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Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764).
Wager TT, Pettersen BA, Schmidt AW, Spracklin DK, Mente S, Butler TW, Howard H, Lettiere DJ, Rubitski DM, Wong DF, Nedza FM, Nelson FR, Rollema H, Raggon JW, Aubrecht J, Freeman JK, Marcek JM, Cianfrogna J, Cook KW, James LC, Chatman LA, Iredale PA, Banker MJ, Homiski ML, Munzner JB, Chandrasekaran RY. Wager TT, et al. Among authors: chandrasekaran ry. J Med Chem. 2011 Nov 10;54(21):7602-20. doi: 10.1021/jm200939b. Epub 2011 Oct 7. J Med Chem. 2011. PMID: 21928839
Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period.
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. Walton KM, et al. J Pharmacol Exp Ther. 2009 Aug;330(2):430-9. doi: 10.1124/jpet.109.151415. Epub 2009 May 19. J Pharmacol Exp Ther. 2009. PMID: 19458106
Identification and Profiling of a Selective and Brain Penetrant Radioligand for in Vivo Target Occupancy Measurement of Casein Kinase 1 (CK1) Inhibitors.
Wager TT, Galatsis P, Chandrasekaran RY, Butler TW, Li J, Zhang L, Mente S, Subramanyam C, Liu S, Doran AC, Chang C, Fisher K, Grimwood S, Hedde JR, Marconi M, Schildknegt K. Wager TT, et al. Among authors: chandrasekaran ry. ACS Chem Neurosci. 2017 Sep 20;8(9):1995-2004. doi: 10.1021/acschemneuro.7b00155. Epub 2017 Jun 30. ACS Chem Neurosci. 2017. PMID: 28609096
Dopamine D3/D2 Receptor Antagonist PF-4363467 Attenuates Opioid Drug-Seeking Behavior without Concomitant D2 Side Effects.
Wager TT, Chappie T, Horton D, Chandrasekaran RY, Samas B, Dunn-Sims ER, Hsu C, Nawreen N, Vanase-Frawley MA, O'Connor RE, Schmidt CJ, Dlugolenski K, Stratman NC, Majchrzak MJ, Kormos BL, Nguyen DP, Sawant-Basak A, Mead AN. Wager TT, et al. Among authors: chandrasekaran ry. ACS Chem Neurosci. 2017 Jan 18;8(1):165-177. doi: 10.1021/acschemneuro.6b00297. Epub 2016 Oct 21. ACS Chem Neurosci. 2017. PMID: 27715007
Casein kinase 1δ/ε inhibitor PF-5006739 attenuates opioid drug-seeking behavior.
Wager TT, Chandrasekaran RY, Bradley J, Rubitski D, Berke H, Mente S, Butler T, Doran A, Chang C, Fisher K, Knafels J, Liu S, Ohren J, Marconi M, DeMarco G, Sneed B, Walton K, Horton D, Rosado A, Mead A. Wager TT, et al. Among authors: chandrasekaran ry. ACS Chem Neurosci. 2014 Dec 17;5(12):1253-65. doi: 10.1021/cn500201x. Epub 2014 Oct 28. ACS Chem Neurosci. 2014. PMID: 25299732 Clinical Trial.
Csnk1e is a genetic regulator of sensitivity to psychostimulants and opioids.
Bryant CD, Parker CC, Zhou L, Olker C, Chandrasekaran RY, Wager TT, Bolivar VJ, Loudon AS, Vitaterna MH, Turek FW, Palmer AA. Bryant CD, et al. Among authors: chandrasekaran ry. Neuropsychopharmacology. 2012 Mar;37(4):1026-35. doi: 10.1038/npp.2011.287. Epub 2011 Nov 16. Neuropsychopharmacology. 2012. PMID: 22089318 Free PMC article.