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JNJ-54175446

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Chemical compound Pharmaceutical compound
JNJ-54175446
Legal status
Legal status
  • Investigational New Drug
Identifiers
IUPAC name
  • (R)-(2-chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyrimidin-2-yl)-4-methyl-6,7-dihydro-1H-triazolopyridin-5(4H)-yl)methanone
CAS Number
PubChem CID
Chemical and physical data
FormulaC18H13ClF4N6O
Molar mass440.79 g·mol
3D model (JSmol)
SMILES
  • C1C2=C(CCN1C(=O)C3=C(C(=CC=C3)C(F)(F)F)Cl)N(N=N2)C4=NC=C(C=N4)F
InChI
  • InChI=1S/C18H13ClF4N6O/c1-9-15-13(29(27-26-15)17-24-7-10(20)8-25-17)5-6-28(9)16(30)11-3-2-4-12(14(11)19)18(21,22)23/h2-4,7-9H,5-6H2,1H3/t9-/m1/s1
  • Key:CWFVVQFVGMFTBD-SECBINFHSA-N

JNJ-54175446 is an investigational P2X7 receptor antagonist developed by Janssen Pharmaceuticals. It is hoped that the drug can reduce neuroinflammation and therefore treat psychiatric disorders such as major depressive disorder.

See also

References

  1. Recourt, Kasper; van der Aart, Jasper; Jacobs, Gabriel; de Kam, Marieke; Drevets, Wayne; van Nueten, Luc; Kanhai, Kawita; Siebenga, Pieter; Zuiker, Rob; Ravenstijn, Paulien; Timmers, Maarten; van Gerven, Joop; de Boer, Peter (September 2020). "Characterisation of the pharmacodynamic effects of the P2X7 receptor antagonist JNJ-54175446 using an oral dexamphetamine challenge model in healthy males in a randomised, double-blind, placebo-controlled, multiple ascending dose trial". Journal of Psychopharmacology. 34 (9): 1030–1042. doi:10.1177/0269881120914206. PMID 32248747. S2CID 214809417.
  2. Timmers, Maarten; Ravenstijn, Paulien; Xi, Liwen; Triana-Baltzer, Gallen; Furey, Maura; Van Hemelryck, Sandy; Biewenga, Jeike; Ceusters, Marc; Bhattacharya, Anindya; van den Boer, Maarten; van Nueten, Luc; de Boer, Peter (December 2018). "Clinical pharmacokinetics, pharmacodynamics, safety, and tolerability of JNJ-54175446, a brain permeable P2X7 antagonist, in a randomised single-ascending dose study in healthy participants". Journal of Psychopharmacology. 32 (12): 1341–1350. doi:10.1177/0269881118800067. PMID 30260294. S2CID 52842478.
  3. Bhattacharya, Anindya; Ceusters, Marc (January 2020). "Targeting neuroinflammation with brain penetrant P2X7 antagonists as novel therapeutics for neuropsychiatric disorders". Neuropsychopharmacology. 45 (1): 234–235. doi:10.1038/s41386-019-0502-9. ISSN 0893-133X. PMC 6879571. PMID 31477815.
  4. Recourt, Kasper; de Boer, Peter; van der Ark, Peter; Benes, Heike; van Gerven, Joop M. A.; Ceusters, Marc; van Nueten, Luc; Drevets, Wayne C.; Bhatacharya, Anindya; Browning, Michael; Jacobs, Gabriel E. (24 July 2023). "Characterization of the central nervous system penetrant and selective purine P2X7 receptor antagonist JNJ-54175446 in patients with major depressive disorder". Translational Psychiatry. 13 (1): 266. doi:10.1038/s41398-023-02557-5. ISSN 2158-3188. PMC 10363543. PMID 37482560. S2CID 260114192.
  5. Koole, Michel; Schmidt, Mark E.; Hijzen, Anja; Ravenstijn, Paulien; Vandermeulen, Corinne; Van Weehaeghe, Donatienne; Serdons, Kim; Celen, Sofie; Bormans, Guy; Ceusters, Marc; Zhang, Wei; Van Nueten, Luc; Kolb, Hartmuth; de Hoon, Jan; Van Laere, Koen (May 2019). "18 F-JNJ-64413739, a Novel PET Ligand for the P2X7 Ion Channel: Radiation Dosimetry, Kinetic Modeling, Test-Retest Variability, and Occupancy of the P2X7 Antagonist JNJ-54175446". Journal of Nuclear Medicine. 60 (5): 683–690. doi:10.2967/jnumed.118.216747. PMID 30262518. S2CID 52880797.
  6. Xu, Yan; Miao, Xin; Ravenstijn, Paulien; Hijzen, Anja; Schmidt, Mark E.; Nandy, Partha; Zhou, Honghui (March 2020). "Translational Model-Informed Dose Selection for a Human Positron Emission Tomography Imaging Study of JNJ-54175446, a P2X7 Receptor Antagonist". Clinical and Translational Science. 13 (2): 309–317. doi:10.1111/cts.12711. PMC 7070800. PMID 31642608. S2CID 204850939.
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