Details

Autor(en) / Beteiligte

• Gao, Yongjun
• Ravert, Hayden T
• Valentine, Heather
• Scheffel, Ursula
• Finley, Paige
• Wong, Dean F
• Dannals, Robert F
• Horti, Andrew G

Titel

5-(5-(6-[(11)C]methyl-3,6-diazabicyclo[3.2.0]heptan-3-yl)pyridin-2-yl)-1H-indole as a potential PET radioligand for imaging cerebral α7-nAChR in mice

Ist Teil von

• Bioorganic & medicinal chemistry, 2012-06, Vol.20 (12), p.3698-3702

Ort / Verlag

England

Erscheinungsjahr

2012

Quelle

MEDLINE

Beschreibungen/Notizen

• The radiosynthesis and in vivo evaluation of 5-(5-(6-[(11)C]methyl-3,6-diazabicyclo[3.2.0]heptan-3-yl)pyridin-2-yl)-1H-indole [(11)C]rac-(1), a potential PET tracer for α7 nicotinic acetylcholine receptors (α7-nAChR), are described. Syntheses of the nonradioactive standard rac-1 and corresponding desmethyl precursor 7 were achieved in several reaction steps. Radiomethylation of 7 with [(11)C]CH(3)I afforded [(11)C]rac-1 in an average radiochemical yield of 30 ± 5% (n=5) with high radiochemical purity and an average specific radioactivity of 444 ± 74 GBq/μmol (n=5). The total synthesis time was 30 min from end-of-bombardment. Biodistribution studies in mice showed that [(11)C]rac-1 penetrates the blood-brain barrier and specifically labels neuronal α7-nAChRs.