5-(5-(6-[¹¹C]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
2012
Gao, Yongjun | Ravert, Hayden T. | Valentine, Heather | Scheffel, Ursula | Finley, Paige | Wong, Dean F. | Dannals, Robert F. | Horti, Andrew G.
The radiosynthesis and in vivo evaluation of 5-(5-(6-[¹¹C]methyl-3,6-diazabicyclo[3.2.0]heptan-3-yl)pyridin-2-yl)-1H-indole [¹¹C]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 [¹¹C]CH₃I afforded [¹¹C]rac-1 in an average radiochemical yield of 30±5% (n=5) with high radiochemical purity and an average specific radioactivity of 444±74GBq/μmol (n=5). The total synthesis time was 30min from end-of-bombardment. Biodistribution studies in mice showed that [¹¹C]rac-1 penetrates the blood–brain barrier and specifically labels neuronal α7-nAChRs.
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