Search Results - "Burns, H. Donald"

Synthesis, characterization, and monkey PET studies of [18F]MK-1312, a PET tracer for quantification of mGluR1 receptor occupancy by MK-5435 by Hostetler, Eric D., Eng, Waisi, Joshi, Aniket D., Sanabria-Bohórquez, Sandra, Kawamoto, Hiroshi, Ito, Satoru, O'Malley, Stacey, Krause, Stephen, Ryan, Christine, Patel, Shil, Williams, Mangay, Riffel, Kerry, Suzuki, Gentaroh, Ozaki, Satoshi, Ohta, Hisashi, Cook, Jacquelynn, Burns, H. Donald, Hargreaves, Richard

“…Two moderately lipophilic, high affinity ligands for metabotropic glutamate receptor subtype 1 (mGluR1) were radiolabeled with a positron‐emitting radioisotope…”
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The synthesis and preclinical evaluation in rhesus monkey of [18F]MK-6577 and [11C]CMPyPB glycine transporter 1 positron emission tomography radiotracers by Hamill, Terence G., Eng, Waisi, Jennings, Andrew, Lewis, Richard, Thomas, Steven, Wood, Suzanne, Street, Leslie, Wisnoski, David, Wolkenberg, Scott, Lindsley, Craig, Sanabria-BohÓRquez, Sandra M., Patel, Shil, Riffel, Kerry, Ryan, Christine, Cook, Jacquelynn, Sur, Cyrille, Burns, H. Donald, Hargreaves, Richard

“…Two positron emission tomography radiotracers for the glycine transporter 1 (GlyT1) are reported here. Each radiotracer is a propylsulfonamide‐containing…”
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Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in rats, primates, and humans by Atack, John R, Wong, Dean F, Fryer, Tim D, Ryan, Christine, Sanabria, Sandra, Zhou, Yun, Dannals, Robert F, Eng, Wai-si, Gibson, Raymond E, Burns, H Donald, Vega, Jose M, Vessy, Laura, Scott-Stevens, Paul, Beech, John S, Baron, Jean-Claude, Sohal, Bindi, Schrag, Michael L, Aigbirhio, Franklin I, McKernan, Ruth M, Hargreaves, Richard J

“…The GABA(A) receptor alpha2/alpha3 subtype-selective compound…”
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Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1 by Blackaby, Wesley P, Lewis, Richard T, Thomson, Joanne L, Jennings, Andrew S. R, Goodacre, Simon C, Street, Leslie J, MacLeod, Angus M, Pike, Andrew, Wood, Suzanne, Thomas, Steve, Brown, Terry A, Smith, Alison, Pillai, Gopalan, Almond, Sarah, Guscott, Martin R, Burns, H. Donald, Eng, Waisi, Ryan, Christine, Cook, Jacquelynn, Hamill, Terence G

“…Amalgamation of the structure−activity relationship of two series of GlyT1 inhibitors developed at Merck led to the discovery of a clinical candidate, compound…”
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[¹⁸F]MK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptor by Burns, H. Donald, Van Laere, Koen, Sanabria-Bohórquez, Sandra, Hamill, Terence G, Bormans, Guy, Eng, Wai-si, Gibson, Ray, Ryan, Christine, Connolly, Brett, Patel, Shil, Krause, Stephen, Vanko, Amy, Van Hecken, Anne, Dupont, Patrick, De Lepeleire, Inge, Rothenberg, Paul, Stoch, S. Aubrey, Cote, Josee, Hagmann, William K, Jewell, James P, Lin, Linus S, Liu, Ping, Goulet, Mark T, Gottesdiener, Keith, Wagner, John A, de Hoon, Jan, Mortelmans, Luc, Fong, Tung M, Hargreaves, Richard J

“…[¹⁸F]MK-9470 is a selective, high-affinity, inverse agonist (human IC₅₀, 0.7 nM) for the cannabinoid CB1 receptor (CB1R) that has been developed for use in…”
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The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine by LIN, Peter, LEHUA CHANG, KURTZ, Marc M, TSAO, Kwei-Lan C, WHEELDON, Alan, CARLSON, Emma J, ENG, Waisi, BURNS, H. Donald, HARGREAVES, Richard J, MILLS, Sander G, DEVITA, Robert J, YOUNG, Jonathan R, EID, Ronsar, XINCHUN TONG, SONG ZHENG, BALL, Richard G, TSOU, Nancy N, CHICCHI, Gary G

“…SAR studies on amides, ureas, and vinylogous amides derived from pyrrolidine led to the discovery of several potent hNK(1) antagonists. One particular…”
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Whole-Body Biodistribution and Radiation Dosimetry of the Human Cannabinoid Type-1 Receptor Ligand 18F-MK-9470 in Healthy Subjects by Van Laere, Koen, Koole, Michel, Sanabria Bohorquez, Sandra M, Goffin, Karolien, Guenther, Ilonka, Belanger, Marie J, Cote, Josee, Rothenberg, Paul, De Lepeleire, Inge, Grachev, Igor D, Hargreaves, Richard J, Bormans, Guy, Burns, H. Donald

