Chemistry:PF-4800567
From HandWiki
Short description: Chemical compound
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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
- ↑ "Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period". The Journal of Pharmacology and Experimental Therapeutics 330 (2): 430–9. August 2009. doi:10.1124/jpet.109.151415. PMID 19458106.
- ↑ "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. August 2010. doi:10.1073/pnas.1005101107. PMID 20696890. Bibcode: 2010PNAS..10715240M.
- ↑ "Protein kinases CK1 and CK2 as new targets for neurodegenerative diseases". Medicinal Research Reviews 31 (6): 924–54. November 2011. doi:10.1002/med.20207. PMID 20577972.
- ↑ "Casein kinase 1 delta (CK1delta) regulates period length of the mouse suprachiasmatic circadian clock in vitro". PLOS ONE 5 (4): e10303. April 2010. doi:10.1371/journal.pone.0010303. PMID 20421981. Bibcode: 2010PLoSO...510303E.
- ↑ "A role for casein kinase 1 epsilon in the locomotor stimulant response to methamphetamine". Psychopharmacology 203 (4): 703–11. May 2009. doi:10.1007/s00213-008-1417-z. PMID 19050854.
- ↑ "Csnk1e is a genetic regulator of sensitivity to psychostimulants and opioids". Neuropsychopharmacology 37 (4): 1026–35. March 2012. doi:10.1038/npp.2011.287. PMID 22089318.
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