916141-36-1

916141-36-1 structure

Name: TCS 1102
Chemical Name: N-2-Biphenylyl-1-{[(1-methyl-1H-benzimidazol-2-yl)sulfanyl]acetyl }-L-prolinamide
CAS Number: 916141-36-1
Molecular Formula: C₂₇H₂₆N₄O₂S
Molecular Weight: 470.58600
Catalog: Signaling Pathways GPCR/G Protein Orexin Receptor (OX Receptor)
Create Date: 2016-10-20 13:33:33
Modify Date: 2024-01-06 08:23:36
TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).IC50 value: 0.2 nM (Ki, OX2 receptor); 3 nM (Ki, OX1 receptor) [1]Target: OX2 and OX1 receptorTCS-1102 (10 and 20 mg/kg, i.p.) were found to decrease fear and anxiety in rats 14 days after exposure to footshock.Furthermore, TCS-1102 (10 mg/kg, i.p.) was found to have anxiolytic effects that were specific for HR when tested in the elevated T-maze. [2]

Name	N-2-Biphenylyl-1-{[(1-methyl-1H-benzimidazol-2-yl)sulfanyl]acetyl }-L-prolinamide
Synonyms	TCS 1102

Description	TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).IC50 value: 0.2 nM (Ki, OX2 receptor); 3 nM (Ki, OX1 receptor) [1]Target: OX2 and OX1 receptorTCS-1102 (10 and 20 mg/kg, i.p.) were found to decrease fear and anxiety in rats 14 days after exposure to footshock.Furthermore, TCS-1102 (10 mg/kg, i.p.) was found to have anxiolytic effects that were specific for HR when tested in the elevated T-maze. [2]
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Orexin Receptor (OX Receptor) Research Areas >> Neurological Disease
References	[1]. Bergman JM, et al. Proline bis-amides as potent dual orexin receptor antagonists. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1425-30. [2]. Chen X, et al. Orexins (hypocretins) contribute to fear and avoidance in rats exposed to a single episode of footshocks. Brain Struct Funct. 2013 Aug 18.