Synonyms: BBAC; (2S)-N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl]-2-pyrrolidinecarboxamide; DORA-1; N-(1,1'-Biphenyl-2-yl)-1-{[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl}-L-prolinamide; TCS 1102; TCS1102; (2S)-N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl]-2-pyrrolidinecarboxamide
Molecular Formula: C27H26N4O2S
Molecular Weight: 470.59
Linear Structural Formula: C27H26N4O2S
MDL Number: MFCD18086894
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: TCS-1102 (DORA-1) is a high-affinity (Ki = 3 nM against [3H]-TCS-1102 for binding hOX1R and Ki = 0.2 nM against [3H]-pyrrolylphenyl analog for binding hOX2R) dual orexin receptor antagonist (DORA) that potently inhibits calcium mobilization in hOX1R & hOX2R CHO transfectants (IC50 = 17 & 4 nM, respectively). TCS-1102 promotes sleep (50-100 mg/kg p.o.), decreases fear/anxiety (10-20 mg/kg i.p.), and inhibits ADL-orexin B peptide-induced locomotion (by 56%/74%/100% with 15/50/100 mg/kg i.p. 30 min before ADL-XB ICV injection) with good pharmacokinetic properties, brain penetration (Brain/plasma conc. = 2.37 muM/3.50 muM 3 hrs post 100 mg/kg i.p.), and oral availability (Cmax/AUC(0-24h) = 1.21 muM/6.8 muM h and 3.01 muM/12.5 muM h, respectively post 50 and 100 mg/kg p.o. dosage) in rats in vivo.