M. Kassiou, H. Ravert, W. B. Mathews
May 1, 1997
Citations
0
Influential Citations
10
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
3-[(1-[ 11 C]Methyl-2(S)-pyrrolidinyl)methoxy]pyridine, [ 11 C]A-84543, a selective radioligand for neuronal nicotinic acetylcholine receptors (nAChRs) was prepared by N-alkylation of N-desmethyl A-84543 with [ 11 C]methyl iodide in DMF. The radioligand was purified by semi-preparative reverse-phase HPLC. The average specific radioactivity was 1755 mCi/μmol calculated at end-of-synthesis (EOS). The average time of synthesis, including formulation, was 17 min. The pharmacologically less active (R) enantiomer, 3-[(1-[ 11 C]methyl-2(R)-pyrrolidinyl) methoxy]pyridine was synthesized in an analogous manner using the appropriate N-desmethyl precursor. The specific radioactivity was calculated to be 2368 mCi/μmol (EOS).