The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging
Zhang, Lei, Chen, Laigao, Beck, Elizabeth M, Chappie, Thomas A, Coelho, Richard V, Doran, Shawn D, Fan, Kuo-Hsien, Helal, Christopher J, Humphrey, John M, Hughes, Zoe, Kuszpit, Kyle, Lachapelle, Erik A, Lazzaro, John T, Lee, Chewah, Mather, Robert J, Patel, Nandini C, Skaddan, Marc B, Sciabola, Simone, Verhoest, Patrick R, Young, Joseph M, Zasadny, Kenneth, Villalobos, Anabella
Published in Journal of medicinal chemistry (26.10.2017)
Published in Journal of medicinal chemistry (26.10.2017)
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Journal Article
Positive allosteric modulation of AMPA receptors from efficacy to toxicity: the interspecies exposure-response continuum of the novel potentiator PF-4778574
Shaffer, Christopher L, Hurst, Raymond S, Scialis, Renato J, Osgood, Sarah M, Bryce, Dianne K, Hoffmann, William E, Lazzaro, John T, Hanks, Ashley N, Lotarski, Susan, Weber, Mark L, Liu, JianHua, Menniti, Frank S, Schmidt, Christopher J, Hajós, Mihály
Published in The Journal of pharmacology and experimental therapeutics (01.10.2013)
Published in The Journal of pharmacology and experimental therapeutics (01.10.2013)
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Journal Article
Striatal, Hippocampal, and Cortical Networks Are Differentially Responsive to the M4- and M1-Muscarinic Acetylcholine Receptor Mediated Effects of Xanomeline
Thorn, Catherine A, Moon, Joshua, Bourbonais, Clinton A, Harms, John, Edgerton, Jeremy R, Stark, Eda, Steyn, Stefanus J, Butter, Christopher R, Lazzaro, John T, O’Connor, Rebecca E, Popiolek, Michael
Published in ACS chemical neuroscience (20.03.2019)
Published in ACS chemical neuroscience (20.03.2019)
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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, Jennifer E, Lee, Che-Wah, Garnsey, Michelle, Brodney, Michael A, Cordes, Jason, Dlugolenski, Keith, Edgerton, Jeremy R, Harris, Anthony R, Helal, Christopher J, Jenkinson, Stephen, Kauffman, Gregory W, Kenakin, Terrence P, Lazzaro, John T, Lotarski, Susan M, Mao, Yuxia, Nason, Deane M, Northcott, Carrie, Nottebaum, Lisa, O’Neil, Steven V, Pettersen, Betty, Popiolek, Michael, Reinhart, Veronica, Salomon-Ferrer, Romelia, Steyn, Stefanus J, Webb, Damien, Zhang, Lei, Grimwood, Sarah
Published in Journal of medicinal chemistry (14.07.2016)
Published in Journal of medicinal chemistry (14.07.2016)
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Journal Article
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, Jennifer E, Garnsey, Michelle, Pettersen, Betty, Brodney, Michael A, Edgerton, Jeremy R, Fortin, Jean-Philippe, Grimwood, Sarah, Harris, Anthony R, Jenkinson, Stephen, Kenakin, Terry, Lazzaro, John T, Lee, Che-Wah, Lotarski, Susan M, Nottebaum, Lisa, O’Neil, Steven V, Popiolek, Michael, Ramsey, Simeon, Steyn, Stefanus J, Thorn, Catherine A, Zhang, Lei, Webb, Damien
Published in Journal of medicinal chemistry (10.08.2017)
Published in Journal of medicinal chemistry (10.08.2017)
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Journal Article
3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization
Duplantier, Allen J., Efremov, Ivan, Candler, John, Doran, Angela C., Ganong, Alan H., Haas, Jessica A., Hanks, Ashley N., Kraus, Kenneth G., Lazzaro, John T., Lu, Jiemin, Maklad, Noha, McCarthy, Sheryl A., O’Sullivan, Theresa J., Rogers, Bruce N., Siuciak, Judith A., Spracklin, Douglas K., Zhang, Lei
Published in Bioorganic & medicinal chemistry letters (01.05.2009)
Published in Bioorganic & medicinal chemistry letters (01.05.2009)
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Journal Article
3-(Imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: A novel series of mGluR2 positive allosteric modulators
Zhang, Lei, Rogers, Bruce N., Duplantier, Allen J., McHardy, Stanley F., Efremov, Ivan, Berke, Helen, Qian, Weimin, Zhang, Andy Q., Maklad, Noha, Candler, John, Doran, Angela C., Lazzaro, John T., Ganong, Alan H.
