science
Year
1998
Tongue
English
Weight
195 KB
Volume
26
Category
Article
ISSN
0045-2068

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✦ Synopsis

Racemic 1- [3-(5-methoxy-1,2,3,4-tetrahydro-1-naphtalenyl)propyl]-4-phenylpiperazine (PNU-157760) was labeled with carbon-11 (t 1/2 ϭ 20.4 min) as a putative radioligand for the noninvasive assessment of 5-HT 1A receptors in vivo with positron emission tomography (PET). The radiochemical synthesis consisted of O-methylation of desmethyl precursor with [ 11 C]methyl iodide in the presence of potassium tert-butoxide in DMF. The desmethyl precursor for the radiosynthesis of [ 11 C]PNU-157760, was prepared by a convenient one-step demethylation of PNU-157760 with boron tribromide. (R,S)-[O-Methyl-11 C]-1-[3-(5-methoxy-1,2,3,4-tetrahydro-1-naphtalenyl)propyl]-4-phenylpiperazine with Ͼ99% radiochemical purity was obtained in 30 min with a radiochemical yield of 10 Ϯ 5% (EOS, nondecay corrected) and a specific radioactivity of 2.5 Ϯ 1 Ci/Ȑmol. Biodistribution studies in rats showed that [ 11 C]PNU-157760 readily crosses the blood-brain barrier with a maximum of brain uptake at 30 min after injection; however, the low specific-to-nonspecific binding ratio in vivo as evidenced by the low hippocampus/cerebellum uptake ratio (1.17 at 60 min postinjection) does not make [ 11 C]PNU-157760 a promising radioligand for serotonin 5-HT 1A receptors.

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