6-Chloro-3-(((1-[11C]methyl)-2-(S)-pyrrolidinyl)methoxy)-5-(2-fluoropyridin-4-yl)pyridine ([11C]JHU85270), a potent ligand for nicotinic acetylcholine receptor imaging by positron emission tomography

Add time:07/11/2019    Source:sciencedirect.com

6-Chloro-3-((1-methyl)-2-(S)-pyrrolidinyl)methoxy)-5-(2-fluoropyridin-4-yl)pyridine (JHU85270), a novel high-affinity ligand for the α4β2 nicotine acetylcholine receptor (nAChR) (Ki=86, 115 pM; KiJHU85270/Kiepibatidine=1.7) with a log D7.4=1.6 was synthesized in 56% overall yield. [11C]JHU85270 was synthesized from [11C]-methyl iodide and the corresponding normethyl precursor. The average time of radiosynthesis, purification, and formulation was 37 min from the end of bombardment. The average radiochemical yield of [11C]JHU85270 was 37%±3% (non-decay corrected). The average specific radioactivity was 398±165 GBq/μmol (10750±4468 mCi/μmol) and the radiochemical purity was greater than 99%.

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