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JNJ-3792165

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JNJ-3792165
Identifiers
  • 1-[(2,6-dichlorophenyl)methyl]-5-methyl-N-(3-methylphenyl)pyrazole-3-carboxamide
PubChem CID
ChemSpider
Chemical and physical data
FormulaC19H17Cl2N3O
Molar mass374.27 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

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  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.
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