Search Results - "Britton, Thomas C"

Metabotropic Glutamate2 Receptors Play a Key Role in Modulating Head Twitches Induced by a Serotonergic Hallucinogen in Mice by Benvenga, Mark J., Chaney, Stephen F., Baez, Melvyn, Britton, Thomas C., Hornback, William J., Monn, James A., Marek, Gerard J.

“…There is substantial evidence that glutamate can modulate the effects of 5-hydroxytryptamine 2A (5-HT 2A ) receptor activation through stimulation of…”
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Metabotropic glutamate 2 receptor potentiators: receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model(s) by Johnson, Michael P, Barda, David, Britton, Thomas C, Emkey, Renee, Hornback, William J, Jagdmann, G Erik, McKinzie, David L, Nisenbaum, Eric S, Tizzano, Joseph P, Schoepp, Darryle D

“…To increase subtype selectivity and provide a novel means to alter receptor function, we discovered and characterization potentiators for the metabotropic…”
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Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor:  Synthesis and Subtype Selectivity of N-(4-(2-Methoxyphenoxy)phenyl)-N-(2,2,2− trifluoroethylsulfonyl)pyrid-3-ylmethylamine by Johnson, Michael P, Baez, Melvyn, Jagdmann, G. Erik, Britton, Thomas C, Large, Thomas H, Callagaro, David O, Tizzano, Joseph P, Monn, James A, Schoepp, Darryle D

“…This report describes recently discovered novel allosteric modulators of metabotropic glutamate2 (mGlu2) receptors. These pyridylmethylsulfonamides (e.g., 3)…”
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Targeting group II metabotropic glutamate (mGlu) receptors for the treatment of psychosis associated with Alzheimer's disease: selective activation of mGlu2 receptors amplifies beta-amyloid toxicity in cultured neurons, whereas dual activation of mGlu2 and mGlu3 receptors is neuroprotective by Caraci, Filippo, Molinaro, Gemma, Battaglia, Giuseppe, Giuffrida, Maria Laura, Riozzi, Barbara, Traficante, Anna, Bruno, Valeria, Cannella, Milena, Merlo, Sara, Wang, Xushan, Heinz, Beverly A, Nisenbaum, Eric S, Britton, Thomas C, Drago, Filippo, Sortino, Maria Angela, Copani, Agata, Nicoletti, Ferdinando

“…Dual orthosteric agonists of metabotropic glutamate 2 (mGlu2) and mGlu3 receptors are being developed as novel antipsychotic agents devoid of the adverse…”
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The asymmetric synthesis of .alpha.-amino acids. Electrophilic azidation of chiral imide enolates, a practical approach to the synthesis of (R)- and (S)-.alpha.-azido carboxylic acids by Evans, David A, Britton, Thomas C, Ellman, Jonathan A, Dorow, Roberta L

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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 by 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

“…As part of our ongoing efforts to identify novel ligands for the metabotropic glutamate 2 and 3 (mGlu2/3) receptors, we have incorporated substitution at the…”
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REM sleep behavior disorder and the risk of developing Parkinson disease or dementia by Britton, Thomas C, Chaudhuri, K Ray

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Potent and Selective 1,2,3-Trisubstituted Indole NPY Y-1 Antagonists by Hipskind, Philip A, Lobb, Karen L, Nixon, James A, Britton, Thomas C, Bruns, Robert F, Catlow, John, Dieckman-McGinty, Donna K, Gackenheimer, Susan L, Gitter, Bruce D, Iyengar, Smriti, Schober, Douglas A, Simmons, Rosa M. A, Swanson, Steve, Zarrinmayeh, Hamideh, Zimmerman, Dennis M, Gehlert, Donald R

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Stereoselective amination of chiral enolates. A new approach to the asymmetric synthesis of .alpha.-hydrazino and .alpha.-amino acid derivatives by Evans, David A, Britton, Thomas C, Dorow, Roberta L, Dellaria, Joseph F

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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 by 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.

