Synthesis of a fluorine-18 labeled derivative of epibatidine for in vivo nicotinic acetylcholine receptor PET imaging

…, F Vaufrey, C Fuseau, M Bottlaender, C Crouzel

Index: Dolci, Lilian; Dolle, Frederic; Valette, Heric; Vaufrey, Francoise; Fuseau, Chantal; Bottlaender, Michel; Crouzel, Christian Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 3 p. 467 - 479

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Citation Number: 86

Abstract

Epibatidine (exo-2-(2′-chloro-5′-pyridyl)-7-azabicyclo [2.2. 1] heptane), a natural compound isolated from the skin of the Ecuadorian poison frog Epipedobates tricolor, is the most potent nicotinic acetylcholine receptor (nAChR) agonist reported to date. In order to visualize and quantify in vivo these receptors in human brain using Positron Emission Tomography (PET),[18F] norchlorofluoroepibatidine (exo-2-(2′-[18F] fluoro-5′-pyridyl)-7 ...