Compounds > 1-(2-4-difluorophenethyl)-4-(4-fluorophenylsulfonyl)piperidine

1-(2-4-difluorophenethyl)-4-(4-fluorophenylsulfonyl)piperidine and Sleep-Initiation-and-Maintenance-Disorders

1-(2-4-difluorophenethyl)-4-(4-fluorophenylsulfonyl)piperidine has been researched along with Sleep-Initiation-and-Maintenance-Disorders* in 1 studies

Other Studies

1 other study(ies) available for 1-(2-4-difluorophenethyl)-4-(4-fluorophenylsulfonyl)piperidine and Sleep-Initiation-and-Maintenance-Disorders

Article	Year
4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia. Bioorganic & medicinal chemistry letters, 2005, Aug-15, Volume: 15, Issue:16 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. Topics: Animals; Dogs; Drug Evaluation, Preclinical; Ligands; Molecular Structure; Piperidines; Rats; Serotonin 5-HT2 Receptor Antagonists; Sleep Initiation and Maintenance Disorders; Structure-Activity Relationship; Time Factors	2005

Article

Year

4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.

Bioorganic & medicinal chemistry letters, 2005, Aug-15, Volume: 15, Issue:16

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.

Topics: Animals; Dogs; Drug Evaluation, Preclinical; Ligands; Molecular Structure; Piperidines; Rats; Serotonin 5-HT2 Receptor Antagonists; Sleep Initiation and Maintenance Disorders; Structure-Activity Relationship; Time Factors

2005