Search Results - "Hargreaves, Richard J"

Translational PET imaging research by Hargreaves, Richard J, Rabiner, Eugenii A

“…Abstract The goal of any early central nervous system (CNS) drug development program is always to test the mechanism and not the molecule in order to support…”
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In vivo quantification of calcitonin gene-related peptide receptor occupancy by telcagepant in rhesus monkey and human brain using the positron emission tomography tracer [11C]MK-4232 by Hostetler, Eric D, Joshi, Aniket D, Sanabria-Bohórquez, Sandra, Fan, Hong, Zeng, Zhizhen, Purcell, Mona, Gantert, Liza, Riffel, Kerry, Williams, Mangay, O'Malley, Stacey, Miller, Patricia, Selnick, Harold G, Gallicchio, Steven N, Bell, Ian M, Salvatore, Christopher A, Kane, Stefanie A, Li, Chi-Chung, Hargreaves, Richard J, de Groot, Tjibbe, Bormans, Guy, Van Hecken, Anne, Derdelinckx, Inge, de Hoon, Jan, Reynders, Tom, Declercq, Ruben, De Lepeleire, Inge, Kennedy, W P, Blanchard, Rebecca, Marcantonio, Eugene E, Sur, Cyrille, Cook, Jacquelynn J, Van Laere, Koen, Evelhoch, Jeffrey L

“…Calcitonin gene-related peptide (CGRP) is a potent neuropeptide whose agonist interaction with the CGRP receptor (CGRP-R) in the periphery promotes…”
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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 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 bioluminescence imaging of β-cell function in obese-hyperglycemic [ob/ob] mice by Patel, Manishkumar, Gleason, Alexa, O'Malley, Stacey, Connolly, Brett, Suresch, Donna, Virostko, John, Phillips, Neil, Lin, Shu-An, Chen, Tsing-Bau, Klimas, Michael, Hargreaves, Richard J, Sur, Cyrille, Williams, Jr, David L, Powers, Alvin C, Bednar, Bohumil

“…Type 2 diabetes results from failure of the β-cells to compensate for increased insulin demand due to abnormal levels of metabolic factors. The ob/ob(lep-/-)…”
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Characteristic time courses of cortical and medullary sodium signals measured by noninvasive 23Na-MRI in rat kidney induced by furosemide by Liu, Haiying, Zhou, Dan, Garcia, Maria L., Kohler, Martin G., Shen, Xiaolan, Williams, Donald S., Klimas, Michael T., Hargreaves, Richard J., Kaczorowski, Gregory J.

“…Background To characterize regional kidney sodium response by MRI following NKCC2 inhibition. Methods Regional renal sodium signals were monitored…”
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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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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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From LBR-101 to Fremanezumab for Migraine by Bigal, Marcelo E., Rapoport, Alan M., Silberstein, Stephen D., Walter, Sarah, Hargreaves, Richard J., Aycardi, Ernesto

“…Calcitonin gene-related peptide (CGRP) is a neuropeptide of importance in migraine pathogenesis. Its central role in migraine was proven pharmacologically by…”
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Investigation of the species selectivity of a nonpeptide CGRP receptor antagonist using a novel pharmacodynamic assay by Hershey, James C., Corcoran, Halea A., Baskin, Elizabeth P., Salvatore, Christopher A., Mosser, Scott, Williams, Theresa M., Koblan, Kenneth S., Hargreaves, Richard J., Kane, Stefanie A.

“…The recent discovery of several nonpeptide CGRP antagonists have led to significant advances in our understanding of CGRP receptor pharmacology. Specifically,…”
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“It Ain’t Over ’til It’s Over” a The Search for Treatments and Cures for Alzheimer’s Disease by Hargreaves, Richard J

“…In the neuroscience landscape, there is no condition with higher unmet medical and societal need than Alzheimer's disease (AD). There are significant…”
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Rizatriptan has central antinociceptive effects against durally evoked responses by Cumberbatch, Michael J, Hill, Raymond G, Hargreaves, Richard J

“…The 5-HT 1B/1D receptor agonist rizatriptan constricts intracranial, extracerebral blood vessels, inhibits neurogenic vasodilation and extravasation in the…”
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Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives by Meurer, Laura C., Finke, Paul E., Owens, Karen A., Tsou, Nancy N., Ball, Richard G., Mills, Sander G., MacCoss, Malcolm, Sadowski, Sharon, Cascieri, Margaret A., Tsao, Kwei-Lan, Chicchi, Gary G., Egger, Linda A., Luell, Silvi, Metzger, Joseph M., MacIntyre, D. Euan, Rupniak, Nadia M.J., Williams, Angela R., Hargreaves, Richard J.

“…The optimization of a cyclopentane-based hNK1 antagonist scaffold will be discussed in the context of enhanced water-solubility, sub-nanomolar hNK1 binding…”
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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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Decision-making using fMRI in clinical drug development: revisiting NK-1 receptor antagonists for pain by Borsook, David, Upadhyay, Jaymin, Klimas, Michael, Schwarz, Adam J., Coimbra, Alexandre, Baumgartner, Richard, George, Edward, Potter, William Z., Large, Thomas, Bleakman, David, Evelhoch, Jeffrey, Iyengar, Smriti, Becerra, Lino, Hargreaves, Richard J.

“…► Reevaluate the failed NK-1RA story in the light of potential contributions functional imaging may contribute to go–no go decisions in drug development. ►…”
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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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Why Does Sleep Stop Migraine? by Bigal, Marcelo E., Hargreaves, Richard J.

“…The relationship between sleep and migraine headaches is complex. Changes in sleep patterns can trigger migraine attacks, and sleep disorders may be associated…”
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Addition of an NK1 receptor antagonist to an SSRI did not enhance the antidepressant effects of SSRI monotherapy: results from a randomized clinical trial in patients with major depressive disorder by Ball, William A., Snavely, Duane B., Hargreaves, Richard J., Szegedi, Armin, Lines, Christopher, Reines, Scott A.

“…Objective Aprepitant is a neurokinin 1 receptor antagonist approved for prevention of chemotherapy‐induced and post‐operative nausea and vomiting. Early…”
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A growth hormone secretagogue prevents ischemic-induced mortality independently of the growth hormone pathway in dogs with chronic dilated cardiomyopathy by Shen, You-Tang, Lynch, Joseph J, Hargreaves, Richard J, Gould, Robert J

“…To determine the functional role of growth hormone (GH) secretagogue in myocardium with ischemia, left ventricular (LV) pressure gauge, wall thickness…”
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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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