Forebrain-selective AMPA-receptor antagonism guided by TARP γ-8 as an antiepileptic mechanism
Kato, Akihiko S, Burris, Kevin D, Gardinier, Kevin M, Gernert, Douglas L, Porter, Warren J, Reel, Jon, Ding, Chunjin, Tu, Yuan, Schober, Douglas A, Lee, Matthew R, Heinz, Beverly A, Fitch, Thomas E, Gleason, Scott D, Catlow, John T, Yu, Hong, Fitzjohn, Stephen M, Pasqui, Francesca, Wang, He, Qian, Yuewei, Sher, Emanuele, Zwart, Ruud, Wafford, Keith A, Rasmussen, Kurt, Ornstein, Paul L, Isaac, John T R, Nisenbaum, Eric S, Bredt, David S, Witkin, Jeffrey M
Published in Nature medicine (01.12.2016)
Published in Nature medicine (01.12.2016)
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Synthesis and Pharmacological Characterization of C4-Disubstituted Analogs of 1S,2S,5R,6S‑2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylate: Identification of a Potent, Selective Metabotropic Glutamate Receptor Agonist and Determination of Agonist-Bound Human mGlu2 and mGlu3 Amino Terminal Domain Structures
Monn, James A, Prieto, Lourdes, Taboada, Lorena, Pedregal, Concepcion, Hao, Junliang, Reinhard, Matt R, Henry, Steven S, Goldsmith, Paul J, Beadle, Christopher D, Walton, Lesley, Man, Teresa, Rudyk, Helene, Clark, Barry, Tupper, David, Baker, S. Richard, Lamas, Carlos, Montero, Carlos, Marcos, Alicia, Blanco, Jaime, Bures, Mark, Clawson, David K, Atwell, Shane, Lu, Frances, Wang, Jing, Russell, Marijane, Heinz, Beverly A, Wang, Xushan, Carter, Joan H, Xiang, Chuanxi, Catlow, John T, Swanson, Steven, Sanger, Helen, Broad, Lisa M, Johnson, Michael P, Knopp, Kelly L, Simmons, Rosa M. A, Johnson, Bryan G, Shaw, David B, McKinzie, David L
Published in Journal of medicinal chemistry (26.02.2015)
Published in Journal of medicinal chemistry (26.02.2015)
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Synthesis and Pharmacological Characterization of C4‑(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)‑2-Amino-4-(1H‑1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812223), a Highly Potent, Functionally Selective mGlu2 Receptor Agonist
Monn, James A, Prieto, Lourdes, Taboada, Lorena, Hao, Junliang, Reinhard, Matthew R, Henry, Steven S, Beadle, Christopher D, Walton, Lesley, Man, Teresa, Rudyk, Helene, Clark, Barry, Tupper, David, Baker, S. Richard, Lamas, Carlos, Montero, Carlos, Marcos, Alicia, Blanco, Jaime, Bures, Mark, Clawson, David K, Atwell, Shane, Lu, Frances, Wang, Jing, Russell, Marijane, Heinz, Beverly A, Wang, Xushan, Carter, Joan H, Getman, Brian G, Catlow, John T, Swanson, Steven, Johnson, Bryan G, Shaw, David B, McKinzie, David L
Published in Journal of medicinal chemistry (24.09.2015)
Published in Journal of medicinal chemistry (24.09.2015)
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Synthesis and Pharmacological Characterization of C4 β -Amide-Substituted 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1 S,2 S,4 S,5 R,6 S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2794193), a Highly Potent and Selective mGlu 3 Receptor Agonist
Monn, James A, Henry, Steven S, Massey, Steven M, Clawson, David K, Chen, Qi, Diseroad, Benjamin A, Bhardwaj, Rajni M, Atwell, Shane, Lu, Frances, Wang, Jing, Russell, Marijane, Heinz, Beverly A, Wang, Xu-Shan, Carter, Joan H, Getman, Brian G, Adragni, Kofi, Broad, Lisa M, Sanger, Helene E, Ursu, Daniel, Catlow, John T, Swanson, Steven, Johnson, Bryan G, Shaw, David B, McKinzie, David L, Hao, Junliang
Published in Journal of medicinal chemistry (22.03.2018)
Published in Journal of medicinal chemistry (22.03.2018)
