Abstract
Incorporation of fluorine at the 4-position of an existing series of sulfonyl piperidine 5-HT 2A antagonists gave compounds with increased selectivity over the IKr potassium channel. This work led to the identification of 3b, a compound that gave no increase in QT c in the anesthetized dog up to plasma levels as high as 148 μM. Furthermore, 3b has been shown to increase slow-wave sleep bout duration and to decrease the number of awakenings in rats, indicating the potential utility of 5-HT 2A antagonists in the treatment of insomnia.
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