“…The cannabinoid type-1 (CB1) receptor is one of the most abundant G-coupled protein receptors in the human body and is responsible for signal transduction of…”
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The Acyclic CB1R Inverse Agonist Taranabant Mediates Weight Loss by Increasing Energy Expenditure and Decreasing Caloric Intake by Addy, Carol, Wright, Hamish, Van Laere, Koen, Gantz, Ira, Erondu, Ngozi, Musser, Bret J., Lu, Kaifeng, Yuan, Jinyu, Sanabria-Bohórquez, Sandra M., Stoch, Aubrey, Stevens, Cathy, Fong, Tung M., De Lepeleire, Inge, Cilissen, Caroline, Cote, Josee, Rosko, Kim, Gendrano, Isaias N., Nguyen, Allison Martin, Gumbiner, Barry, Rothenberg, Paul, de Hoon, Jan, Bormans, Guy, Depré, Marleen, Eng, Wai-si, Ravussin, Eric, Klein, Samuel, Blundell, John, Herman, Gary A., Burns, H. Donald, Hargreaves, Richard J., Wagner, John, Gottesdiener, Keith, Amatruda, John M., Heymsfield, Steven B.

“…Cannabinoid 1 receptor (CB1R) inverse agonists are emerging as a potential obesity therapy. However, the physiological mechanisms by which these agents…”
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Non-invasive radiotracer imaging as a tool for drug development by Gibson, R E, Burns, H D, Hamill, T G, Eng, W S, Francis, B E, Ryan, C

“…Non-Invasive Radiotracer Imaging (NIRI) uses either short-lived positron-emitting isotopes, such as 11C and 18F, for Positron Emis ion Tomography (PET) or…”
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Neuropeptide Y5 receptor antagonism does not induce clinically meaningful weight loss in overweight and obese adults by Erondu, Ngozi, Gantz, Ira, Musser, Bret, Suryawanshi, Shailaja, Mallick, Madhuja, Addy, Carol, Cote, Josee, Bray, George, Fujioka, Ken, Bays, Harold, Hollander, Priscilla, Sanabria-Bohórquez, Sandra M., Eng, WaiSi, Långström, Bengt, Hargreaves, Richard J., Burns, H. Donald, Kanatani, Akio, Fukami, Takehiro, MacNeil, Douglas J., Gottesdiener, Keith M., Amatruda, John M., Kaufman, Keith D., Heymsfield, Steven B.

“…Neuropeptide Y (NPY) is a potent orexigenic neuropeptide, and antagonism of NPY Y1 and NPY Y5 receptors (NPYxR) is considered a potentially important…”
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(11)C-MK-8278 PET as a tool for pharmacodynamic brain occupancy of histamine 3 receptor inverse agonists by Van Laere, Koenraad J, Sanabria-Bohórquez, Sandra M, Mozley, David P, Burns, Donald H, Hamill, Terence G, Van Hecken, Anne, De Lepeleire, Inge, Koole, Michel, Bormans, Guy, de Hoon, Jan, Depré, Marleen, Cerchio, Kristine, Plalcza, John, Han, Lingling, Renger, John, Hargreaves, Richard J, Iannone, Robert

“…The histamine 3 (H3) receptor is a presynaptic autoreceptor in the central nervous system that regulates the synthesis and release of histamine and modulates…”
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Kinetic analysis of the cannabinoid-1 receptor PET tracer [18F]MK-9470 in human brain by Sanabria-Bohórquez, Sandra Marina, Hamill, Terence G., Goffin, Karolien, De Lepeleire, Inge, Bormans, Guy, Burns, H. Donald, Van Laere, Koen

“…Purpose Quantitative imaging of the type 1 cannabinoid receptor (CB1R) opens perspectives for many neurological and psychiatric disorders. We characterized the…”
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Evaluation of [18F]MK-0911, a positron emission tomography (PET) tracer for opioid receptor-like 1 (ORL1), in rhesus monkey and human by Hostetler, Eric D., Sanabria-Bohórquez, Sandra, Eng, Waisi, Joshi, Aniket D., Patel, Shailendra, Gibson, Raymond E., O'Malley, Stacey, Krause, Stephen M., Ryan, Christine, Riffel, Kerry, Bi, Sheng, Okamoto, Osamu, Kawamoto, Hiroshi, Ozaki, Satoshi, Ohta, Hisashi, de Groot, Tjibbe, Bormans, Guy, Depré, Marleen, de Hoon, Jan, De Lepeleire, Inge, Reynders, Tom, Cook, Jacquelynn J., Burns, H. Donald, Egan, Michael, Cho, William, van Laere, Koen, Hargreaves, Richard J.

