Výsledky vyhledávání - "A D, Medhurst"

Discovery of potent azaindazole leucine-rich repeat kinase 2 (LRRK2) inhibitors possessing a key intramolecular hydrogen bond - Part 2

Autor: Daniel G. Shore, Andrew D. Medhurst, Zachary Kevin Sweeney, Xingrong Liu, Andrew W. Gill, Edward G. McIver, John Moffat, Jason Drummond, Alan Beresford, Bryan K. Chan, Tracy Kleinheinz, Haitao Zhu, Huifen Chen, Anthony A. Estrada

Publikováno v: Bioorganicmedicinal chemistry letters. 29(4)

The discovery of disease-modifying therapies for Parkinson’s Disease (PD) represents a critical need in neurodegenerative medicine. Genetic mutations in LRRK2 are risk factors for the development of PD, and some of these mutations have been linked

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::037486ba107ae90cb34b8b5dd9f63986
https://pubmed.ncbi.nlm.nih.gov/30522953

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Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor

Publikováno v: ACS Medicinal Chemistry Letters. 4:85-90

The modulation of LRRK2 kinase activity by a selective small molecule inhibitor has been proposed as a potentially viable treatment for Parkinson's disease. By using aminopyrazoles as aniline bioisosteres, we discovered a novel series of LRRK2 inhibi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::79ca6d12fe121b38c5bfe4ca1517ec13
https://doi.org/10.1021/ml3003007

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Preservation of cortical histamine H3 receptors in ischemic vascular and mixed dementias

Autor: Gordon K. Wilcock, Margaret M. Esiri, Mitchell K.P. Lai, Andrew D. Medhurst, Jasinda H. Lee, Peter T.-H. Wong, Yuan Sheng, Christopher Chen

Publikováno v: Journal of the Neurological Sciences. 315:110-114

Aim: Histamine H3 receptor antagonists have been proposed as a novel therapeutic approach for the symptomatic treatment of Alzheimer's disease (AD). However, it is unclear whether there is a neurochemical basis for extending their potential use in va

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a15033d4ecbbd68930b5f4526141db3e
https://doi.org/10.1016/j.jns.2011.11.013

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Regional Differential Effects of the Novel Histamine H3 Receptor Antagonist 6-[(3-Cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide hydrochloride (GSK189254) on Histamine Release in the Central Nervous System of Freely Moving Rats

Autor: Andrew D. Medhurst, Maria Grazia Giovannini, Laura Della Corte, Patrizia Giannoni, Chiara Ballini, Patrizio Blandina, Maria Beatrice Passani

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 332:164-172

After oral administration, the nonimidazole histamine H3 receptor antagonist, 6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide hydrochloride (GSK189254), increased histamine release from the tuberomammillar

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fd2229c42b85137dd75fe7bf6d862f5d
https://doi.org/10.1124/jpet.109.158444

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H3 Receptor Antagonism Enhances NCAM PSA-Mediated Plasticity and Improves Memory Consolidation in Odor Discrimination and Delayed Match-to-Position Paradigms

Autor: Andrew D. Medhurst, Ciaran M. Regan, Claire Barry, Darren Scully, Alison Prendergast, Andrew G. Foley, Neil Upton

Publikováno v: Neuropsychopharmacology. 34:2585-2600

To further understand the procognitive actions of GSK189254, a histamine H(3) receptor antagonist, we determined its influence on the modulation of hippocampal neural cell adhesion molecule (NCAM) polysialylation (PSA) state, a necessary neuroplastic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe2cc82fa9745626ff7bdaf3aad9cada
https://doi.org/10.1038/npp.2009.89

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Relationship between microglial activation and dopaminergic neuronal loss in the substantia nigra: a time course study in a 6-hydroxydopamine model of Parkinson’s disease

Autor: Lauren Broom, David T. Dexter, Lilia Marinova-Mutafchieva, Andrew D. Medhurst, John B. Davis, Mona Sadeghian

Publikováno v: Journal of Neurochemistry. 110:966-975

Cellular interactions between activated microglia and degenerating neurons in in vivo models of Parkinson's disease are not well defined. This time course study assesses the dynamics of morphological and immunophenotypic properties of activated micro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e10311ce28cbf2cfd5ec4f054e68512d
https://doi.org/10.1111/j.1471-4159.2009.06189.x

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Differential effects of acute and repeat dosing with the H3 antagonist GSK189254 on the sleep-wake cycle and narcoleptic episodes in Ox−/− mice

Autor: Andrew D. Medhurst, Patricia Franco, Neil Upton, RX Guo, Jenny C. Roberts, Mei Zhang, JQ Feng, Régis Parmentier, S. H. Brown, Christelle Anaclet, Jean-Pierre Sastre, Jian-Sheng Lin, Colette Buda, G. Guidon

Publikováno v: British Journal of Pharmacology. 157:104-117

Background and purpose: Histamine H3 receptor antagonists are currently being evaluated in clinical trials for a number of central nervous system disorders including narcolepsy. These agents can increase wakefulness (W) in cats and rodents following

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1d24d14967252b6a3d392c22d081d846
https://doi.org/10.1111/j.1476-5381.2009.00205.x

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Autoradiographical imaging of PPARγ agonist effects on PBR/TSPO binding in TASTPM mice

Autor: Andrew D. Medhurst, Jennifer C. Roberts, John B. Davis, David Virley, Marion J. Perren, Sarah Friel, Shilina Roman, Jill C. Richardson, Alex J. Harper

Publikováno v: Experimental Neurology. 216:459-470

Chronic inflammation is known to occur in the brains of Alzheimer's Disease (AD) patients, including the presence of activated microglia close to amyloid plaques. We utilised real time autoradiography and immunohistochemistry to investigate microglia

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::554e24339561ef685c3bb36b4edce2a4
https://doi.org/10.1016/j.expneurol.2009.01.002

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Characterization of histamine H3 receptors in Alzheimer's Disease brain and amyloid over-expressing TASTPM mice

Autor: S. H. Brown, Jenny C. Roberts, J. Lee, Shilina Roman, Andrew D. Medhurst, C. P. L.-H. Chen, Mitchell K.P. Lai

Publikováno v: British Journal of Pharmacology. 157:130-138

Background and purpose: Histamine H3 receptor antagonists are currently being evaluated for their potential use in a number of central nervous system disorders including Alzheimer's Disease (AD). To date, little is known about the state of H3 recepto

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9ec438bd5fbe1fdadd27c056c09b52b5
https://doi.org/10.1111/j.1476-5381.2008.00075.x

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The PPARγ agonist pioglitazone is effective in the MPTP mouse model of Parkinson's disease through inhibition of monoamine oxidase B

Autor: Neil Upton, David Virley, Helen Chapman, Martin P. Vidgeon-Hart, Andrew D. Medhurst, Leann P. Quinn, M E Hows, Barry Crook

Publikováno v: British Journal of Pharmacology. 154:226-233

Background and purpose: The peroxisome proliferator-activated receptor-g (PPARg) agonist pioglitazone has previously been shown to attenuate dopaminergic cell loss in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mouse model of Parkinson’

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::59ade69cd1baf2af10434e18a932ba47
https://doi.org/10.1038/bjp.2008.78

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