TCS-1102

TCS-1102 (also known as DORA-1) is a potent, small molecule dual orexin receptor antagonist (DORA). It exhibits high affinity for both orexin receptors, with Ki values of 0.2 nM for the OX2 receptor and 3 nM for the OX1 receptor. Developed by Merck & Co., Inc. as a research tool, it demonstrates excellent blood-brain barrier permeability and moderate oral bioavailability in animal models. In preclinical studies, TCS-1102 has been shown to promote sleep, reduce fear and anxiety-like behaviors, and inhibit orexin-A-induced feeding. It is primarily used in neuroscience research to investigate the role of the orexin system in sleep-wake regulation, metabolic processes, and emotional states. It is not currently in clinical development for human use.

Other names

(2S)-N-[1,1′-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl]-2-pyrrolidinecarboxamide