PF-4800567
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| Formula | C17H18ClN5O2 |
| Molar mass | 359.81 g·mol−1 |
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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[edit]
- ^ Walton KM, Fisher K, Rubitski D, Marconi M, Meng QJ, Sládek M, et al. (August 2009). "Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period". The Journal of Pharmacology and Experimental Therapeutics. 330 (2): 430–9. doi:10.1124/jpet.109.151415. PMID 19458106. S2CID 26565986.
- ^ Meng QJ, Maywood ES, Bechtold DA, Lu WQ, Li J, Gibbs JE, et al. (August 2010). "Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes". Proceedings of the National Academy of Sciences of the United States of America. 107 (34): 15240–5. Bibcode:2010PNAS..10715240M. doi:10.1073/pnas.1005101107. PMC 2930590. PMID 20696890.
- ^ Perez DI, Gil C, Martinez A (November 2011). "Protein kinases CK1 and CK2 as new targets for neurodegenerative diseases". Medicinal Research Reviews. 31 (6): 924–54. doi:10.1002/med.20207. hdl:10261/87060. PMID 20577972. S2CID 206251000.
- ^ Etchegaray JP, Yu EA, Indic P, Dallmann R, Weaver DR (April 2010). Yamazaki S (ed.). "Casein kinase 1 delta (CK1delta) regulates period length of the mouse suprachiasmatic circadian clock in vitro". PLOS ONE. 5 (4): e10303. Bibcode:2010PLoSO...510303E. doi:10.1371/journal.pone.0010303. PMC 2858662. PMID 20421981.
- ^ Bryant CD, Graham ME, Distler MG, Munoz MB, Li D, Vezina P, et al. (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.
- ^ Bryant CD, Parker CC, Zhou L, Olker C, Chandrasekaran RY, Wager TT, et al. (March 2012). "Csnk1e is a genetic regulator of sensitivity to psychostimulants and opioids". Neuropsychopharmacology. 37 (4): 1026–35. doi:10.1038/npp.2011.287. PMC 3280656. PMID 22089318.
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