1301738-60-2Relevant articles and documents
Structure-activity relationship, biological, and pharmacological characterization of the proline sulfonamide ACT-462206: A potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonist
Boss, Christoph,Roch-Brisbare, Catherine,Steiner, Michel A.,Treiber, Alexander,Dietrich, Hendrik,Jenck, Francois,Von Raumer, Markus,Sifferlen, Thierry,Brotschi, Christine,Heidmann, Bibia,Williams, Jodi T.,Aissaoui, Hamed,Siegrist, Romain,Gatfield, John
supporting information, p. 2486 - 2496 (2015/04/22)
The orexin system consists of two G-protein-coupled receptors, the orexin 1 and orexin 2 receptors, widely expressed in diverse regions of the brain, and two peptide agonists, orexin A and orexin B, which are produced in a small assembly of neurons in the lateral hypothalamus. The orexin system plays an important role in the maintenance of wakefulness. Several compounds (almorexant, SB-649868, suvorexant) have been in advanced clinical trials for treating primary insomnia. ACT-462206 is a new, potent, and selective dual orexin receptor antagonist (DORA) that inhibits the stimulating effects of the orexin peptides at both the orexin 1 and 2 receptors. It decreases wakefulness and increases non-rapid eye movement (non-REM) and REM sleep while maintaining natural sleep architectures in rat and dog electroencephalography/electromyography (EEG/EMG) experiments. ACT-462206 shows anxiolytic-like properties in rats without affecting cognition and motor function. It is therefore a potential candidate for the treatment of insomnia.
Structure-Activity Relationship, Biological, and Pharmacological Characterization of the Proline Sulfonamide ACT-462206: A Potent, Brain-Penetrant Dual Orexin1/Orexin2 Receptor Antagonist
Boss, Christoph,Roch-Brisbare, Catherine,Steiner, Michel A.,Treiber, Alexander,Dietrich, Hendrik,Jenck, Francois,Vonraumer, Markus,Sifferlen, Thierry,Brotschi, Christine,Heidmann, Bibia,Williams, Jodi T.,Aissaoui, Hamed,Siegrist, Romain,Gatfield, John
supporting information, p. 2486 - 2496 (2015/08/24)
The orexin system consists of two G-protein-coupled receptors, the orexin1 and orexin2 receptors, widely expressed in diverse regions of the brain, and two peptide agonists, orexinA and orexinB, which are produced in a small assembly of neurons in the lat
PROLINE SULFONAMIDE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
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Paragraph 0252, (2013/06/27)
The present invention relates to (S)-proline sulfonamide compounds of formula (I) wherein R1 and R2 are as described in the description, or pharmaceutically acceptable salts thereof, for use in the prevention or treatment of diseases