797749-90-7Relevant academic research and scientific papers
4-Fluorosulfonylpiperidines: Selective 5-HT2A ligands for the treatment of insomnia
Fish, L. Rebecca,Gilligan, Myra T.,Humphries, Alexander C.,Ivarsson, Magnus,Ladduwahetty, Tammy,Merchant, Kevin J.,O'Connor, Desmond,Patel, Smita,Philipps, Elisabeth,Vargas, Hugo M.,Hutson, Peter H.,MacLeod, Angus M.
, p. 3665 - 3669 (2007/10/03)
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 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-HT2A antagonists in the treatment of insomnia.
4-ARYLSULPHONYLPIPERIDINE DERIVATIVES FOR ANTAGONISM OF THE 5-HT2A RECEPTOR
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Page 25, (2010/02/09)
Compounds of formula (I): are selective antagonists of the 5-HT2A receptor, and hence are useful in treatment of adverse conditions at the central nervous system, such as sleep disorders and schizophrenia.