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Further Evaluation of Mechanisms Associated with the Antidepressantlike Signature of Scopolamine in Mice
Martin, Anna E, Schober, Douglas A, Nikolayev, Alexander, Tolstikov, Vladimir V, Anderson, Wesley H, Higgs, Richard E, Kuo, Ming-Shang, Laksmanan, Anastasia, Catlow, John T, Li, Xia, Felder, Christian C, Witkin, Jeffrey M
Published in CNS & neurological disorders drug targets (01.01.2017)
Published in CNS & neurological disorders drug targets (01.01.2017)
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Discovery of (1S,2R,3S,4S,5R,6R)‑2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity
Chappell, Mark D, Li, Renhua, Smith, Stephon C, Dressman, Bruce A, Tromiczak, Eric G, Tripp, Allie E, Blanco, Maria-Jesus, Vetman, Tatiana, Quimby, Steven J, Matt, James, Britton, Thomas C, Fivush, Adam M, Schkeryantz, Jeffrey M, Mayhugh, Daniel, Erickson, Jon A, Bures, Mark G, Jaramillo, Carlos, Carpintero, Mercedes, Diego, José Eugenio de, Barberis, Mario, Garcia-Cerrada, Susana, Soriano, José F, Antonysamy, Stephen, Atwell, Shane, MacEwan, Iain, Condon, Bradley, Sougias, Christine, Wang, Jing, Zhang, Aiping, Conners, Kris, Groshong, Chris, Wasserman, Stephen R, Koss, John W, Witkin, Jeffrey M, Li, Xia, Overshiner, Carl, Wafford, Keith A, Seidel, Wesley, Wang, Xu-Shan, Heinz, Beverly A, Swanson, Steven, Catlow, John T, Bedwell, David W, Monn, James A, Mitch, Charles H, Ornstein, Paul L
Published in Journal of medicinal chemistry (22.12.2016)
Published in Journal of medicinal chemistry (22.12.2016)
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Targeted Blockade of TARP-γ8-Associated AMPA Receptors: Anticonvulsant Activity with the Selective Antagonist LY3130481 (CERC-611)
Witkin, Jeffrey M, Schober, Douglas A, Gleason, Scott D, Catlow, John T, Porter, Warren J, Reel, Jon, Jin, Xiaoming, Hobbs, Jonathan, Gehlert, Donald, Gernert, Douglas L, Gardinier, Kevin M, Kato, Akihiko S, Ping, Xingjie, Smith, Jodi L
Published in CNS & neurological disorders drug targets (01.12.2017)
Published in CNS & neurological disorders drug targets (01.12.2017)
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N-(4-((2-(trifluoromethyl)-3-hydroxy-4-(isobutyryl)phenoxy)methyl)benzyl)-1-methyl-1H-imidazole-4-carboxamide (THIIC), a novel metabotropic glutamate 2 potentiator with potential anxiolytic/antidepressant properties: in vivo profiling suggests a link between behavioral and central nervous system neurochemical changes
Fell, Matthew J, Witkin, Jeffrey M, Falcone, Julie F, Katner, Jason S, Perry, Kenneth W, Hart, John, Rorick-Kehn, Linda, Overshiner, Carl D, Rasmussen, Kurt, Chaney, Stephen F, Benvenga, Mark J, Li, Xia, Marlow, Deanna L, Thompson, Linda K, Luecke, Susan K, Wafford, Keith A, Seidel, Wesley F, Edgar, Dale M, Quets, Anne T, Felder, Christian C, Wang, XuShan, Heinz, Beverly A, Nikolayev, Alexander, Kuo, Ming-Shang, Mayhugh, Daniel, Khilevich, Albert, Zhang, Deyi, Ebert, Philip J, Eckstein, James A, Ackermann, Bradley L, Swanson, Steven P, Catlow, John T, Dean, Robert A, Jackson, Kimberley, Tauscher-Wisniewski, Sitra, Marek, Gerard J, Schkeryantz, Jeffrey M, Svensson, Kjell A
Published in The Journal of pharmacology and experimental therapeutics (01.01.2011)
Published in The Journal of pharmacology and experimental therapeutics (01.01.2011)
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Further evaluation of the neuropharmacological determinants of the antidepressant-like effects of curcumin
Witkin, Jeffrey M, Leucke, Susan, Thompson, Linda K, Lynch, Renee A, Ding, Chunjin, Heinz, Beverly, Catlow, John T, Gleason, Scott D, Li, Xia
