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  • Title: 4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.
    Author: Fish LR, Gilligan MT, Humphries AC, Ivarsson M, Ladduwahetty T, Merchant KJ, O'Connor D, Patel S, Philipps E, Vargas HM, Hutson PH, MacLeod AM.
    Journal: Bioorg Med Chem Lett; 2005 Aug 15; 15(16):3665-9. PubMed ID: 15993598.
    Abstract:
    Incorporation of fluorine at the 4-position of an existing series of sulfonyl piperidine 5-HT2A 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 QTc in the anesthetized dog up to plasma levels as high as 148 microM. 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-HT2A antagonists in the treatment of insomnia.
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