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

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

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

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 (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.

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

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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