In vivo muscarinic binding selectivity of (R, S)-and (R, R)-[18F]-fluoromethyl QNB

…, EM Jagoda, CJ Endres, MG Der, P Herscovitch…

Index: Kiesewetter, Dale O.; Carson, Richard E.; Jagoda, Elaine M.; Endres, Christopher J.; Der, Margaret G.; Herscovitch, Peter; Eckelman, William C. Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 8 p. 1555 - 1567

Full Text: HTML

Citation Number: 14

Abstract

We have developed a multistep radiochemical synthesis of two diastereomers of quinuclidinyl-4-[18F]-fluoromethylbenzilate ([18F]-FMeQNB), a high-affinity ligand for muscarinic acetylcholine receptors. Previously, we have shown that the nonradioactive (R, R)-diastereomer displays an eightfold selectivity for M1 over M2 while the nonradioactive (R, S)-diastereomer displays a sevenfold selectivity for M2 over M1 in vitro. This paper reports ...