“…Antagonism of the central opioid receptor like-1 receptor (ORL1) has been implicated in cognition, and has been a focus of drug discovery efforts to ameliorate…”
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Synthesis, characterization, and monkey positron emission tomography (PET) studies of [18F]Y1-973, a PET tracer for the neuropeptide Y Y1 receptor by Hostetler, Eric D., Sanabria-Bohórquez, Sandra, Fan, Hong, Zeng, Zhizhen, Gantert, Liza, Williams, Mangay, Miller, Patricia, O'Malley, Stacey, Kameda, Minoru, Ando, Makoto, Sato, Nagaaki, Ozaki, Satoshi, Tokita, Shigeru, Ohta, Hisashi, Williams, David, Sur, Cyrille, Cook, Jacquelynn J., Burns, H. Donald, Hargreaves, Richard

“…Neuropeptide Y receptor subtype 1 (NPY Y1) has been implicated in appetite regulation, and antagonists of NPY Y1 are being explored as potential therapeutics…”
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Inverse agonist histamine H3 receptor PET tracers labelled with carbon-11 or fluorine-18 by Hamill, Terence G., Sato, Nagaaki, Jitsuoka, Makoto, Tokita, Shigeru, Sanabria, Sandra, Eng, Waisi, Ryan, Christine, Krause, Stephen, Takenaga, Norihiro, Patel, Shil, Zeng, Zhizhen, Williams Jr, David, Sur, Cyrille, Hargreaves, Richard, Burns, H. Donald

“…Two histamine H3 receptor (H3R) inverse agonist PET tracers have been synthesized and characterized in preclinical studies. Each tracer has high affinity for…”
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Decreased Neurokinin-1 (Substance P) Receptor Binding in Patients with Panic Disorder: Positron Emission Tomographic Study with [18 F]SPA-RQ by Fujimura, Yota, Yasuno, Fumihiko, Farris, Amanda, Liow, Jeih-San, Geraci, Marilla, Drevets, Wayne, Pine, Daniel S, Ghose, Subroto, Lerner, Alicja, Hargreaves, Richard, Burns, H. Donald, Morse, Cheryl, Pike, Victor W, Innis, Robert B

“…Background Positron emission tomography (PET) can localize and quantify neurokinin-1 (NK1 ) receptors in brain using the nonpeptide antagonist radioligand, [18…”
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Human positron emission tomography studies of brain neurokinin 1 receptor occupancy by aprepitant by Bergström, Mats, Hargreaves, Richard J, Burns, H.Donald, Goldberg, Michael R, Sciberras, David, Reines, Scott A, Petty, Kevin J, Ögren, Mattias, Antoni, Gunnar, Långström, Bengt, Eskola, Olli, Scheinin, Mika, Solin, Olof, Majumdar, Anup K, Constanzer, Marvin L, Battisti, Wendy P, Bradstreet, Thomas E, Gargano, Cynthia, Hietala, Jarmo

“…Aprepitant is a highly selective substance P (neurokinin 1 [NK 1] receptor) antagonist that significantly improves the pharmacotherapy of acute and delayed…”
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Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers by Hamill, Terence G., Krause, Stephen, Ryan, Christine, Bonnefous, Celine, Govek, Steve, Seiders, T. Jon, Cosford, Nicholas D.P., Roppe, Jeffrey, Kamenecka, Ted, Patel, Shil, Gibson, Raymond E., Sanabria, Sandra, Riffel, Kerry, Eng, Waisi, King, Christopher, Yang, Xiaoqing, Green, Mitchell D., O'malley, Stacey S., Hargreaves, Richard, Burns, H. Donald

“…Three metabotropic glutamate receptor subtype 5 (mGluR5) PET tracers have been labeled with either carbon‐11 or fluorine‐18 and their in vitro and in vivo…”
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In vivo characterization and dynamic receptor occupancy imaging of TPA023B, an alpha 2/alpha 3/alpha 5 subtype selective gamma-aminobutyric acid-a partial agonist by Van Laere, Koen, Bormans, Guy, Sanabria-Bohórquez, Sandra M, de Groot, Tjibbe, Dupont, Patrick, De Lepeleire, Inge, de Hoon, Jan, Mortelmans, Luc, Hargreaves, Richard J, Atack, John R, Burns, H Donald

“…A novel, high-affinity (.7-2.0 nmol) compound that selectively activates the alpha2, alpha 3, and alpha 5 (but not alpha1) gamma-aminobutyric acid-A (GABA(A))…”
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Characterization of [18F]Y1-973, a novel PET tracer for the neuropeptide Y Y1 receptor (NPY Y1), in rhesus monkey by Hostetler, Eric, Sanabria, Sandra, Fan, Hong, Kameda, Minoru, Ando, Makato, Zeng, Zhizhen, O'Malley, Stacey, Miller, Patricia, Gantert, Liza, Williams, David, Tokita, Shigeru, Sato, Nagaaki, Ozaki, Satoshi, Ohta, Hisashi, Cook, Jacquelynn, Burns, H. Donald, Hargreaves, Richard

“…Blockade of [18F]Y1-973 uptake with Y1-718 was dose-dependent, and at the highest dose reduced tracer uptake in the striatum and cortical regions to a level of…”
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