ciproxifan and Sleep-Disorders--Circadian-Rhythm

ciproxifan has been researched along with Sleep-Disorders--Circadian-Rhythm* in 1 studies

Other Studies

1 other study(ies) available for ciproxifan and Sleep-Disorders--Circadian-Rhythm

Article	Year
Discovery of a potent, selective, and orally bioavailable histamine H3 receptor antagonist SAR110068 for the treatment of sleep-wake disorders. Bioorganic & medicinal chemistry letters, 2013, Nov-15, Volume: 23, Issue:22 Previous studies have shown that compound 1 displayed high affinity towards histamine H3 receptor (H3R), (human (h-H3R), K(i)=8.6 nM, rhesus monkey (rh-H3R), K(i)=1.2 nM, and rat (r-H3R), K(i)=16.5 nM), but exhibited high affinity for hERG channel. Herein, we report the discovery of a novel, potent, and highly selective H3R antagonist/inverse agonist 5a(SS) (SAR110068) with acceptable hERG channel selectivity and desirable pharmacological and pharmacokinetic properties through lead optimization sequence. The significant awakening effects of 5a(SS) on sleep-wake cycles studied by using EEG recording in rats during their light phase support its potential therapeutic utility in human sleep-wake disorders. Topics: Administration, Oral; Animals; Dogs; Drug Stability; Guinea Pigs; Haplorhini; Histamine H3 Antagonists; Humans; Male; Mice; Pyrans; Pyrrolidines; Rabbits; Rats; Rats, Sprague-Dawley; Receptors, Histamine H3; Sheep; Sleep Disorders, Circadian Rhythm; Substrate Specificity	2013

Article

Year

Discovery of a potent, selective, and orally bioavailable histamine H3 receptor antagonist SAR110068 for the treatment of sleep-wake disorders.

Bioorganic & medicinal chemistry letters, 2013, Nov-15, Volume: 23, Issue:22

Previous studies have shown that compound 1 displayed high affinity towards histamine H3 receptor (H3R), (human (h-H3R), K(i)=8.6 nM, rhesus monkey (rh-H3R), K(i)=1.2 nM, and rat (r-H3R), K(i)=16.5 nM), but exhibited high affinity for hERG channel. Herein, we report the discovery of a novel, potent, and highly selective H3R antagonist/inverse agonist 5a(SS) (SAR110068) with acceptable hERG channel selectivity and desirable pharmacological and pharmacokinetic properties through lead optimization sequence. The significant awakening effects of 5a(SS) on sleep-wake cycles studied by using EEG recording in rats during their light phase support its potential therapeutic utility in human sleep-wake disorders.

Topics: Administration, Oral; Animals; Dogs; Drug Stability; Guinea Pigs; Haplorhini; Histamine H3 Antagonists; Humans; Male; Mice; Pyrans; Pyrrolidines; Rabbits; Rats; Rats, Sprague-Dawley; Receptors, Histamine H3; Sheep; Sleep Disorders, Circadian Rhythm; Substrate Specificity

2013