PF-4800567

PF-4800567
Identifiers

IUPAC name 3-(3-chloro-phenoxymethyl)-1-(tetrahydro-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine
CAS Number	1188296-52-7
PubChem CID	53472153
IUPHAR/BPS	8050
ChemSpider	26325201
ChEBI	CHEBI:87237
Chemical and physical data
Formula	C₁₇H₁₈ClN₅O₂
Molar mass	359.809 g/mol
3D model (JSmol)	Interactive image
SMILES c4c(Cl)cccc4OCc(c1c3N)nn(c1ncn3)C2CCOCC2
InChI InChI=1S/C17H18ClN5O2/c18-11-2-1-3-13(8-11)25-9-14-15-16(19)20-10-21-17(15)23(22-14)12-4-6-24-7-5-12/h1-3,8,10,12H,4-7,9H2,(H2,19,20,21) Key:AUMDBEHGJRZSOO-UHFFFAOYSA-N

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

↑ 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. PMID 19458106. doi:10.1124/jpet.109.151415.
↑ 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. PMC 2930590 . PMID 20696890. doi:10.1073/pnas.1005101107.
↑ 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. PMID 20577972. doi:10.1002/med.20207.
↑ 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. PMC 2858662 . PMID 20421981. doi:10.1371/journal.pone.0010303.
↑ 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 (Berlin). 203 (4): 703–11. PMC 2729782 . PMID 19050854. doi:10.1007/s00213-008-1417-z.
↑ 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. PMC 3280656 . PMID 22089318. doi:10.1038/npp.2011.287.

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