Abstract
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 ± 74 GBq/μmol (n = 5). The total synthesis time was 30 min from end-of-bombardment. Biodistribution studies in mice showed that [11C]rac-1 penetrates the blood-brain barrier and specifically labels neuronal α7-nAChRs.
Original language | English (US) |
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Pages (from-to) | 3698-3702 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 20 |
Issue number | 12 |
DOIs | |
State | Published - Jun 15 2012 |
Externally published | Yes |
Keywords
- Nicotinic acetylcholine receptors
- Positron emission tomography
- Radioligand
- α7-nAChR
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry