Chemistry:JNJ-63533054
From HandWiki
JNJ-63533054 is a chemical compound which acts as a small-molecule agonist of the previously orphan receptor GPR139.[1][2][3] It has been used to investigate the role of GPR139 in various behavioral processes[4] including sleep,[5] anxiety,[6] addiction,[7] and cognition.[8]
References
- ↑ "Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor". ACS Medicinal Chemistry Letters 6 (9): 1015–1018. September 2015. doi:10.1021/acsmedchemlett.5b00247. PMID 26396690.
- ↑ "GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine". Molecular Pharmacology 88 (5): 911–925. November 2015. doi:10.1124/mol.115.100412. PMID 26349500.
- ↑ "Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139". European Journal of Pharmacology 943. March 2023. doi:10.1016/j.ejphar.2023.175553. PMID 36736525.
- ↑ "GPR139, an Ancient Receptor and an Emerging Target for Neuropsychiatric and Behavioral Disorders". Molecular Neurobiology 62 (7): 9324–9337. July 2025. doi:10.1007/s12035-025-04828-2. PMID 40102345.
- ↑ "Putative role of GPR139 on sleep modulation using pharmacological and genetic rodent models". European Journal of Pharmacology 882. September 2020. doi:10.1016/j.ejphar.2020.173256. PMID 32531213.
- ↑ "GPR139 agonist and antagonist differentially regulate retrieval and consolidation of fear memory in the zebrafish". Frontiers in Neuroscience 18. 2024. doi:10.3389/fnins.2024.1461148. PMID 39717703.
- ↑ "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 (3). 2018. doi:10.1523/ENEURO.0153-18.2018. PMID 29971251.
- ↑ "Up-regulation of GPR139 in the medial septum ameliorates cognitive impairment in two mouse models of Alzheimer's disease". International Immunopharmacology 130. March 2024. doi:10.1016/j.intimp.2024.111786. PMID 38447415.