Published in CNS & neurological disorders drug targets (01.06.2013)
Published in CNS & neurological disorders drug targets (01.06.2013)
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Pharmacological and Pharmacokinetic Properties of a Structurally Novel, Potent, and Selective Metabotropic Glutamate 2/3 Receptor Agonist: In Vitro Characterization of Agonist (â)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic Acid (LY404039)
Rorick-Kehn, Linda M, Johnson, Bryan G, Burkey, Jennifer L, Wright, Rebecca A, Calligaro, David O, Marek, Gerard J, Nisenbaum, Eric S, Catlow, John T, Kingston, Ann E, Giera, Deborah D, Herin, Marc F, Monn, James A, McKinzie, David L, Schoepp, Darryle D
Published in The Journal of pharmacology and experimental therapeutics (01.04.2007)
Published in The Journal of pharmacology and experimental therapeutics (01.04.2007)
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Synthesis and Pharmacological Characterization of 4‑Substituted-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates: Identification of New Potent and Selective Metabotropic Glutamate 2/3 Receptor Agonists
Monn, James A, Valli, Matthew J, Massey, Steven M, Hao, Junliang, Reinhard, Matthew R, Bures, Mark G, Heinz, Beverly A, Wang, Xushan, Carter, Joan H, Getman, Brian G, Stephenson, Gregory A, Herin, Marc, Catlow, John T, Swanson, Steven, Johnson, Bryan G, McKinzie, David L, Henry, Steven S
Published in Journal of medicinal chemistry (13.06.2013)
Published in Journal of medicinal chemistry (13.06.2013)
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Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression
Dressman, Bruce A., Tromiczak, Eric G., Chappell, Mark D., Tripp, Allie E., Quimby, Steven J., Vetman, Tatiana, Fivush, Adam M., Matt, James, Jaramillo, Carlos, Li, Renhua, Khilevich, Albert, Blanco, Maria-Jesus, Smith, Stephon C., Carpintero, Mercedes, de Diego, José Eugenio, Barberis, Mario, García-Cerrada, Susana, Soriano, José F., Schkeryantz, Jeffrey M., Witkin, Jeffrey M., Wafford, Keith A., Seidel, Wesley, Britton, Thomas, Overshiner, Carl D., Li, Xia, Wang, Xu-Shan, Heinz, Beverly A., Catlow, John T., Swanson, Steven, Bedwell, David, Ornstein, Paul L., Mitch, Charles H.
Published in Bioorganic & medicinal chemistry letters (01.12.2016)
Published in Bioorganic & medicinal chemistry letters (01.12.2016)
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In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu 2/3 receptor antagonist
Witkin, Jeffrey M, Ornstein, Paul L, Mitch, Charles H, Li, Renhua, Smith, Stephon C, Heinz, Beverly A, Wang, Xu-Shan, Xiang, Chuanxi, Carter, Joan H, Anderson, Wesley H, Li, Xia, Broad, Lisa M, Pasqui, Francesca, Fitzjohn, Stephen M, Sanger, Helen E, Smith, Jodi L, Catlow, John, Swanson, Steven, Monn, James A
Published in Neuropharmacology (01.03.2017)
Published in Neuropharmacology (01.03.2017)
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Preclinical findings predicting efficacy and side‐effect profile of LY2940094, an antagonist of nociceptin receptors
Witkin, Jeffrey M., Rorick‐Kehn, Linda M., Benvenga, Mark J., Adams, Benjamin L., Gleason, Scott D., Knitowski, Karen M., Li, Xia, Chaney, Steven, Falcone, Julie F., Smith, Janice W., Foss, Julie, Lloyd, Kirsti, Catlow, John T., McKinzie, David L., Svensson, Kjell A., Barth, Vanessa N., Toledo, Miguel A., Diaz, Nuria, Lafuente, Celia, Jiménez, Alma, Benito, Alfonso, Pedregal, Conception, Martínez‐Grau, Maria A., Post, Anke, Ansonoff, Michael A., Pintar, John E., Statnick, Michael A.
