PF-4800567: Difference between revisions

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;
CompTox Dashboard (EPA)	DTXSID20703849 ;
Chemical and physical data
Formula	C17H18ClN5O2
Molar mass	359.809 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES c4c(Cl)cccc4OCc(c1c3N)nn(c1ncn3)C2CCOCC2;

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Revision as of 02:45, 28 January 2012

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] While this research has shown that circadian rhythm is modulated primarily by the alternate isoform CK1-δ rather than CK1-ε,^[3] 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.^[4]^[5]

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. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. Journal of Pharmacology and Experimental Therapeutics. 2009 Aug;330(2):430-9. PMID 19458106
^ 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. Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes. Proceedings of the National Academy of Sciences USA. 2010 Aug 24;107(34):15240-5. PMID 20696890
^ Attention: This template ({{cite doi}}) is deprecated. To cite the publication identified by doi:10.1371/journal.pone.0010303, please use {{cite journal}} (if it was published in a bona fide academic journal, otherwise {{cite report}} with |doi=10.1371/journal.pone.0010303 instead.
^ Bryant CD, Graham ME, Distler MG, Munoz MB, Li D, Vezina P, Sokoloff G, Palmer AA. A role for casein kinase 1 epsilon in the locomotor stimulant response to methamphetamine. Psychopharmacology (Berlin). 2009 May;203(4):703-11. PMID 19050854
^ Bryant CD, Parker CC, Zhou L, Olker C, Chandrasekaran RY, Wager TT, Bolivar VJ, Loudon AS, Vitaterna MH, Turek FW, Palmer AA. Csnk1e Is a Genetic Regulator of Sensitivity to Psychostimulants and Opioids. Neuropsychopharmacology. 2011 Nov 16. PMID 22089318 DOI 10.1038/npp.2011.287

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[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. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. Journal of Pharmacology and Experimental Therapeutics. 2009 Aug;330(2):430-9. 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. Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes. Proceedings of the National Academy of Sciences USA. 2010 Aug 24;107(34):15240-5. PMID 20696890

[3] Attention: This template ({{cite doi}}) is deprecated. To cite the publication identified by doi:10.1371/journal.pone.0010303, please use {{cite journal}} (if it was published in a bona fide academic journal, otherwise {{cite report}} with |doi=10.1371/journal.pone.0010303 instead.

[4] Bryant CD, Graham ME, Distler MG, Munoz MB, Li D, Vezina P, Sokoloff G, Palmer AA. A role for casein kinase 1 epsilon in the locomotor stimulant response to methamphetamine. Psychopharmacology (Berlin). 2009 May;203(4):703-11. PMID 19050854

[5] Bryant CD, Parker CC, Zhou L, Olker C, Chandrasekaran RY, Wager TT, Bolivar VJ, Loudon AS, Vitaterna MH, Turek FW, Palmer AA. Csnk1e Is a Genetic Regulator of Sensitivity to Psychostimulants and Opioids. Neuropsychopharmacology. 2011 Nov 16. PMID 22089318 DOI 10.1038/npp.2011.287

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Revision as of 02:43, 28 January 2012 edit Meodipt (talk \| contribs) Autopatrolled, Extended confirmed users, Pending changes reviewers, Rollbackers 35,077 edits No edit summary ← Previous edit		Revision as of 02:45, 28 January 2012 edit undo Meodipt (talk \| contribs) Autopatrolled, Extended confirmed users, Pending changes reviewers, Rollbackers 35,077 edits No edit summary Next edit →
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	'''PF-4800567''' is a drug developed by [[Pfizer]] which acts as a selective inhibitor of the [[enzyme]] [[CSNK1E\|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]].<ref>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. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. ''Journal of Pharmacology and Experimental Therapeutics''. 2009 Aug;330(2):430-9. PMID 19458106</ref><ref>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. Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes. ''Proceedings of the National Academy of Sciences USA''. 2010 Aug 24;107(34):15240-5. PMID 20696890</ref> While this research has shown that circadian rhythm is modulated primarily by the alternate isoform CK1-δ rather than CK1-ε, 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.<ref>Bryant CD, Graham ME, Distler MG, Munoz MB, Li D, Vezina P, Sokoloff G, Palmer AA. A role for casein kinase 1 epsilon in the locomotor stimulant response to methamphetamine. ''Psychopharmacology (Berlin)''. 2009 May;203(4):703-11. PMID 19050854</ref><ref>Bryant CD, Parker CC, Zhou L, Olker C, Chandrasekaran RY, Wager TT, Bolivar VJ, Loudon AS, Vitaterna MH, Turek FW, Palmer AA. Csnk1e Is a Genetic Regulator of Sensitivity to Psychostimulants and Opioids. ''Neuropsychopharmacology''. 2011 Nov 16. PMID 22089318 DOI 10.1038/npp.2011.287</ref>		'''PF-4800567''' is a drug developed by [[Pfizer]] which acts as a selective inhibitor of the [[enzyme]] [[CSNK1E\|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]].<ref>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. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. ''Journal of Pharmacology and Experimental Therapeutics''. 2009 Aug;330(2):430-9. PMID 19458106</ref><ref>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. Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes. ''Proceedings of the National Academy of Sciences USA''. 2010 Aug 24;107(34):15240-5. PMID 20696890</ref> While this research has shown that circadian rhythm is modulated primarily by the alternate isoform CK1-δ rather than CK1-ε,<ref>{{Cite doi\|10.1371/journal.pone.0010303}}</ref> 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.<ref>Bryant CD, Graham ME, Distler MG, Munoz MB, Li D, Vezina P, Sokoloff G, Palmer AA. A role for casein kinase 1 epsilon in the locomotor stimulant response to methamphetamine. ''Psychopharmacology (Berlin)''. 2009 May;203(4):703-11. PMID 19050854</ref><ref>Bryant CD, Parker CC, Zhou L, Olker C, Chandrasekaran RY, Wager TT, Bolivar VJ, Loudon AS, Vitaterna MH, Turek FW, Palmer AA. Csnk1e Is a Genetic Regulator of Sensitivity to Psychostimulants and Opioids. ''Neuropsychopharmacology''. 2011 Nov 16. PMID 22089318 DOI 10.1038/npp.2011.287</ref>