Published in Bioorganic & medicinal chemistry (15.10.2008)
Published in Bioorganic & medicinal chemistry (15.10.2008)
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Journal Article
Harnessing biosynthesis and quantitative NMR for late stage functionalization of lead molecules: Application to the M1 positive allosteric modulator (PAM) program
Brodney, Michael A., Sharma, Raman, Lazzaro, John T., Walker, Gregory S., Scott Obach, R.
Published in Bioorganic & medicinal chemistry letters (15.06.2018)
Published in Bioorganic & medicinal chemistry letters (15.06.2018)
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Journal Article
Synthesis of Novel Pyrrolo[3,4-d]pyrazole-dicarboxylic Acids and Evaluation of Their Interaction with Glutamate Receptors
Conti, Paola, di Ventimiglia, Samuele Joppolo, Pinto, Andrea, Tamborini, Lucia, Menniti, Frank S., Lazzaro, John T., De Micheli, Carlo
Published in Chemistry & biodiversity (01.04.2008)
Published in Chemistry & biodiversity (01.04.2008)
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Journal Article
Characterization of a Novel M1 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator Radioligand, [3H]PT-1284
Smith, Deborah L, Davoren, Jennifer E, Edgerton, Jeremy R, Lazzaro, John T, Lee, Che-Wah, Neal, Sarah, Zhang, Lei, Grimwood, Sarah
Published in Molecular pharmacology (01.09.2016)
Published in Molecular pharmacology (01.09.2016)
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Journal Article
Striatal, Hippocampal, and Cortical Networks Are Differentially Responsive to the M4- and M1-Muscarinic Acetylcholine Receptor Mediated Effects of Xanomeline
Thorn, Catherine A, Moon, Joshua, Bourbonais, Clinton A, Harms, John, Edgerton, Jeremy R, Stark, Eda, Steyn, Stefanus J, Butler, Christopher R, Lazzaro, John T, O’Connor, Rebecca E, Popiolek, Michael
Published in ACS chemical neuroscience (21.08.2019)
Published in ACS chemical neuroscience (21.08.2019)
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Journal Article
Design and optimization of selective azaindole amide M1 positive allosteric modulators
Davoren, Jennifer E., O’Neil, Steven V., Anderson, Dennis P., Brodney, Michael A., Chenard, Lois, Dlugolenski, Keith, Edgerton, Jeremy R., Green, Michael, Garnsey, Michelle, Grimwood, Sarah, Harris, Anthony R., Kauffman, Gregory W., LaChapelle, Erik, Lazzaro, John T., Lee, Che-Wah, Lotarski, Susan M., Nason, Deane M., Obach, R. Scott, Reinhart, Veronica, Salomon-Ferrer, Romelia, Steyn, Stefanus J., Webb, Damien, Yan, Jiangli, Zhang, Lei
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
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Journal Article
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, Christopher L, Patel, Nandini C, Schwarz, Jacob, Scialis, Renato J, Wei, Yunjing, Hou, Xinjun J, Xie, Longfei, Karki, Kapil, Bryce, Dianne K, Osgood, Sarah M, Hoffmann, William E, Lazzaro, John T, Chang, Cheng, McGinnis, Dina F, Lotarski, Susan M, Liu, JianHua, Obach, R. Scott, Weber, Mark L, Chen, Laigao, Zasadny, Kenneth R, Seymour, Patricia A, Schmidt, Christopher J, Hajós, Mihály, Hurst, Raymond S, Pandit, Jayvardhan, O’Donnell, Christopher J
Published in Journal of medicinal chemistry (28.05.2015)
Published in Journal of medicinal chemistry (28.05.2015)
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Journal Article
Discovery of Selective M4 Muscarinic Acetylcholine Receptor Agonists with Novel Carbamate Isosteres
Yang, Qingyi, Lachapelle, Erik A, Kablaoui, Natasha M, Webb, Damien, Popiolek, Michael, Grimwood, Sarah, Kozak, Rouba, O’Connor, Rebecca E, Lazzaro, John T, Butler, Christopher R, Zhang, Lei
Published in ACS medicinal chemistry letters (13.06.2019)
Published in ACS medicinal chemistry letters (13.06.2019)
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Journal Article
Design and Synthesis of γ- and δ-Lactam M 1 Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M 1 -Selective PAM with Weak Agonist Activity
Davoren, Jennifer E, Garnsey, Michelle, Pettersen, Betty, Brodney, Michael A, Edgerton, Jeremy R, Fortin, Jean-Philippe, Grimwood, Sarah, Harris, Anthony R, Jenkinson, Stephen, Kenakin, Terry, Lazzaro, John T, Lee, Che-Wah, Lotarski, Susan M, Nottebaum, Lisa, O'Neil, Steven V, Popiolek, Michael, Ramsey, Simeon, Steyn, Stefanus J, Thorn, Catherine A, Zhang, Lei, Webb, Damien
