JNJ-63533054

Last updated

JNJ-63533054
JNJ-63533054 structure.png
Identifiers
  • 3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]benzamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
PDB ligand
Chemical and physical data
Formula C17H17ClN2O2
Molar mass 316.79 g·mol−1
3D model (JSmol)
  • C[C@@H](C1=CC=CC=C1)NC(=O)CNC(=O)C2=CC(=CC=C2)Cl
  • InChI=1S/C17H17ClN2O2/c1-12(13-6-3-2-4-7-13)20-16(21)11-19-17(22)14-8-5-9-15(18)10-14/h2-10,12H,11H2,1H3,(H,19,22)(H,20,21)/t12-/m0/s1
  • Key:MWDVCHRYCKXEBY-LBPRGKRZSA-N

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

  1. ↑ Dvorak CA, Coate H, Nepomuceno D, Wennerholm M, Kuei C, Lord B, et al. (September 2015). "Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor". ACS Medicinal Chemistry Letters. 6 (9): 1015–1018. doi:10.1021/acsmedchemlett.5b00247. PMC   4569879 . PMID   26396690.
  2. ↑ Liu C, Bonaventure P, Lee G, Nepomuceno D, Kuei C, Wu J, et al. (November 2015). "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. doi:10.1124/mol.115.100412. PMID   26349500.
  3. ↑ Pallareti L, Rath TF, Trapkov B, Tsonkov T, Nielsen AT, Harpsøe K, et al. (March 2023). "Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139". European Journal of Pharmacology. 943 175553. doi:10.1016/j.ejphar.2023.175553. PMID   36736525.
  4. ↑ Chan M, Ogawa S (July 2025). "GPR139, an Ancient Receptor and an Emerging Target for Neuropsychiatric and Behavioral Disorders". Molecular Neurobiology. 62 (7): 9324–9337. doi:10.1007/s12035-025-04828-2. PMC   12208981 . PMID   40102345.
  5. ↑ Wang L, Dugovic C, Yun S, White A, Lord B, Dvorak C, et al. (September 2020). "Putative role of GPR139 on sleep modulation using pharmacological and genetic rodent models". European Journal of Pharmacology. 882 173256. doi:10.1016/j.ejphar.2020.173256. PMID   32531213.
  6. ↑ Roy N, Ogawa S, Tsuda S, Parhar IS (2024). "GPR139 agonist and antagonist differentially regulate retrieval and consolidation of fear memory in the zebrafish". Frontiers in Neuroscience. 18 1461148. doi: 10.3389/fnins.2024.1461148 . PMC   11665214 . PMID   39717703.
  7. ↑ Kononoff J, Kallupi M, Kimbrough A, Conlisk D, de Guglielmo G, George O (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 (3). doi:10.1523/ENEURO.0153-18.2018. PMC   6027959 . PMID   29971251.
  8. ↑ Mu R, Hou X, Liu Q, Wang W, Qin C, Li H (March 2024). "Up-regulation of GPR139 in the medial septum ameliorates cognitive impairment in two mouse models of Alzheimer's disease". International Immunopharmacology. 130 111786. doi:10.1016/j.intimp.2024.111786. PMID   38447415.
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