Search Results - "Reel, Jon"

Discovery of the First α‑Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ‑8 by Gardinier, Kevin M, Gernert, Douglas L, Porter, Warren J, Reel, Jon K, Ornstein, Paul L, Spinazze, Patrick, Stevens, F. Craig, Hahn, Patric, Hollinshead, Sean P, Mayhugh, Daniel, Schkeryantz, Jeff, Khilevich, Albert, De Frutos, Oscar, Gleason, Scott D, Kato, Akihiko S, Luffer-Atlas, Debra, Desai, Prashant V, Swanson, Steven, Burris, Kevin D, Ding, Chunjin, Heinz, Beverly A, Need, Anne B, Barth, Vanessa N, Stephenson, Gregory A, Diseroad, Benjamin A, Woods, Tim A, Yu, Hong, Bredt, David, Witkin, Jeffrey M

“…Transmembrane AMPA receptor regulatory proteins (TARPs) are a family of scaffolding proteins that regulate AMPA receptor trafficking and function. TARP γ-8 is…”
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Targeted Blockade of TARP-γ8-Associated AMPA Receptors: Anticonvulsant Activity with the Selective Antagonist LY3130481 (CERC-611) by 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

“…6-[(1S)-1-[1-[5-(2-hydroxyethoxy)-2-pyridyl]pyrazol-3-yl]ethyl]- 3H-1,3-benzothiazol-2-one (LY3130481 or CERC-611) is a selective antagonist of AMPA receptors…”
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Substituted 3-Imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino- [6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as Highly Selective and Potent Inhibitors of Glycogen Synthase Kinase-3 by Engler, Thomas A, Henry, James R, Malhotra, Sushant, Cunningham, Brian, Furness, Kelly, Brozinick, Joseph, Burkholder, Timothy P, Clay, Michael P, Clayton, Joshua, Diefenbacher, Clive, Hawkins, Eric, Iversen, Philip W, Li, Yihong, Lindstrom, Terry D, Marquart, Angela L, McLean, Johnathan, Mendel, David, Misener, Elizabeth, Briere, Daniel, O'Toole, John C, Porter, Warren J, Queener, Steven, Reel, Jon K, Owens, Rebecca A, Brier, Richard A, Eessalu, Thomas E, Wagner, Jill R, Campbell, Robert M, Vaughn, Renee

“…Glycogen synthase kinase-3 (GSK3) is involved in signaling from the insulin receptor. Inhibitors of GSK3 are expected to effect lowering of plasma glucose…”
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Discovery and SAR studies of novel GlyT1 inhibitors by Walter, Magnus W., Hoffman, Beth J., Gordon, Kimberly, Johnson, Kirk, Love, Patrick, Jones, Matthew, Man, Teresa, Phebus, Lee, Reel, Jon K., Rudyk, Helene C., Shannon, Harlan, Svensson, Kjell, Yu, Hong, Valli, Matthew J., Porter, Warren J.

“…A novel series of GlyT1 inhibitors and their structure–activity Relationships (SAR) are described. Members of this series are highly potent and selective…”
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The development of potent and selective bisarylmaleimide GSK3 inhibitors by Engler, Thomas A., Malhotra, Sushant, Burkholder, Timothy P., Henry, James R., Mendel, David, Porter, Warren J., Furness, Kelly, Diefenbacher, Clive, Marquart, Angela, Reel, Jon K., Li, Yihong, Clayton, Joshua, Cunningham, Brian, McLean, Johnathan, O’Toole, John C., Brozinick, Joseph, Hawkins, Eric, Misener, Elizabeth, Briere, Daniel, Brier, Richard A., Wagner, Jill R., Campbell, Robert M., Anderson, Bryan D., Vaughn, Renee, Bennett, Donald B., Meier, Timothy I., Cook, James A.

“…3-(Imidazo[1,2- a]pyridin-3-yl)-, its aza-analogs, and 3-(pyrazolo[1,5- a]pyridin-3-yl)-4-(2-acyl-(1,2,3,4-tetrahydro[1,4]diazepino[6,7,1-…”
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Forebrain-selective AMPA-receptor antagonism guided by TARP γ-8 as an antiepileptic mechanism by 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

“…Selective pharmacological blockade of forebrain excitatory AMPA receptors that express the TARP γ-8 subunit enables antiepileptic therapy in rodent models of…”
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Reconstitution of synaptic Ion channels from rodent and human brain in Xenopus oocytes: a biochemical and electrophysiological characterization by Mazzo, Francesca, Zwart, Ruud, Serratto, Giulia Maia, Gardinier, Kevin M., Porter, Warren, Reel, Jon, Maraula, Giovanna, Sher, Emanuele

“…Disruption in the expression and function of synaptic proteins, and ion channels in particular, is critical in the pathophysiology of human neuropsychiatric…”
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Electroencephalographic, cognitive, and neurochemical effects of LY3130481 (CERC-611), a selective antagonist of TARP-γ8-associated AMPA receptors by Witkin, Jeffrey M., Li, Jennifer, Gilmour, Gary, Mitchell, Stephen N., Carter, Guy, Gleason, Scott D., Seidel, Wesley F., Eastwood, Brian J., McCarthy, Andrew, Porter, Warren J., Reel, Jon, Gardinier, Kevin M., Kato, Akihiko S., Wafford, Keith A.

