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%.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Arabinofuranosyluracil / analogs & derivatives*
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Arabinofuranosyluracil / chemistry
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Arabinofuranosyluracil / isolation & purification
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Brain / diagnostic imaging
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Brain / metabolism
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Fluorine Radioisotopes / chemistry*
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Fluorine Radioisotopes / isolation & purification
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Fluorine Radioisotopes / pharmacokinetics
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Humans
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Isotope Labeling / methods
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Positron-Emission Tomography / methods*
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Pyridines / chemistry*
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Pyridines / pharmacokinetics*
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Pyrrolidines / chemistry*
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Pyrrolidines / pharmacokinetics*
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Radiopharmaceuticals / chemical synthesis
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Radiopharmaceuticals / isolation & purification
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Receptors, Nicotinic / metabolism
Substances
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6-chloro-3-(((1-methyl)-2-pyrrolidinyl)methoxy)-5-(2-fluoropyridin-4-yl)pyridine
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Fluorine Radioisotopes
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Pyridines
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Pyrrolidines
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Radiopharmaceuticals
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Receptors, Nicotinic
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Arabinofuranosyluracil
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clevudine