Novel TC‐99M N₂S₂ derivatives for imaging 5HT_2A receptors

Abstract

One of the major subtypes of serotonin receptors is the serotonin-2A (5-HTzA) receptors, which are therapeutic targets of psychiatric disorders i.e. schizophrenia and depression. Thus, imaging this particular receptors in vivo may provide useful information on the basic pharmacology of serotonin system and the relationship of clinical efficacy vs drug occupancy. Various PET and SPECT tracers have been reported, including "C-N-methylspiperohe2, '*F-altanserin3. "C-MDL 1009074 as well as R-5-'231-R-911505*6. In search of new tracers for SPECT imaging of 5-HTzAreceptors in the brain, we prepared a series of NzS2 derivatives of ketanserin and butyrophenone, known to have high affinities for HT2A receptors. The 1. Labelled Cpd Radiopham 41. Suppl. 1 (2001)