“…6-[(1S)-1-[1-[5-(2-hydroxyethoxy)-2-pyridyl]pyrazol-3-yl]ethyl]-3H-1,3-benzothiazol-2-one (LY3130481 or CERC-611) is a selective antagonist of AMPA receptors…”
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Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for .mu.- and .kappa.-opioid receptors by Zimmerman, Dennis M, Leander, J. David, Cantrell, Buddy E, Reel, Jon K, Snoddy, John, Mendelsohn, Laurane G, Johnson, Bryan G, Mitch, Charles H

“…A series of racemic N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines were evaluated for opioid agonist and antagonist activity at mu and kappa…”
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Modulation of TARP γ 8-Containing AMPA Receptors as a Novel Therapeutic Approach for Chronic Pain by 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

“…Nonselective glutamate -amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists are efficacious in chronic pain but have significant…”
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A novel class of 5-HT2A receptor antagonists: aryl aminoguanidines by Bryant, H U, Nelson, D L, Button, D, Cole, H W, Baez, M B, Lucaites, V L, Wainscott, D B, Whitesitt, C, Reel, J, Simon, R, Koppel, G A

“…Local delivery of serotonin (5-HT) produces a rapid edematous response in soft tissues via increased fluid extravasation which is prevented by 5-HT2…”
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Forebrain-selective AMPA-receptor antagonism guided by TARP [gamma]-8 as an antiepileptic mechanism by 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

“…Pharmacological manipulation of specific neural circuitsto optimize therapeutic index is an unrealized goal in neurology and psychiatry. AMPA receptors are…”
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Structural Evolution and Pharmacology of a Novel Series of Triacid Angiotensin II Receptor Antagonists by Palkowitz, Alan D, Steinberg, Mitchell I, Thrasher, K. Jeff, Reel, Jon K, Hauser, Kenneth L, Zimmerman, Karen M, Wiest, Sally A, Whitesitt, Celia A, Simon, Richard L

“…cis-4-(4-Phenoxy)-1-[1-oxo-2(R)-[4-[(2-sulfobenzoyl)amino)-1H- imidazol-1-yl]octyl]-L-proline derivatives represent a novel class of potent nonpeptide…”
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Synthesis and structure-activity relationships of benzophenones as inhibitors of cathepsin D by Whitesitt, Celia A., Simon, Richard L., Reel, Jon K., Sigmund, Sandra K., Phillips, Michael L., Kevin Shadle, J., Heinz, Lawrence J., Koppel, Gary A., Hunden, David C., Lifer, Sherryl L., Berry, Dennis, Ray, Judy, Little, Sheila P, Xiadong Liu, Marshall, Winston S., Panetta, Jill A.

“…Non peptide inhibitors of cathepsin D, an aspartyl protease that has been implicated in many disease states including Alzheimer's disease, were prepared and…”
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Abstract 1131: Novel inhibitor of Notch signaling for the treatment of cancer by Bender, Mark H., Gao, Hong, Capen, Andrew R., Clay, Julia M., Hipskind, Philip A., Reel, Jon K., Zamek-Gliszczynski, Maciej J., Manro, Jason R., Benhadji, Karim, Patel, Bharvin K. R.

“…The Notch pathway is a highly conserved signaling system that plays an important role in development and tissue homeostasis. While Notch mutations are well…”
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Synthesis and absolute configuration of LY255582, a potent opioid antagonist by Mitch, Charles H, Zimmerman, Dennis M, Snoddy, John D, Reel, Jon K, Cantrell, Buddy E

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Characterization of the neurotoxic potential of m-methoxy-MPTP and the use of its N-ethyl analog as a means of avoiding exposure to a possible Parkinson-causing agent by Zimmerman, Dennis M, Cantrell, Buddy E, Reel, Jon K, Hemrick-Luecke, Susan K, Fuller, Ray W

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Non-peptide angiotensin II receptor antagonists discriminate subtypes of 125I-angiotensin II binding sites in the rat brain by Gehlert, D R, Gackenheimer, S L, Reel, J K, Lin, H S, Steinberg, M I

“…We have utilized quantitative autoradiography to define subtypes of 125I-angiotensin II (AII) binding in rat brain. AII-1 binding (displaced by DuP 753) was…”
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3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity by Mitch, Charles H, Leander, J. David, Mendelsohn, Laurane G, Shaw, Walter N, Wong, David T, Cantrell, Buddy E, Johnson, Bryan G, Reel, John K, Snoddy, John D

“…A series of (3R*,4R*)-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists with varying substituents on the nitrogen were evaluated for their effect…”
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A novel class of 5-HT 2a receptor antagonists: Aryl aminoguanidines by Bryant, Henry U., Nelson, David L., Button, Donald, Cole, Harlan W., Baez, Melvyn B., Lucaites, Virginia L., Wainscott, David B., Whitesitt, Cecilia, Reel, Jon, Simon, Richard, Koppel, Gary A.

“…Local delivery of serotonin (5-HT) produces a rapid edematous response in soft tissues via increased fluid extravasation which is prevented by 5-HT 2…”
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