| Identification | Back Directory | [Name]
N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide | [CAS]
916141-36-1 | [Synonyms]
CS-916
TCS-102
TCS 1102
TCS1102; TCS-1102
TCS 1102 , CID11960895
N-2-Biphenylyl-1-{[(1-methyl-1H-benzimidazol-2-yl)sulfanyl]acetyl }-L-prolinamide
(2S)-1-[2-(1-METHYLBENZIMIDAZOL-2-YL)SULFANYLACETYL]-N-(2-PHENYLPHENYL)PYRROLIDINE-2-CARBOXAMIDE
N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide
(2S)-N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl]-2-pyrrolidinecarboxamide
(2S)- 2-Pyrrolidinecarboxamide, N-[1,1'-biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl]
2-PyrrolidinecarboxaMide, N-[1,1'-biphenyl]-2-yl-1-[2-[(1-Methyl-1H-benziMidazol-2-yl)thio]acetyl]-, (2S)-
(2S)-N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl]-2-pyrrolidinecarboxamide TCS1102
TCS 1102 N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide | [Molecular Formula]
C27H26N4O2S | [MDL Number]
MFCD18086894 | [MOL File]
916141-36-1.mol | [Molecular Weight]
470.59 |
| Chemical Properties | Back Directory | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMF: 25 mg/ml; DMF:PBS (pH 7) (1:10): 0.09 mg/ml; DMSO: 14 mg/ml; Ethanol: 10 mg/ml | [form ]
Powder | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
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 (Kis = 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. | [Uses]
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. | [in vivo]
TCS 1102 (compound 18) (15, 50, 100 mg/kg; i.p; single dose) induces locomotion inhibition in rat in a dose dependent manner[1].
TCS-1102 (10 and 20 mg/kg; i.p.; single dose) decreases fear and anxiety in rats after exposure to footshock. Furthermore, TCS-1102 (10 mg/kg; i.p.; single dose) also shows anxiolytic effects for high responders (HR) rat when tested in the elevated T-maze[3].
PK of TCS 1102 in Rat (100 mg/kg; i.p.; measured at 30 min)[1]
| CL (mL/min/kg) | T1/2 (h) | F (%) | Brain/plasma/CSF (nM) | | 3.7 | 0.3 | 11 | 2370/3500/43 |
| Animal Model: | Male Sprague–Dawley rats (130-160 g)[3] | | Dosage: | 10 and 20 mg/kg | | Administration: | Intraperitoneal injection; 30 min before received the footshocks | | Result: | Decreased fear and anxiety in rats 14 days after exposure to footshock. |
| [IC 50]
OX1 Receptor: 3 nM (Ki); OX2 Receptor: 0.2 nM (Ki) | [storage]
Store at RT | [References]
[1] JEFFREY M. BERGMAN . Proline bis-amides as potent dual orexin receptor antagonists[J]. Bioorganic & Medicinal Chemistry Letters, 2008, 18 4: Pages 1425-1430. DOI: 10.1016/j.bmcl.2008.01.001
[2] CHRISTOPHER J. WINROW . Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure[J]. Neuropharmacology, 2010, 58 1: Pages 185-194. DOI: 10.1016/j.neuropharm.2009.07.008
[3] XIAOYU CHEN. Orexins (hypocretins) contribute to fear and avoidance in rats exposed to a single episode of footshocks.[J]. Brain Structure & Function, 2014, 219 6: 2103-2118. DOI: 10.1007/s00429-013-0626-3 |
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