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  • Title: 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.
    Author: Gao Y, Ravert HT, Holt D, Dannals RF, Horti AG.
    Journal: Appl Radiat Isot; 2007 Aug; 65(8):947-51. PubMed ID: 17566748.
    Abstract:
    6-Chloro-3-((1-methyl)-2-(S)-pyrrolidinyl)methoxy)-5-(2-fluoropyridin-4-yl)pyridine (JHU85270), a novel high-affinity ligand for the alpha4beta2 nicotine acetylcholine receptor (nAChR) (K(i)=86, 115 pM; K(i)(JHU85270)/K(i)(epibatidine)=1.7) with a log D(7.4)=1.6 was synthesized in 56% overall yield. [(11)C]JHU85270 was synthesized from [(11)C]-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 [(11)C]JHU85270 was 37%+/-3% (non-decay corrected). The average specific radioactivity was 398+/-165 GBq/micromol (10750+/-4468 mCi/micromol) and the radiochemical purity was greater than 99%.
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