Radiosynthesis of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[ 11C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine, a high affinity ligand for studying nicotinic acetylcholine receptors by positron emission tomography

La Verne L. Brown, Olga Pavlova, Alexey Mukhin, Alane S. Kimes, Andrew G. Horti

Research output: Contribution to journalArticlepeer-review

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-[11C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine (1c), a potential tracer for the study of nAChR by positron emission tomography, has been developed.

Original languageEnglish (US)
Pages (from-to)3055-3058
Number of pages4
JournalBioorganic and Medicinal Chemistry
Volume9
Issue number11
DOIs
StatePublished - Oct 9 2001
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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