Published in Journal of medicinal chemistry (10.08.2017)
Published in Journal of medicinal chemistry (10.08.2017)
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Journal Article
Discovery and Characterization of (R)‑6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1‑c][1,4]oxazin-4(9H)‑one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates
Stepan, Antonia F, Claffey, Michelle M, Reese, Matthew R, Balan, Gayatri, Barreiro, Gabriela, Barricklow, Jason, Bohanon, Michael J, Boscoe, Brian P, Cappon, Gregg D, Chenard, Lois K, Cianfrogna, Julie, Chen, Laigao, Coffman, Karen J, Drozda, Susan E, Dunetz, Joshua R, Ghosh, Somraj, Hou, Xinjun, Houle, Christopher, Karki, Kapil, Lazzaro, John T, Mancuso, Jessica Y, Marcek, John M, Miller, Emily L, Moen, Mark A, O’Neil, Steven, Sakurada, Isao, Skaddan, Marc, Parikh, Vinod, Smith, Deborah L, Trapa, Patrick, Tuttle, Jamison B, Verhoest, Patrick R, Walker, Daniel P, Won, Annie, Wright, Ann S, Whritenour, Jessica, Zasadny, Kenneth, Zaleska, Margaret M, Zhang, Lei, Shaffer, Christopher L
Published in Journal of medicinal chemistry (28.09.2017)
Published in Journal of medicinal chemistry (28.09.2017)
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Journal Article
Discovery and Characterization of a Novel Dihydroisoxazole Class of α‑Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) Receptor Potentiators
Patel, Nandini C, Schwarz, Jacob, Hou, Xinjun J, Hoover, Dennis J, Xie, Longfei, Fliri, Anton J, Gallaschun, Randall J, Lazzaro, John T, Bryce, Dianne K, Hoffmann, William E, Hanks, Ashley N, McGinnis, Dina, Marr, Eric S, Gazard, Justin L, Hajós, Mihály, Scialis, Renato J, Hurst, Raymond S, Shaffer, Christopher L, Pandit, Jayvardhan, O’Donnell, Christopher J
Published in Journal of medicinal chemistry (27.11.2013)
Published in Journal of medicinal chemistry (27.11.2013)
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Journal Article
1-[(1-Methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines as mGluR2 Positive Allosteric Modulators for the Treatment of Psychosis
Zhang, Lei, Brodney, Michael A, Candler, John, Doran, Angela C, Duplantier, Allen J, Efremov, Ivan V, Evrard, Edel, Kraus, Kenneth, Ganong, Alan H, Haas, Jessica A, Hanks, Ashley N, Jenza, Keith, Lazzaro, John T, Maklad, Noha, McCarthy, Sheryl A, Qian, Weimin, Rogers, Bruce N, Rottas, Melinda D, Schmidt, Christopher J, Siuciak, Judith A, Tingley, F. David, Zhang, Andy Q
Published in Journal of medicinal chemistry (24.03.2011)
Published in Journal of medicinal chemistry (24.03.2011)
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Journal Article
Design and Synthesis of gamma- and delta-Lactarn M-1 Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M-1-Selective PAM with Weak Agonist Activity
Davoren, Jennifer E., Garney, Michelle, Pettersen, Betty, Brodney, Michael A., Edgerton, Jeremy R., Fortin, Jean-Philippe, Grimwood, Sarah, Harris, Anthony R., Jenkinson, Stephen, Kenakin, Terry, Lazzaro, John T., Lee, Che-Wah, Lotarski, Susan M., Nottebaum, Lisa, O'Neil, Steven V., Popiolek, Michael, Ramsey, Simeon, Steyn, Stefanus J., Thorn, Catherine A., Zhang, Lei, Webb, Damien
Published in Journal of medicinal chemistry (10.08.2017)
Published in Journal of medicinal chemistry (10.08.2017)
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Journal Article
Design and optimization of selective azaindole amide M-1 positive allosteric modulators
Davoren, Jennifer E., O'Neil, Steven V., Anderson, Dennis P., Brodney, Michael A., Chenard, Lois, Dlugolenski, Keith, Edgerton, Jeremy R., Green, Michael, Garnsey, Michelle, Grimwood, Sarah, Harris, Anthony R., Kauffman, Gregory W., LaChapelle, Erik, Lazzaro, John T., Lee, Che-Wah, Lotarski, Susan M., Nason, Deane M., Obach, R. Scott, Reinhart, Veronica, Salomon-Ferrer, Romelia, Steyn, Stefanus J., Webba, Damien, Yan, Jiangli, Zhang, Lei
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
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Journal Article