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Page 1
Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects.
Davoren JE, Lee CW, Garnsey M, Brodney MA, Cordes J, Dlugolenski K, Edgerton JR, Harris AR, Helal CJ, Jenkinson S, Kauffman GW, Kenakin TP, Lazzaro JT, Lotarski SM, Mao Y, Nason DM, Northcott C, Nottebaum L, O'Neil SV, Pettersen B, Popiolek M, Reinhart V, Salomon-Ferrer R, Steyn SJ, Webb D, Zhang L, Grimwood S. Davoren JE, et al. Among authors: lotarski sm. J Med Chem. 2016 Jul 14;59(13):6313-28. doi: 10.1021/acs.jmedchem.6b00544. Epub 2016 Jul 1. J Med Chem. 2016. PMID: 27275946
Positive allosteric modulation of AMPA receptors from efficacy to toxicity: the interspecies exposure-response continuum of the novel potentiator PF-4778574.
Shaffer CL, Hurst RS, Scialis RJ, Osgood SM, Bryce DK, Hoffmann WE, Lazzaro JT, Hanks AN, Lotarski S, Weber ML, Liu J, Menniti FS, Schmidt CJ, Hajós M. Shaffer CL, et al. Among authors: lotarski s. J Pharmacol Exp Ther. 2013 Oct;347(1):212-24. doi: 10.1124/jpet.113.204735. Epub 2013 Jul 30. J Pharmacol Exp Ther. 2013. PMID: 23899905
The discovery and characterization of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor potentiator N-{(3S,4S)-4-[4-(5-cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242).
Shaffer CL, Patel NC, Schwarz J, Scialis RJ, Wei Y, Hou XJ, Xie L, Karki K, Bryce DK, Osgood SM, Hoffmann WE, Lazzaro JT, Chang C, McGinnis DF, Lotarski SM, Liu J, Obach RS, Weber ML, Chen L, Zasadny KR, Seymour PA, Schmidt CJ, Hajós M, Hurst RS, Pandit J, O'Donnell CJ. Shaffer CL, et al. Among authors: lotarski sm. J Med Chem. 2015 May 28;58(10):4291-308. doi: 10.1021/acs.jmedchem.5b00300. Epub 2015 May 14. J Med Chem. 2015. PMID: 25905800
Design and optimization of selective azaindole amide M1 positive allosteric modulators.
Davoren JE, O'Neil SV, Anderson DP, Brodney MA, Chenard L, Dlugolenski K, Edgerton JR, Green M, Garnsey M, Grimwood S, Harris AR, Kauffman GW, LaChapelle E, Lazzaro JT, Lee CW, Lotarski SM, Nason DM, Obach RS, Reinhart V, Salomon-Ferrer R, Steyn SJ, Webb D, Yan J, Zhang L. Davoren JE, et al. Among authors: lotarski sm. Bioorg Med Chem Lett. 2016 Jan 15;26(2):650-655. doi: 10.1016/j.bmcl.2015.11.053. Epub 2015 Nov 17. Bioorg Med Chem Lett. 2016. PMID: 26631313
Design and Synthesis of γ- and δ-Lactam M1 Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M1-Selective PAM with Weak Agonist Activity.
Davoren JE, Garnsey M, Pettersen B, Brodney MA, Edgerton JR, Fortin JP, Grimwood S, Harris AR, Jenkinson S, Kenakin T, Lazzaro JT, Lee CW, Lotarski SM, Nottebaum L, O'Neil SV, Popiolek M, Ramsey S, Steyn SJ, Thorn CA, Zhang L, Webb D. Davoren JE, et al. Among authors: lotarski sm. J Med Chem. 2017 Aug 10;60(15):6649-6663. doi: 10.1021/acs.jmedchem.7b00597. Epub 2017 Jul 26. J Med Chem. 2017. PMID: 28598634
In Vivo Modulation of Hippocampal Excitability by M4 Muscarinic Acetylcholine Receptor Activator: Implications for Treatment of Alzheimer's Disease and Schizophrenic Patients.
Popiolek M, Mandelblat-Cerf Y, Young D, Garst-Orozco J, Lotarski SM, Stark E, Kramer M, Butler CR, Kozak R. Popiolek M, et al. Among authors: lotarski sm. ACS Chem Neurosci. 2019 Mar 20;10(3):1091-1098. doi: 10.1021/acschemneuro.8b00496. Epub 2018 Oct 26. ACS Chem Neurosci. 2019. PMID: 30335349
Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor.
Butler CR, Popiolek M, McAllister LA, LaChapelle EA, Kramer M, Beck EM, Mente S, Brodney MA, Brown M, Gilbert A, Helal C, Ogilvie K, Starr J, Uccello D, Grimwood S, Edgerton J, Garst-Orozco J, Kozak R, Lotarski S, Rossi A, Smith D, O'Connor R, Lazzaro J, Steppan C, Steyn SJ. Butler CR, et al. J Med Chem. 2024 Jul 11;67(13):10831-10847. doi: 10.1021/acs.jmedchem.4c00293. Epub 2024 Jun 18. J Med Chem. 2024. PMID: 38888621
(S)-4-Methyl-2-(methylamino)pentanoic acid [4, 4-bis(4-fluorophenyl)butyl]amide hydrochloride, a novel calcium channel antagonist, is efficacious in several animal models of pain.
Song Y, Bowersox SS, Connor DT, Dooley DJ, Lotarski SM, Malone T, Miljanich G, Millerman E, Rafferty MF, Rock D, Roth BD, Schmidt J, Stoehr S, Szoke BG, Taylor C, Vartanian M, Wang YX. Song Y, et al. Among authors: lotarski sm. J Med Chem. 2000 Sep 21;43(19):3474-7. doi: 10.1021/jm000134n. J Med Chem. 2000. PMID: 11000000 No abstract available.
26 results