916141-36-1

Basic information

• Product Name: N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide
• Synonyms: 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;(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;TCS-102;(2S)- 2-Pyrrolidinecarboxamide, N-[1,1'-biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl];N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide;TCS 1102
• CAS NO: 916141-36-1
• Molecular Formula: C27H26N4O2S
• Molecular Weight: 470.58594
• Product Categories: Inhibitors
• Mol File: 916141-36-1.mol
• Article Data: 3

Chemical Properties

• Appearance: /
• Storage Temp.: Store at RT
• CAS DataBase Reference: N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide(CAS DataBase Reference)
• NIST Chemistry Reference: N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide(916141-36-1)
• EPA Substance Registry System: N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide(916141-36-1)

Safety Data

• Hazardous Substances Data: 916141-36-1(Hazardous Substances Data)

Usage

Description

N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide, also known as TCS 1102, is a dual antagonist of both orexin receptors 1 (OX1R) and OX2R. It is a poor substrate for P-glycoprotein, which allows for good brain penetration when administered intraperitoneally. TCS 1102 has potential applications in promoting sleep and preventing drug-induced plasticity and drug relapse.

Uses

Used in Pharmaceutical Industry:
TCS 1102 is used as a dual orexin receptor antagonist for promoting sleep and preventing drug-induced plasticity and drug relapse. Its ability to block both OX1R and OX2R receptors makes it a potential treatment for sleep disorders and addiction.
Used in Neuroscience Research:
TCS 1102 is used as a research tool to study the role of orexin receptors in the central nervous system. Its ability to penetrate the blood-brain barrier and block orexin receptors makes it a valuable compound for investigating the neural mechanisms underlying sleep, wakefulness, and stress responses.
Used in Stress and Anxiety Management:
TCS 1102 is used as a potential therapeutic agent for managing stress and anxiety. Systemic injection of TCS 1102 in rats has been shown to decrease fear and anxiety in response to acute episodes of stress, suggesting its potential use in treating stress-related disorders in humans.

Upstream product

• 916143-36-7 C₁₅H₁₇N₃O₃S 
• 90-41-5 2-phenylaniline 
• 2360-22-7 1-methyl-1H-benzimidazole-2-thiol 
• 134469-07-1 Benzimidazol-2-thiol 
• 74-88-4 methyl iodide 
• 916201-30-4 (S)-2-([1,1'-biphenyl]-2-yl)-1-(pyrrolidin-2-yl)ethanone 
• 3042-00-0 2-(1H-benzimidazol-2-ylthio)acetic acid 
• 916143-32-3 methyl 1-{[(1H-benzimidazol-2-yl)sulfanyl]acetyl}pyrrolidine-2-carboxylate 

Relevant articles and documents

Radiosynthesis of [11C]BBAC and [11C]BBPC as potential PET tracers for orexin2 receptors

Radiosynthesis of [N-methyl-11C](S)-N-([1,1′-biphenyl]-2- yl)-1-(2-((1-methyl-1H-benzo[d]imidazol-2-yl)thio)acetyl)pyrrolidine-2- carboxamide ([11C]BBAC or [11C]3) and [N-methyl- 11C] (S)-N-([1,1′-biphenyl]-2-yl

PROLINE BIS-AMIDE OREXIN RECEPTOR ANTAGONISTS

The present invention is directed to proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.