TCS 1102

TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).IC50 value: 0.2 nM (Ki, OX2 receptor); 3 nM (Ki, OX1 receptor) [1]Target: OX2 and OX1 receptorTCS-1102 (10 and 20 mg/kg, i.p.) were found to decrease fear and anxiety in rats 14 days after exposure to footshock.Furthermore, TCS-1102 (10 mg/kg, i.p.) was found to have anxiolytic effects that were specific for HR when tested in the elevated T-maze. [2]

Signaling Pathways >> GPCR/G Protein >> Orexin Receptor (OX Receptor)

Research Areas >> Neurological Disease

[1]. Bergman JM, et al. Proline bis-amides as potent dual orexin receptor antagonists. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1425-30.

[2]. Chen X, et al. Orexins (hypocretins) contribute to fear and avoidance in rats exposed to a single episode of footshocks. Brain Struct Funct. 2013 Aug 18.

SB 334867 | lemborexant | Almorexant HCI | Filorexant | Orexin 2 Receptor Agonist | TCS-OX2-29 | MK-1064 | SB-674042 | GSK1059865 | IPSU | SB408124 | MK-3697 | Nemorexant | Orexin B (mouse, rat) | SB-649868