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Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor Butler, Christopher R.; Popiolek, Michael; McAllister, Laura A.; LaChapelle, Erik A.; Kramer, Melissa; Beck, Elizabeth M.; Mente, Scot; Brodney, Michael A.; Brown, Matthew; Gilbert, Adam; Helal, Chris; Ogilvie, Kevin; Starr, Jeremy; Uccello, Daniel; Grimwood, Sarah; Edgerton, Jeremy; Garst-Orozko, Jonathan; Kozak, Rouba; Lotarski, Susan; Rossi, Amie; Smith, Deborah; O'Connor, Rebecca; Lazzaro, John; Steppan, Claire; Steyn, Stefanus J. 分享 收藏
Target occupancy study and whole-body dosimetry with a MAGL PET ligand [11C]PF-06809247 in non-human primates Arakawa, Ryosuke; Takano, Akihiro; Nag, Sangram; Jia, Zhisheng; Amini, Nahid; Maresca, Kevin P.; Zhang, Lei; Keliher, Edmund J.; Butler, Christopher R.; Piro, Justin R.; Samad, Tarek A.; Smith, Deborah; Nason, Deane; O'Neil, Steve; Trapa, Patrick; Fonseca, Kari R.; Litchfield, John; McCarthy, Timothy; Carson, Richard E.; Halldin, Christer 分享 收藏
Identification and Development of an Irreversible Monoacylglycerol Lipase (MAGL) Positron Emission Tomography (PET) Radioligand with High Specificity 具有高特异性的不可逆单酰基甘油脂肪酶 (MAGL) 正电子发射断层扫描 (PET) 放射性配体的鉴定和开发 Zhang, Lei; Butler, Christopher R.; Maresca, Kevin P.; Takano, Akihiro; Nag, Sangram; Jia, Zhisheng; Arakawa, Ryosuke; Piro, Justin R.; Samad, Tarek; Smith, Deborah L.; Nason, Deane M.; O'Neil, Steven; McAllister, Laura; Schildknegt, Klaas; Trapa, Patrick; McCarthy, Timothy J.; Villalobos, Anabella; Halldin, Christer 分享 收藏
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. 分享 收藏
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Discovery and Preclinical Characterization of 1-Methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator Zhang, Lei; Balan, Gayatri; Barreiro, Gabriela; Boscoe, Brian P.; Chenard, Lois K.; Cianfrogna, Julie; Claffey, Michelle M.; Chen, Laigao; Coffman, Karen J.; Drozda, Susan E.; Dunetz, Joshua R.; Fonseca, Kari R.; Galatsis, Paul; Grimwood, Sarah; Lazzaro, John T.; Mancuso, Jessica Y.; Miller, Emily L.; Reese, Matthew R.; Rogers, Bruce N.; Sakurada, Isao; Skaddan, Marc; Smith, Deborah L.; Stepan, Antonia F.; Trapa, Patrick; Tuttle, Jamison B.; Verhoest, Patrick R.; Walker, Daniel P.; Wright, Ann S.; Zaleska, Margaret M.; Zasadny, Kenneth; Shaffer, Christopher L. 分享 收藏
Negative Allosteric Modulation of the mGluR5 Receptor Reduces Repetitive Behaviors and Rescues Social Deficits in Mouse Models of Autism Silverman, Jill L.; Smith, Daniel G.; Rizzo, Stacey J. Sukoff; Karras, Michael N.; Turner, Sarah M.; Tolu, Seda S.; Bryce, Dianne K.; Smith, Deborah L.; Fonseca, Kari; Ring, Robert H.; Crawley, Jacqueline N. 分享 收藏