Published in Pharmacology research & perspectives (01.12.2016)
Published in Pharmacology research & perspectives (01.12.2016)
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Discovery of (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-yl)isothiazol-5-yl)-2-methylcyclopropanecarboxamide, a potent and orally efficacious mGlu5 receptor negative allosteric modulator
Hao, Junliang, Dehlinger, Veronique, Fivush, Adam M., Rudyk, Helene C.E., Britton, Thomas C., Hollinshead, Sean P., Vokits, Benjamin P., Clark, Barry P., Henry, Steven S., Massey, Steven M., Peng, Langu, Dressman, Bruce A., Heinz, Beverly A., Roberts, Edda F., Bracey-Walker, Mallorie R., Swanson, Steven, Catlow, John T., Love, Patrick L., Tepool, Anita D., Peters, Steven C., Simmons, Rosa Maria A., Iyengar, Smriti, McKinzie, David L., Monn, James A.
Published in Bioorganic & medicinal chemistry letters (01.03.2013)
Published in Bioorganic & medicinal chemistry letters (01.03.2013)
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Journal Article
Preclinical findings predicting efficacy and side‐effect profile of LY 2940094, an antagonist of nociceptin receptors
Witkin, Jeffrey M., Rorick‐Kehn, Linda M., Benvenga, Mark J., Adams, Benjamin L., Gleason, Scott D., Knitowski, Karen M., Li, Xia, Chaney, Steven, Falcone, Julie F., Smith, Janice W., Foss, Julie, Lloyd, Kirsti, Catlow, John T., McKinzie, David L., Svensson, Kjell A., Barth, Vanessa N., Toledo, Miguel A., Diaz, Nuria, Lafuente, Celia, Jiménez, Alma, Benito, Alfonso, Pedregal, Conception, Martínez‐Grau, Maria A., Post, Anke, Ansonoff, Michael A., Pintar, John E., Statnick, Michael A.
Published in Pharmacology research & perspectives (01.12.2016)
Published in Pharmacology research & perspectives (01.12.2016)
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Synthesis and Pharmacological Characterization of C4(beta)-Amide-Substituted 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1S,2S,4S,5R,6S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2794193), a Highly Potent and Selective mGlu3 Receptor Agonist
Monn, James A., Henry, Steven S., Massey, Steven M., Clawson, David K., Chen, Qi, Diseroad, Benjamin A., Bhardwaj, Rajni M., Atwel, Shane, Lu, Frances, Wang, Jing, Russell, Marijane, Heinz, Beverly A., Wang, Xu-shan, Carter, Joan H., Getman, Brian G., Adragni, Kofi, Broad, Lisa M., Sanger, Helene E., Ursu, Daniel, Catlow, John T., Swanson, Steven, Johnson, Bryan G., Shaw, David B., McKinzie, David L., Hao, Junliang
Published in Journal of medicinal chemistry (22.03.2018)
Published in Journal of medicinal chemistry (22.03.2018)
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Journal Article
Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812223), a Highly Potent, Functionally Selective mGlu(2) Receptor Agonist
Monn, James A., Prieto, Lourdes, Taboada, Lorena, Hao, Junliang, Reinhard, Matthew R., Hen, Steven S., Beadle, Christopher D., Walton, Lesley, Man, Teresa, Rudyk, Helene, Clark, Barry, Tupper, David, Baker, S. Richard, Lamas, Carlos, Montero, Carlos, Marcos, Alicia, Blanco, Jaime, Bures, Mark, Clawson, David K., Atwell, Shane, Lu, Frances, Wang, Jing, Russell, Marijane, Heinz, Beverly A., Wang, Xushan, Carter, Joan H., Getman, Brian G., Catlow, John T., Swanson, Steven, Johnson, Bryan G., Shaw, David B., McKinzie, David L.
Published in Journal of medicinal chemistry (18.03.2016)
Published in Journal of medicinal chemistry (18.03.2016)
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Modulation of TARP γ8-Containing AMPA Receptors as a Novel Therapeutic Approach for Chronic Pain
Knopp, Kelly L, Simmons, Rosa Maria A, Guo, Wenhong, Adams, Benjamin L, Gardinier, Kevin M, Gernert, Douglas L, Ornstein, Paul L, Porter, Warren, Reel, Jon, Ding, Chunjin, Wang, He, Qian, Yuewei, Burris, Kevin D, Need, Anne, Barth, Vanessa, Swanson, Steven, Catlow, John, Witkin, Jeffrey M, Zwart, Ruud, Sher, Emanuele, Choong, Kar-Chan, Wall, Theron M, Schober, Douglas, Felder, Christian C, Kato, Akihiko S, Bredt, David S, Nisenbaum, Eric S
Published in The Journal of pharmacology and experimental therapeutics (01.06.2019)
Published in The Journal of pharmacology and experimental therapeutics (01.06.2019)
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