A dual antagonist of both OX1R and OX2R (Kis = 0.2 and 3 nM

TCS 1102 – 1 mg

Brand:
Cayman
CAS:
916141-36-1
Storage:
-20
UN-No:
Non-Hazardous - /

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).{29783} It is a poor substrate for P-glycoprotein and, as a result, demonstrates good brain penetration when administered intraperitoneally.{29783} Dual orexin receptor antagonists, including TCS 1102, promote sleep and prevent drug-induced plasticity and drug relapse.{29785} Systemic injection of TCS 1102 (10 mg/kg i.p.) in rats decreases fear and anxiety in response to acute episodes of stress.{29784}  

 

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Description

A dual antagonist of both OX1R and OX2R (Kis = 0.2 and 3 nM, respectively) that demonstrates good brain penetration when administered intraperitoneally; promotes sleep, prevents drug-induced plasticity and drug relapse, and decreases fear and anxiety in response to acute episodes of stress

Formal name: (2S)-N-[1,1′-biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl]-2-pyrrolidinecarboxamide

Synonyms: 

Molecular weight: 470.6

CAS: 916141-36-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Behavioral Neuroscience|Sleep & Biological Rhythms

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