PF-4800567

PF-4800567
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEBI
Chemical and physical data
Formula C17H18ClN5O2
Molar mass 359.809 g/mol
3D model (JSmol)

PF-4800567 is a drug developed by Pfizer which acts as a selective inhibitor of the enzyme Casein kinase 1 epsilon (CK1-ε), and has mainly been used in the study of the casein kinase 1 enzymes in the regulation of circadian rhythm,[1][2] as well as showing potential neuroprotective effects.[3] While this research has shown that circadian rhythm is modulated primarily by the alternate isoform CK1-δ rather than CK1-ε,[4] both PF-4800567 and the related non-selective CK1-δ/ε inhibitor PF-670462 were found in animal studies to enhance responses to certain drugs of abuse such as methamphetamine and fentanyl, which suggests a role for CK1-ε in negative regulation of sensitivity to stimulant and opioid drugs.[5][6]

References

  1. ↑ Walton, KM; Fisher, K; Rubitski, D; Marconi, M; Meng, QJ; Sládek, M; Adams, J; Bass, M; Chandrasekaran, R; Butler, T; Griffor, M; Rajamohan, F; Serpa, M; Chen, Y; Claffey, M; Hastings, M; Loudon, A; Maywood, E; Ohren, J; Doran, A; Wager, TT (Aug 2009). "Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period". Journal of Pharmacology and Experimental Therapeutics. 330 (2): 430–9. doi:10.1124/jpet.109.151415. PMID 19458106.
  2. ↑ Meng, QJ; Maywood, ES; Bechtold, DA; Lu, WQ; Li, J; Gibbs, JE; Dupré, SM; Chesham, JE; Rajamohan, F; Knafels, J; Sneed, B; Zawadzke, LE; Ohren, JF; Walton, KM; Wager, TT; Hastings, MH; Loudon, AS (Aug 2010). "Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes". Proceedings of the National Academy of Sciences USA. 107 (34): 15240–5. doi:10.1073/pnas.1005101107. PMC 2930590. PMID 20696890.
  3. ↑ Perez, D. I.; Gil, C.; Martinez, A. (2011). "Protein kinases CK1 and CK2 as new targets for neurodegenerative diseases". Medicinal Research Reviews. 31 (6): 924–954. doi:10.1002/med.20207. PMID 20577972.
  4. ↑ Etchegaray, J. P.; Yu, E. A.; Indic, P.; Dallmann, R.; Weaver, D. R. (2010). Yamazaki, Shin, ed. "Casein Kinase 1 Delta (CK1δ) Regulates Period Length of the Mouse Suprachiasmatic Circadian Clock in Vitro". PLoS ONE. 5 (4): e10303. doi:10.1371/journal.pone.0010303. PMC 2858662. PMID 20421981.
  5. ↑ Bryant, CD; Graham, ME; Distler, MG; Munoz, MB; Li, D; Vezina, P; Sokoloff, G; Palmer, AA (May 2009). "A role for casein kinase 1 epsilon in the locomotor stimulant response to methamphetamine". Psychopharmacology. 203 (4): 703–11. doi:10.1007/s00213-008-1417-z. PMC 2729782. PMID 19050854.
  6. ↑ Bryant, C. D.; Parker, C. C.; Zhou, L.; Olker, C.; Chandrasekaran, R. Y.; Wager, T. T.; Bolivar, V. J.; Loudon, A. S.; Vitaterna, M. H.; Turek, F. W.; Palmer, A. A. (2011). "Csnk1e is a Genetic Regulator of Sensitivity to Psychostimulants and Opioids". Neuropsychopharmacology. 37 (4): 1026–1035. doi:10.1038/npp.2011.287. PMC 3280656. PMID 22089318.


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