title: Radiosynthesis of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[(11)C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine, a high affinity ligand for studying nicotinic acetylcholine receptors by positron emission tomography.
abstract: 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-methyl-2-(S)-pyrrolidinylmethoxy)pyridine (1b) exhibited high affinity for nicotinic acetylcholine receptors in the in vitro competition binding assays, with a K(d) value in the low picomolar range, performed at room temperature and at physiological temperature. An efficient radiochemical synthesis of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[(11)C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine (1c), a potential tracer for the study of nAChR by positron emission tomography, has been developed.
authors.affiliation: Brain Imaging Center, National Institute on Drug Abuse, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA. laverneb@prodigy.net
authors.forename: L L
authors.initials: LL
authors.lastname: Brown
authors.forename: O
authors.initials: O
authors.lastname: Pavlova
authors.forename: A
authors.initials: A
authors.lastname: Mukhin
authors.forename: A S
authors.initials: AS
authors.lastname: Kimes
authors.forename: A G
authors.initials: AG
authors.lastname: Horti
mesh_terms: D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000166:cytology; D002250:Carbon Radioisotopes; D002462:Cell Membrane / Q000737:chemistry; D008024:Ligands; D011725:Pyridines / Q000138:chemical synthesis* / Q000378:metabolism; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000378:metabolism; D011869:Radioligand Assay; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000378:metabolism; D051381:Rats; D011978:Receptors, Nicotinic / Q000032:analysis* / Q000378:metabolism; D014055:Tomography, Emission-Computed
chemical_list: C449180:5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-methyl-2-pyrrolidinylmethoxy)pyridine; D002250:Carbon Radioisotopes; D008024:Ligands; D011725:Pyridines; D011759:Pyrrolidines; D019275:Radiopharmaceuticals; D011978:Receptors, Nicotinic