N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide

Orexin receptors 1 (OX1R) and OX2R mediate the action of the neuropeptides orexin A and orexin B. TCS 1102 is a dual antagonist of both OX1R and OX2R (K_is = 0.2 and 3 nM, respectively). It is a poor substrate for P-glycoprotein and, as a result, demonstrates good brain penetration when administered intraperitoneally. Dual orexin receptor antagonists, including TCS 1102, promote sleep and prevent drug-induced plasticity and drug relapse. Systemic injection of TCS 1102 (10 mg/kg i.p.) in rats decreases fear and anxiety in response to acute episodes of stress.

TCS 1102 is a dual antagonist of both OX1R and OX2R. It is a poor substrate for P-glycoprotein and, as a result, demonstrates good brain penetration when administered intraperitoneally. Dual orexin receptor antagonists, including TCS 1102, promote sleep and prevent drug-induced plasticity and drug relapse.

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