Search Results - "Hamill, Terence G."

[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 relationship between glycine transporter 1 occupancy and the effects of the glycine transporter 1 inhibitor RG1678 or ORG25935 on object retrieval performance in scopolamine impaired rhesus monkey by Eddins, Donnie, Hamill, Terence G., Puri, Vanita, Cannon, Christopher E., Vivian, Jeffrey A., Sanabria-Bohórquez, Sandra M., Cook, Jacquelynn J., Morrow, John A., Thomson, Fiona, Uslaner, Jason M.

“…Reduced NMDA receptor functioning is hypothesized to underlie the cognitive and negative symptoms associated with schizophrenia. However, because direct…”
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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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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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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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Preclinical evaluation of [11C]L‐235 as a radioligand for Positron Emission Tomography cathepsin K imaging in bone by Bennacef, Idriss, Rubins, Daniel, Riffel, Kerry, Williams, Mangay, Posavec, Diane J., Holahan, Marie A., Purcell, Mona L., Haley, Hyking D., Wolf, Mary, Stachel, Shawn J., Lubbers, Laura S., Wesolowski, Gregg A., Duong, Le T., Hamill, Terence G., Evelhoch, Jeffrey L., Hostetler, Eric D.

“…The cathepsin K (CatK) enzyme is abundantly expressed in osteoclasts, and CatK inhibitors have been developed for the treatment of osteoporosis. In our effort…”
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Species differences in mGluR5 binding sites in mammalian central nervous system determined using in vitro binding with [18 F]F-PEB by Patel, Shil, Hamill, Terence G, Connolly, Brett, Jagoda, Elaine, Li, Wenping, Gibson, Raymond E

“…Abstract Binding of [18 F]3-fluoro-5-[(pyridin-3-yl)ethynyl]benzonitrile ([18 F]F-PEB) was evaluated in membranes and tissue sections prepared from rat, rhesus…”
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Characterization of the novel GlyT1 PET tracer [18F]MK-6577 in humans by Joshi, Aniket D., Sanabria-Bohórquez, Sandra M., Bormans, Guy, Koole, Michel, De Hoon, Jan, Van Hecken, Anne, Depre, Marleen, De Lepeleire, Inge, Van Laere, Koen, Sur, Cyrille, Hamill, Terence G.

“…ABSTRACT Decreased glutamatergic neurotransmission is hypothesized to be involved in the pathophysiology of schizophrenia. Inhibition of glycine transporter…”
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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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Comparative evaluation of two glycine transporter 1 radiotracers [11C]GSK931145 and [18F]MK-6577 in baboons by Zheng, Ming-Qiang, Lin, Shu-Fei, Holden, Daniel, Naganawa, Mika, Ropchan, Jim R., Najafzaden, Soheila, Kapinos, Michael, Tabriz, Mike, Carson, Richard E., Hamill, Terence G., Huang, Yiyun

“…SUV images summed from 30 to 45 min post injection of [11C]GSK931145 (A) and [18F]MK‐6577 (B) in coronal (left), transverse (middle) and sagittal (right)…”
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Quantification of the glycine transporter 1 in rhesus monkey brain using [18F]MK-6577 and a model-based input function by Sanabria-Bohórquez, Sandra M., Joshi, Aniket D., Holahan, Marie, Daneker, Lori, Riffel, Kerry, Williams, Mangay, Li, Wenping, Cook, Jacquelynn J., Hamill, Terence G.

“…Glycine transporter 1 (GlyT1) inhibitors have emerged as potential treatments for schizophrenia due to their potentiation of NMDA receptor activity by…”
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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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18F-FPEB, a PET radiopharmaceutical for quantifying metabotropic glutamate 5 receptors: a first-in-human study of radiochemical safety, biokinetics, and radiation dosimetry by Wong, Dean F, Waterhouse, Rikki, Kuwabara, Hiroto, Kim, Jongho, Brašić, James R, Chamroonrat, Wichana, Stabins, Michael, Holt, Daniel P, Dannals, Robert F, Hamill, Terence G, Mozley, P David

“…Identification of safe and valid PET radioligands for metabotropic glutamate receptor, type 5 (mGluR5), is essential to measure changes in brain mGluR5 in…”
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Biodistribution and radiation dosimetry of [18F]F-PEB in nonhuman primates by Bélanger, Marie-José, Krause, Stephen M, Ryan, Christine, Sanabria-Bohorquez, Sandra, Li, Wenping, Hamill, Terence G, Burns, Hugh Donald

“…INTRODUCTIONThe metabotropic glutamate receptor subtype 5 (mGluR5) is distributed throughout the central nervous system (CNS), and has been suggested to be a…”
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Erratum to: 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

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Discovery of N-{(1S,2S)-2-(3-Cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a Cannabinoid-1 Receptor Positron Emission Tomography Tracer Suitable for Clinical Use by Liu, Ping, Lin, Linus S, Hamill, Terence G, Jewell, James P, Lanza, Thomas J, Gibson, Raymond E, Krause, Stephen M, Ryan, Christine, Eng, Waisi, Sanabria, Sandra, Tong, Xinchun, Wang, Junying, Levorse, Dorothy A, Owens, Karen A, Fong, Tung M, Shen, Chun-Pyn, Lao, Julie, Kumar, Sanjeev, Yin, Wenji, Payack, Joseph F, Springfield, Shawn A, Hargreaves, Richard, Burns, H. Donald, Goulet, Mark T, Hagmann, William K

“…The discovery of a structurally distinct cannabinoid-1 receptor (CB1R) positron emission tomography tracer is described. Starting from an acyclic amide CB1R…”
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PET Imaging Studies in Rhesus Monkey with the Cannabinoid-1 (CB1) Receptor Ligand [11C]CB-119 by Hamill, Terence G., Lin, Linus S., Hagmann, William, Liu, Ping, Jewell, James, Sanabria, Sandra, Eng, WaiSi, Ryan, Christine, Fong, Tung M., Connolly, Brett, Vanko, Amy, Hargreaves, Richard, Goulet, Mark T., Burns, H. Donald

“…Purpose The in vitro and in vivo evaluation of the selective, high affinity (human CB1 IC 50 0.49 nM) inverse agonist CB1R tracer [ 11 C]CB-119, a close analog…”
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Radiosynthesis of the HIV integrase inhibitor [18F]MK-0518 (Isentress) by Li, Wenping, Thompson, Wayne, Fisher, Thorsten, Wai, John S., Hazuda, Daria, Burns, H. Donald, Hamill, Terence G.

“…The human immunodeficiency virus integrase inhibitor, [18F]MK‐0518, was prepared via a three‐step, one‐pot radiosynthesis. [18F]4‐Fluorobenzylamine was…”
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An asymmetric total synthesis of fragrant spiro[4.5]decane sesquiterpene (-)-.beta.-vetivone via an enantiomerically pure vinylic sulfoxide by Posner, Gary H, Hamill, Terence G

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