1802326-66-4 Usage
Uses
Used in Pharmaceutical Industry:
JNJ 63533054 is used as a therapeutic agent for the treatment of alcohol dependence. It has been shown to decrease compulsive-like alcohol drinking and hyperalgesia in alcohol-dependent rodents, making it a promising candidate for the development of new treatments for alcohol use disorder.
Additionally, JNJ 63533054 is used as a potential treatment for pain management. It has been demonstrated to suppress morphine intake in a mouse self-administration model, suggesting its potential in reducing opioid dependence and providing alternative pain relief options.
Furthermore, JNJ 63533054 is used as a research tool in the study of the central nervous system, particularly in understanding the role of hGPR139 in various physiological processes. Its ability to penetrate the brain and selectively bind to GPR139 makes it a valuable compound for investigating the receptor's function and potential therapeutic applications.
Biochem/physiol Actions
JNJ-63533054 is a potent and selective agonist of the orphan receptor hGPR139, a GPCR receptor expressed in the brain in circumventricular regions of the habenula and septum. JNJ-63533054 has an EC50 value of 16 nM, crosses the blood-brain barrier, and is orally available.
References
1) Dvorak?et al.?(2015),?Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor;?ACS Med. Chem. Lett.,?6?1015
2) Liu?et al. (2015),?GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine; Mol. Pharmacol.,?88?911
3) Kononoff?et al.?(2018),?Systemic and Intra-Habenular Activation of the Orphan G Protein-Coupled Receptor GPR139 Decreases Compulsive-Like Alcohol Drinking and Hyperalgesia in Alcohol-Dependent Rats;?eNeuro,?5?ENEURO 0153-18 2018
4) Wang?et al.?(2019),?Genetic behavioral screen identifies an orphan anti-opioid system; Science,?365?1267
Check Digit Verification of cas no
The CAS Registry Mumber 1802326-66-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,8,0,2,3,2 and 6 respectively; the second part has 2 digits, 6 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1802326-66:
(9*1)+(8*8)+(7*0)+(6*2)+(5*3)+(4*2)+(3*6)+(2*6)+(1*6)=144
144 % 10 = 4
So 1802326-66-4 is a valid CAS Registry Number.
1802326-66-4Relevant articles and documents
Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor
Dvorak, Curt A.,Coate, Heather,Nepomuceno, Diane,Wennerholm, Michelle,Kuei, Chester,Lord, Brian,Woody, David,Bonaventure, Pascal,Liu, Changlu,Lovenberg, Timothy,Carruthers, Nicholas I.
, p. 1015 - 1018 (2015)
A focused high throughput screening for GPR139 was completed for a select 100K compounds, and new agonist leads were identified. Subsequent analysis and structure-activity relationship studies identified (S)-3-chloro-N-(2-oxo-2-((1-phenylethyl)amino)ethyl