The Metabotropic Glutamate Receptor 7 Allosteric Modulator AMN082: A Monoaminergic Agent in Disguise? Rizzo, Stacey J. Sukoff; Leonard, Sarah K.; Gilbert, Adam; Dollings, Paul; Smith, Deborah L.; Zhang, Mei-Yi; Di, Li; Platt, Brian J.; Neal, Sarah; Dwyer, Jason M.; Bender, Corey N.; Zhang, Jean; Lock, Tim; Kowal, Dianne; Kramer, Angela; Randall, Andrew; Huselton, Christine; Vishwanathan, Karthick; Tse, Susanna Y.; Butera, John; Ring, Robert H.; Rosenzweig-Lipson, Sharon; Hughes, Zoe A.; Dunlop, John 分享 收藏
Characterization of Vabicaserin (SCA-136), a Selective 5-Hydroxytryptamine 2C Receptor Agonist Dunlop, John; Watts, Stephanie W.; Barrett, James E.; Coupet, Joseph; Harrison, Boyd; Mazandarani, Hossein; Nawoschik, Stanley; Pangalos, Menelas N.; Ramamoorthy, Siva; Schechter, Lee; Smith, Deborah; Stack, Gary; Zhang, Jean; Zhang, Guoming; Rosenzweig-Lipson, Sharon 分享 收藏
Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT6 antagonists Liu, Kevin G.; Robichaud, Albert J.; Greenfield, Alexander A.; Lo, Jennifer R.; Grosanu, Cristina; Mattes, James F.; Cai, Yanxuan; Zhang, Guo Ming; Zhang, Jean Y.; Kowal, Dianne M.; Smith, Deborah L.; Di, Li; Kerns, Edward H.; Schechter, Lee E.; Comery, Thomas A. 分享 收藏
5-Piperazinyl-3-sulfonylindazoles as Potent and Selective 5-Hydroxytryptamine-6 Antagonists Liu, Kevin G.; Robichaud, Albert J.; Bernotas, Ronald C.; Yan, Yinfa; Lo, Jennifer R.; Zhang, Mei-Yi; Hughes, Zoe A.; Huselton, Christine; Zhang, Guo Ming; Zhang, Jean Y.; Kowal, Dianne M.; Smith, Deborah L.; Schechter, Lee E.; Comery, Thomas A. 分享 收藏
5-Cyclic Amine-3-arylsulfonylindazoles as Novel 5-HT6 Receptor Antagonists Haydar, Simon N.; Yun, Heedong; Andrae, Patrick M.; Mattes, James; Zhang, Jean; Kramer, Angela; Smith, Deborah L.; Huselton, Christine; Graf, Radka; Aschmies, Suzan; Schechter, Lee E.; Comery, Thomas A.; Robichaud, Albert J. 分享 收藏
WS-50030 [7-{4-[3-(1H-inden-3-yl)propyl]piperazin-1-yl}-1,3-benzoxazol-2(3H)-one]: A Novel Dopamine D2 Receptor Partial Agonist/Serotonin Reuptake Inhibitor with Preclinical Antipsychotic-Like and Antidepressant-Like Activity Brennan, Julie A.; Graf, Radka; Grauer, Steven M.; Navarra, Rachel L.; Pulicicchio, Claudine M.; Hughes, Zoe A.; Lin, Qian; Wantuch, Caitlin; Rosenzweig-Lipson, Sharon; Pruthi, Farhana; Lai, Margaret; Smith, Deborah; Goutier, Wouter; van de Neut, Martina; Robichaud, Albert J.; Rotella, David; Feenstra, Rolf W.; Kruse, Chris; Broqua, Pierre; Beyer, Chad E.; McCreary, Andrew C.; Pausch, Mark H.; Marquis, Karen L. 分享 收藏
Synthesis, Potency, and in Vivo Evaluation of 2-Piperazin-1-ylquinoline Analogues as Dual Serotonin Reuptake Inhibitors and Serotonin 5-HT1A Receptor Antagonists Zhou, Dahui; Stack, Gary P.; Lo, Jennifer; Failli, Amedeo A.; Evrard, Deborah A.; Harrison, Boyd L.; Hatzenbuhler, Nicole T.; Tran, Megan; Croce, Susan; Yi, Soo; Golembieski, Jeannette; Hornby, Geoffrey A.; Lai, Margaret; Lin, Qian; Schechter, Lee E.; Smith, Deborah L.; Shilling, Adam D.; Huselton, Christine; Mitchell, Paul; Beyer, Chad E.; Andree, Terrance H. 分享 收藏
Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT6 agonists Bernotas, Ronald C.; Lenicek, Steven; Antane, Schuyler; Cole, Derek C.; Harrison, Boyd L.; Robichaud, Albert J.; Zhang, Guo Ming; Smith, Deborah; Platt, Brian; Lin, Qian; Li, Ping; Coupet, Joseph; Rosenzweig-Lipson, Sharon; Beyer, Chad E.; Schechter, Lee E. 分享 收藏
ADX47273 [S-(4-Fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: A Novel Metabotropic Glutamate Receptor 5-Selective Positive Allosteric Modulator with Preclinical Antipsychotic-Like and Procognitive Activities Liu, Feng; Grauer, Steve; Kelley, Cody; Navarra, Rachel; Graf, Radka; Zhang, Guoming; Atkinson, Peter J.; Popiolek, Michael; Wantuch, Caitlin; Khawaja, Xavier; Smith, Deborah; Olsen, Michael; Kouranova, Evguenia; Lai, Margaret; Pruthi, Farhana; Pulicicchio, Claudine; Day, Mark; Gilbert, Adam; Pausch, Mark H.; Brandon, Nicholas J.; Beyer, Chad E.; Comery, Tom A.; Logue, Sheree; Rosenzweig-Lipson, Sharon; Marquis, Karen L. 分享 收藏
Advances toward New Antidepressants with Dual Serotonin Transporter and 5-HT1A Receptor Affinity within a Class of 3-Aminochroman Derivatives. Part 2 Hatzenbuhler, Nicole T.; Baudy, Reinhardt; Evrard, Deborah A.; Failli, Amedeo; Harrison, Boyd L.; Lenicek, Steven; Mewshaw, Richard E.; Saab, Annmarie; Shao, Uresh; Sze, Jean; Zhang, Minsheng; Zhou, Dahui; Chlenov, Michael; Kagan, Michael; Golembieski, Jeannette; Hornby, Geoffrey; Lai, Margaret; Smith, Deborah L.; Sullivan, Kelly M.; Schechter, Lee E.; Andree, Terrance H. 分享 收藏
Studies toward the discovery of the next generation of antidepressants.: Part 6:: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives Zhou, Dahui; Zhou, Ping; Evrard, Deborah A.; Meagher, Kristin; Webb, Michael; Harrison, Boyd L.; Huryn, Donna M.; Golembieski, Jeannette; Hornby, Geoffrey A.; Schechter, Lee E.; Smith, Deborah L.; Andree, Terrance H.; Mewshaw, Richard E. 分享 收藏
Correlating efficacy in rodent cognition models with in vivo 5-hydroxytryptamine1A receptor occupancy by a novel antagonist, (R)-N-(2-methyl-(4-indolyl-1-piperazinyl)ethyl)-N-(2-pyridinyl)-cyclohexane carboxamide (WAY-101405) Hirst, Warren D.; Andree, Terrance H.; Aschmies, Suzan; Childers, Wayne E.; Comery, Thomas A.; Dawson, Lee A.; Day, Mark; Feingold, Irene B.; Grauer, Steven M.; Harrison, Boyd L.; Hughes, Zoe A.; Kao, John; Kelly, Michael G.; van der Lee, Heidi; Rosenzweig-Lipson, Sharon; Saab, Annmarie L.; Smith, Deborah L.; Sullivan, Kelly; Rizzo, Stacey J. Sukoff; Tio, Cesario; Zhang, Mei-Yi; Schechter, Lee E. 分享 收藏
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