Search Results - "GIBSON, Raymond E"

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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Hepatic glucagon receptor binding and glucose-lowering in vivo by peptidyl and non-peptidyl glucagon receptor antagonists by Dallas-Yang, Qing, Shen, Xiaolan, Strowski, Mathias, Brady, Edward, Saperstein, Richard, Gibson, Raymond E., Szalkowski, Deborah, Qureshi, Sajjad A., Candelore, Mari Rios, Fenyk-Melody, Judith E., Parmee, Emma R., Zhang, Bei B., Jiang, Guoqiang

“…Glucagon receptor antagonists have been actively pursued as potential therapeutics for the treatment of type 2 diabetes. Peptidyl and non-peptidyl glucagon…”
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Downregulation of Notch Pathway by a γ-Secretase Inhibitor Attenuates AKT/Mammalian Target of Rapamycin Signaling and Glucose Uptake in an ERBB2 Transgenic Breast Cancer Model by EFFERSON, Clay L, WINKELMANN, Christopher T, BUSER, Carolyn, YEATMAN, Timothy, COPPOLA, Domenico, WINTER, Christopher, CLARK, Edwin A, DRAETTA, Giulio F, STRACK, Peter R, MAJUMDER, Pradip K, WARE, Christopher, SULLIVAN, Timothy, GIAMPAOLI, Saverio, TAMMAM, Jennifer, PATEL, Shailendra, MESITI, Giuseppe, REILLY, John F, GIBSON, Raymond E

“…ERBB2/neu and Notch signaling are known to be deregulated in many human cancers. However, pathway cross-talk and dependencies are not well understood. In this…”
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Generation and characterization of a human bradykinin receptor B1 transgenic rat as a pharmacodynamic model by Hess, J Fred, Ransom, Richard W, Zeng, Zhizhen, Chang, Raymond S L, Hey, Patricia J, Warren, Lee, Harrell, Charles M, Murphy, Kathryn L, Chen, Tsing-Bau, Miller, Patricia J, Lis, Edward, Reiss, Duane, Gibson, Raymond E, Markowitz, M Kristine, DiPardo, Robert M, Su, Dai-Shi, Bock, Mark G, Gould, Robert J, Pettibone, Douglas J

“…Antagonists of the B1 bradykinin receptor (B1R) offer the promise of novel therapeutic agents for the treatment of inflammatory and neuropathic pain. However,…”
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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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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 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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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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In vitro characterization of a γ‐secretase radiotracer in mammalian brain by Patel, Shil, O'Malley, Stacey, Connolly, Brett, Liu, Wensheng, Hargreaves, Richard, Sur, Cyrille, Gibson, Raymond E.

“…Inhibition of γ‐secretase is a potential therapeutic target for Alzheimer's disease (AD). The present studies have characterized the in vitro properties of a…”
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Screening cascade and development of potential Positron Emission Tomography radiotracers for mGluR5: in vitro and in vivo characterization by Patel, Shil, Ndubizu, Obinna, Hamill, Terence, Chaudhary, A, Burns, H Donald, Hargreaves, R, Gibson, Raymond E

“…Use of mGluR5 receptor radiotracers to determine whether an in vitro binding assay is able to predict how good a radiotracer is likely to be in imaging…”
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Positron emission tomography neuroreceptor imaging as a tool in drug discovery, research and development by Burns, H Donald, Hamill, Terence G, Eng, Wai-si, Francis, Barbara, Fioravanti, Christine, Gibson, Raymond E

“…Improved communication and cooperation between researchdriven drug companies and academic positron emmision tomography (PET) centers, coupled with improvements…”
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An in vitro assay for predicting successful imaging radiotracers by Patel, Shil, Hamill, Terence, Hostetler, Eric, Burns, H Donald, Gibson, Raymond E

“…To develop an in vitro binding assay able to predict whether a radiolabel is likely to be a useful clinical tracer for positron emission tomography (PET)…”
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Molecular Imaging, Principles and Practices by Gibson, Raymond E

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A cell-based radioligand binding assay for farnesyl: protein transferase inhibitors by Lobell, Robert B, Davide, Joseph P, Kohl, Nancy E, Burns, H Donald, Eng, Wai-Si, Gibson, Raymond E

“…Farnesyl:protein transferase (FPTase) catalyzes the covalent addition of the isoprenyl moiety of farnesylpyrophosphate to the C-terminus of the Ras oncoprotein…”
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Radioiodinated α1-adrenergic receptor ligands by Hamill, Terence G., Burns, H. Donald, Gibson, Raymond E.

“…The synthesis and preliminary characterization of three radioiodinated α1‐adrenergic receptor ligands [125I]5a–c are described. These tracers are analogs of…”
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Radioiodinated endothelin-1: a radiotracer for imaging endothelin receptor distribution and occupancy by Gibson, Raymond E, Fioravanti, Christine, Francis, Barbara, Burns, H.Donald

“…Endothelin (ET) is one of the most potent vasoconstrictors known. Recently, ET has been implicated in various diseases, e.g., acute renal failure and…”
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Muscarinic Acetylcholine Receptors in Alzheimer's Disease: In Vivo Imaging With Iodine 123—Labeled 3-Quinuclidinyl-4-Iodobenzilate and Emission Tomography by Holman, B. Leonard, Gibson, Raymond E, Hill, Thomas C, Eckelman, William C, Albert, Marilyn, Reba, Richard C

“…In vivo imaging of muscarinic acetylcholine receptor binding function in a patient with Alzheimer's disease, using single-photon emission computed tomography…”
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In Vivo Labeling of Angiotensin II Receptors with a Carbon-11-Labeled Selective Nonpeptide Antagonist by Kim, Sang Eun, Scheffel, Ursula, Szabo, Zsolt, Burns, H. Donald, Gibson, Raymond E, Ravert, Hayden T, Mathews, William B, Hamill, Terence G, Dannals, Robert

“…Angiotensin II (ANG II) initiates a variety of physiological effects by binding to high affinity receptors. Two ANG II receptor subtypes, AT1 and AT2, have…”
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Characterization of specific binding of [formula omitted]L-762,459, a selective α1A-adrenoceptor radioligand to rat and human tissues by O'Malley, Stacey S, Chen, Tsing B, Francis, Barbara E, Gibson, Raymond E, Burns, H.Donald, DiSalvo, Jerry, Bayne, Marvin L, Wetzel, John M, Nagarathnam, Dhanapalan, Marzabadi, Mohammad, Gluchowski, Charles, Chang, Raymond S.L

“…L-762,459…”
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External Imaging of Cerebral Muscarinic Acetylcholine Receptors by Eckelman, William C., Reba, Richard C., Rzeszotarski, Waclaw J., Gibson, Raymond E., Hill, Thomas, Holman, B. Leonard, Budinger, Thomas, Conklin, James J., Eng, Robert, Grissom, Michael P.

“…A radioiodinated ligand that binds to muscarinic acetylcholine receptors was shown to distribute in the brain by a receptor-mediated process. With…”
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