SYNTHESIS AND PRELIMINARY IN-VIVO EVALUATION OF [C-11] MDL-100907 - APOTENT AND SELECTIVE RADIOLIGAND FOR THE 5-HT2A RECEPTOR SYSTEM

C-11-Labeled MDL 100907 and MDL 100009 were prepared by the reaction o f [C-11]CH3I with the corresponding phenol precursors. In vivo studies conducted in rats and a baboon demonstrated that intravenously inject ed [2-O[C-11]CH3]MDL 100907 was regionally distributed in the brain in a manner consistent with the known distribution of 5-HT2A receptors. Injection of [2-O[C-11]CH3]MDL 100009 resulted in a uniform brain dist ribution of radioactivity without regional localization consistent wit h the lower affinity of MDL 100009 for 5-HT2A receptors.