Search Results - "Sheardown, M"

Functional characterization of agonists at recombinant human 5‐HT2A, 5‐HT2B and 5‐HT2C receptors in CHO‐K1 cells by Porter, R H P, Benwell, K R, Lamb, H, Malcolm, C S, Allen, N H, Revell, D F, Adams, D R, Sheardown, M J

“…The goal of this study was to characterize the agonist pharmacology of human 5‐HT2A, 5‐HT2B and 5‐HT2C (VSV) receptors expressed in CHO‐K1 (Chinese hamster…”
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Regional changes in interstitial K+ and Ca2+ levels following cortical compression contusion trauma in rats by Nilsson, P, Hillered, L, Olsson, Y, Sheardown, M J, Hansen, A J

“…Brain trauma is associated with acute functional impairment and neuronal injury. At present, it is unclear to what extent disturbances in ion homeostasis are…”
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Sulfate content and specific glycosaminoglycan backbone of perlecan are critical for perlecan's enhancement of islet amyloid polypeptide (amylin) fibril formation by CASTILLO, G. M, CUMMINGS, J. A, WENHUA YANG, JUDGE, M. E, SHEARDOWN, M. J, RIMVALL, K, HANSEN, J. B, SNOW, A. D

“…Sulfate content and specific glycosaminoglycan backbone of perlecan are critical for perlecan's enhancement of islet amyloid polypeptide (amylin) fibril…”
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2,3-Dihydroxy-6-nitro-7-sulfamoyl-benzo(F)quinoxaline: A Neuroprotectant for Cerebral Ischemia by Sheardown, Malcolm J., Nielsen, Elsebet Ø., Hansen, Anker J., Jacobsen, Poul, Honoré, Tage

“…2,3-Dihydroxy-6-nitro-7-sulfamoyl-benzo(F)quinoxaline (NBQX) is an analog of the quinoxalinedione antagonists to the non-N-methyl-D-aspartate (non-NMDA)…”
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AMPA, but not NMDA, receptor antagonism is neuroprotective in gerbil global ischaemia, even when delayed 24 h by Sheardown, M J, Suzdak, P D, Nordholm, L

“…The selective alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) antagonist 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo(f)quinoxaline (NBQX) and the…”
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The muscarinic receptor agonist xanomeline has an antipsychotic-like profile in the rat by Stanhope, K J, Mirza, N R, Bickerdike, M J, Bright, J L, Harrington, N R, Hesselink, M B, Kennett, G A, Lightowler, S, Sheardown, M J, Syed, R, Upton, R L, Wadsworth, G, Weiss, S M, Wyatt, A

“…The muscarinic receptor agonist xanomeline was examined and compared with the antipsychotics clozapine and/or haloperidol in the following in vivo rat models:…”
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Xanomeline: a novel muscarinic receptor agonist with functional selectivity for M1 receptors by Shannon, H E, Bymaster, F P, Calligaro, D O, Greenwood, B, Mitch, C H, Sawyer, B D, Ward, J S, Wong, D T, Olesen, P H, Sheardown, M J, Swedberg, M D, Suzdak, P D, Sauerberg, P

“…Xanomeline [3(3-hexyloxy-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1- methylpyridine] has been evaluated as a muscarinic receptor agonist. In vitro, xanomeline…”
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The triggering of spreading depression in the chicken retina: a pharmacological study by Sheardown, M J

“…Spreading depression (S.D.) can be reproducibly evoked in the retinas of 3- to 6-day-old chickens by K+ ions, N-methyl-D-aspartate (NMDA), kainate (KA), and…”
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Xanomeline compared to other muscarinic agents on stimulation of phosphoinositide hydrolysis in vivo and other cholinomimetic effects by Bymaster, Frank P., Carter, Petra A., Peters, Steven C., Zhang, Wei, Ward, John S., Mitch, Charles H., Calligaro, David O., Whitesitt, Celia A., DeLapp, Neil, Shannon, Harlan E., Rimvall, Karin, Jeppesen, Lone, Sheardown, Malcolm J., Fink-Jensen, Anders, Sauerberg, Per

“…Activation of muscarinic m1 receptors which are coupled to the phosphoinositide (PI) second messenger transduction system is the initial objective of…”
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Muscarinic receptor agonists decrease cocaine self-administration rates in drug-naive mice by Rasmussen, Thøger, Sauerberg, Per, Nielsen, Erik B, Swedberg, Michael D.B, Thomsen, Christian, Sheardown, Malcolm J, Jeppesen, Lone, Calligaro, David O, DeLapp, Neil W, Whitesitt, Celia, Ward, John S, Shannon, Harlan E, Bymaster, Frank P, Fink-Jensen, Anders

