Stereoselective synthesis and biodistribution of potent [11C]-labeled antagonists for positron emission tomography imaging of muscarinic receptors in the airways

…, TW van der Mark, J Kraan, K Ensing…

Index: Visser, Ton J.; Van Waarde, Aren; Jansen, Twan J. H.; Visser, Gerben M.; Van Der Mark, Thom W.; Kraan, Jan; Ensing, Kees; Vaalburg, Willem Journal of Medicinal Chemistry, 1997 , vol. 40, # 1 p. 117 - 124

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Citation Number: 16

Abstract

Quantitation of muscarinic receptors in the lungs in vivo with positron emission tomography (PET) is of clinical interest. For that purpose we decided to develop [11C]-labeled ligands with a high affinity (KD< 0.1 nM). Three quaternary muscarinic antagonists, racemic N- methylpiperidin-4-yl 2-cyclohexyl-2-hydroxy-2-phenylacetate methiodide 1a (p KB= 10.39), its (R)-isomer 1b (p KB= 11.08), and (R, R)-quinuclidin-3-yl 2-cyclohexyl-2-hydroxy-2- ...