“…A novel series of selective negative allosteric modulators (NAMs) for metabotropic glutamate receptor 5 (mGlu5) was discovered from an isothiazole scaffold…”
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Electrophilic azide transfer to chiral enolates. A general approach to the asymmetric synthesis of .alpha.-amino acids by Evans, David A, Britton, Thomas C

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SAR study of a subtype selective allosteric potentiator of metabotropic glutamate 2 receptor, N-(4-phenoxyphenyl)- N-(3-pyridinylmethyl)ethanesulfonamide by Barda, David A., Wang, Zhao-Qing, Britton, Thomas C., Henry, Steven S., Jagdmann, G.Erik, Coleman, Darrell S., Johnson, Michael P., Andis, Sherri L., Schoepp, Darryle D.

“…The structure–activity relationship of a subtype selective mGlu2 potentiator, LY181837 is explored. The major excitatory neurotransmitter in the Central…”
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Synthesis and Evaluation of a Series of Novel 2-[(4-Chlorophenoxy)methyl]- benzimidazoles as Selective Neuropeptide Y Y1 Receptor Antagonists by Zarrinmayeh, Hamideh, Nunes, Anne M, Ornstein, Paul L, Zimmerman, Dennis M, Arnold, M. Brian, Schober, Douglas A, Gackenheimer, Susan L, Bruns, Robert F, Hipskind, Philip A, Britton, Thomas C, Cantrell, Buddy E, Gehlert, Donald R

“…A series of novel benzimidazoles (BI) derived from the indole 2 was synthesized and evaluated as selective neuropeptide Y (NPY) Y1 receptor antagonists with…”
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Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists by Zarrinmayeh, Hamideh, Zimmerman, Dennis M., Cantrell, Buddy E., Schober, Douglas A., Bruns, Robert E., Gackenheimer, Susan L., Ornstein, Paul L., Hipskind, Philip A., Britton, Thomas C., Gehlert, Donald R.

“…A series of benzimidazoles ( 4) was synthesized and evaluated in vitro as potent and selective NPY Y1 receptor antagonists. Substitution of the piperidine…”
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Clinical use of the magnetic stimulator in the investigation of peripheral conduction time by Britton, T C, Meyer, B U, Herdmann, J, Benecke, R

“…The application of rapidly changing magnetic fields (magnetic stimulation) over the neck or lower back elicits EMG responses in the muscles of the arm or leg…”
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Structure-activity relationships of a series of benzothiophene-derived NPY Y1 antagonists: Optimization of the C-2 side chain by Britton, Thomas C., Spinazze, Patrick G., Hipskind, Philip A., Zimmerman, Dennis M., Zarrinmayeh, Hamideh, Schober, Douglas A., Gehlert, Donald R., Bruns, Robert F.

“…A series of benzo[ b]thiophene-derived NPY-1 receptor antagonists is described. Systematic modification of the C-2 substituent afforded a 1000-fold range in Y1…”
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Metabotropic Glutamate 2 Receptors Play a Key Role in Modulating Head Twitches Induced by a Serotonergic Hallucinogen in Mice by Benvenga, Mark J, Chaney, Stephen F, Baez, Melvyn, Britton, Thomas C, Hornback, William J, Monn, James A, Marek, Gerard J

“…There is substantial evidence that glutamate can modulate the effects of 5-hydroxytryptamine (5-HT ) receptor activation through stimulation of metabotropic…”
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Discovery of allosteric potentiators for the metabotropic glutamate 2 receptor : Synthesis and subtype selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,2-trifluoroethylsulfonyl)pyrid-3-ylmethyl- amine by JOHNSON, Michael P, BAEZ, Melvyn, JAGDMANN, G. Erik, BRITTON, Thomas C, LARGE, Thomas H, CALLAGARO, David O, TIZZANO, Joseph P, MONN, James A, SCHOEPP, Darryle D

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Degradation chemistry of gemcitabine hydrochloride, a new antitumor agent by Anliker, S L, McClure, M S, Britton, T C, Stephan, E A, Maple, S R, Cooke, G G

“…The anti-tumor agent gemcitabine hydrochloride, a beta-difluoronucleoside, is remarkably stable in the solid state. In 0.1 N HCI solution at 40 degrees C,…”
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Novel 1,2,3-thiadiazolyl sulfines from the reaction of N-substituted hydrazones with thionyl chloride by Britton, Thomas C, Lobl, Thomas J, Chidester, Constance G

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