“…(5 R,6 R)-6-(3-Propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[3.2.1]octane (PTAC) is a selective muscarinic receptor ligand. The compound exhibits high…”
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Novel functional M1 selective muscarinic agonists. Synthesis and structure-activity relationships of 3-(1,2,5-thiadiazolyl)-1,2,5,6-tetrahydro-1-methylpyridines by Sauerberg, Per, Olesen, Preben H, Nielsen, Susanne, Treppendahl, Svend, Sheardown, Malcolm J, Honore, Tage, Mitch, Charles H, Ward, John S, Pike, Andrew J

“…A series of novel 3-(3-substituted-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahydro- 1-methylpyridines (substituted-TZTP; 5a-l, 7a-h, 8, 9c-n, 11, 13j) were…”
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Unexpected antipsychotic-like activity with the muscarinic receptor ligand (5 R,6 R)6-(3-propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[3.2.1]octane by Bymaster, Frank P, Shannon, Harlan E, Rasmussen, Kurt, Delapp, Neil W, Mitch, Charles H, Ward, John S, Calligaro, David O, Ludvigsen, Thomas S, Sheardown, Malcolm J, Olesen, Preben H, Swedberg, Michael D.B, Sauerberg, Per, Fink-Jensen, Anders

“…(5 R,6 R) 6-(3-propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[3.2.1]octane (PTAC) is a potent muscarinic receptor ligand with high affinity for central…”
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The triggering of spreading depression in the chick retina by nicotinic receptor agonists by Sheardown, Malcolm J

“…Spreading depression was evoked in vitro in retinas of 3–6 day old chickens by the nicotinic cholinergic agonists nicotine and cytisine. The response was…”
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The pharmacology of AMPA receptors and their antagonists by Sheardown, M J

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Muscarinic Agonists with Antipsychotic-like Activity:  Structure−Activity Relationships of 1,2,5-Thiadiazole Analogues with Functional Dopamine Antagonist Activity by Sauerberg, Per, Jeppesen, Lone, Olesen, Preben H, Rasmussen, Thøger, Swedberg, Michael D. B, Sheardown, Malcolm J, Fink-Jensen, Anders, Thomsen, Christian, Thøgersen, Henning, Rimvall, Karin, Ward, John S, Calligaro, David O, DeLapp, Neil W, Bymaster, Frank P, Shannon, Harlan E

“…Muscarinic agonists were tested in two models indicative of clinical antipsychotic activity:  conditioned avoidance responding (CAR) in rats and inhibition of…”
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N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects by Knutsen, L J, Lau, J, Petersen, H, Thomsen, C, Weis, J U, Shalmi, M, Judge, M E, Hansen, A J, Sheardown, M J

“…The synthesis and pharmacological profile of a series of neuroprotective adenosine agonists are described. Novel A(1) agonists with potent central nervous…”
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Metabotropic glutamate receptor agonists reduce epileptiform activity in the rat cortex by Sheardown, M J

“…Slices of rat cingulate cortex, when incubated in magnesium-free medium, produce spontaneous epileptiform spikes. Here it is demonstrated that the metabotropic…”
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Neurochemical effects of the M1 muscarinic agonist xanomeline (LY246708/NNC11-0232) by Bymaster, F P, Wong, D T, Mitch, C H, Ward, J S, Calligaro, D O, Schoepp, D D, Shannon, H E, Sheardown, M J, Olesen, P H, Suzdak, P D, Swedberg, M D, Sauerberg, P

“…Xanomeline [3(3-hexyloxy-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1-me thylpyridine)] was evaluated in vivo in rat brain for effects on neurotransmitter…”
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1,2,5-Thiadiazole Analogues of Aceclidine as Potent m1 Muscarinic Agonists by Ward, John S, Merritt, Leander, Calligaro, David O, Bymaster, Franklin P, Shannon, Harlan E, Mitch, Charles H, Whitesitt, Celia, Brunsting, David, Sheardown, Malcolm J, Olesen, Preben H, Swedberg, Michael D. B, Jeppesen, Lone, Sauerberg, Per

“…The acetyl group of the muscarinic agonist aceclidine 4 was replaced by various 1,2,5-thiadiazoles to provide a new series of potent m1 muscarinic agonists 17…”
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Muscarinic agonists exhibit functional dopamine antagonism in unilaterally 6-OHDA lesioned rats by Fink-Jensen, Anders, Kristensen, Peter, Shannon, Harlan E, Calligaro, David O, Delapp, Neil W, Whitesitt, Cilia, Ward, John S, Thomsen, Christian, Rasmusseen, Thøger, Sheardown, Malcolm J, Jeppesen, Lone, Sauerberg, Per, Bymaster, Frank P

“…(5R,6R) 6-(3-P-ROPYLTHIO-1,2,5-THIADIAZOL-4-YL)-1-AZABICYCLO[3.2.1]OCTANE (PTAC) is a selective muscarinic ligand with high affinity for central muscarinic…”
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