JNJ-3792165

Last updated
JNJ-3792165
JNJ-3792165 structure.png
Identifiers
  • 1-[(2,6-dichlorophenyl)methyl]-5-methyl-N-(3-methylphenyl)pyrazole-3-carboxamide
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
Formula C19H17Cl2N3O
Molar mass 374.27 g·mol−1
3D model (JSmol)
  • CC1=CC(=CC=C1)NC(=O)C2=NN(C(=C2)C)CC3=C(C=CC=C3Cl)Cl
  • InChI=1S/C19H17Cl2N3O/c1-12-5-3-6-14(9-12)22-19(25)18-10-13(2)24(23-18)11-15-16(20)7-4-8-17(15)21/h3-10H,11H2,1-2H3,(H,22,25)
  • Key:SKUQQQWNGFTXFN-UHFFFAOYSA-N

JNJ-3792165 is a chemical compound which acts as a small-molecule antagonist of the previously orphan receptor GPR139. It has been shown to modulate dopamine release in the brain via interaction with the Dopamine receptor D2, and increases the effect of morphine at the mu opioid receptor. [1] [2] [3] [4] [5]

References

  1. Nepomuceno D, Kuei C, Dvorak C, Lovenberg T, Liu C, Bonaventure P (2018). "Re-evaluation of Adrenocorticotropic Hormone and Melanocyte Stimulating Hormone Activation of GPR139 in Vitro". Frontiers in Pharmacology. 9: 157. doi: 10.3389/fphar.2018.00157 . PMC   5863515 . PMID   29599718.
  2. Wang L, Lee G, Kuei C, Yao X, Harrington A, Bonaventure P, et al. (2019). "GPR139 and Dopamine D2 Receptor Co-express in the Same Cells of the Brain and May Functionally Interact". Frontiers in Neuroscience. 13: 281. doi: 10.3389/fnins.2019.00281 . PMC   6443882 . PMID   30971885.
  3. Vedel L, Nøhr AC, Gloriam DE, Bräuner-Osborne H (June 2020). "Pharmacology and function of the orphan GPR139 G protein-coupled receptor". Basic & Clinical Pharmacology & Toxicology. 126 (Suppl 6): 35–46. doi:10.1111/bcpt.13263. PMC   7318219 . PMID   31132229.
  4. Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsøe K, et al. (February 2022). "Molecular insights into ligand recognition and G protein coupling of the neuromodulatory orphan receptor GPR139". Cell Research. 32 (2): 210–213. doi:10.1038/s41422-021-00591-w. PMC   8807744 . PMID   34916631.
  5. 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. S2CID   256562486.