Syntheses, biological evaluation, and molecular modeling of 18F-labeled 4-anilidopiperidines as μ-opioid receptor imaging agents

…, S Platzer, J Marton, A Hauser, A Berthele…

Index: Henriksen, Gjermund; Platzer, Stefan; Marton, Janos; Hauser, Andrea; Berthele, Achim; Schwaiger, Markus; Marinelli, Luciana; Lavecchia, Antonio; Novellino, Ettore; Wester, Hans-Juergen Journal of Medicinal Chemistry, 2005 , vol. 48, # 24 p. 7720 - 7732

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Citation Number: 21

Abstract

The synthesis, evaluation, and molecular modeling of a series of 18F-labeled 4- anilidopiperidines with high affinities for the μ-opioid receptor (μ-OR) are reported. On the basis of the high brain uptake and selective retention in brain regions that contain a high concentration of the μ-OR, combined with a good metabolic stability,[18F] fluoro-pentyl carfentanil ([18F] 4) and 2-(±)[18F] fluoropropyl-sufentanil ([18F] 6) were selected as the ...