Výsledky vyhledávání - "K. L. Saywell"

4-Substituted-3-phenylquinolin-2(1H)-ones: Acidic and Nonacidic Glycine SiteN-Methyl-d-aspartate Antagonists withinVivoActivity

Autor: Sarah Grimwood, Paul D. Leeson, John A. Kemp, Christopher Moyes, Mark D. Tricklebank, Robert W. Carling, Kevin W. Moore, Raymond Baker, Alan C. Foster, George R. Marshall, Martin L. Hudson, K. L. Saywell, Duncton Matthew A J

Publikováno v: Journal of Medicinal Chemistry. 40:754-765

4-Substituted-3-phenylquinolin-2(1H)-ones have been synthesized and evaluated in vitro for antagonist activity at the glycine site on the NMDA (N-methyl-D-aspartate) receptor and in vivo for anticonvulsant activity in the DBA/2 strain of mouse in an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5da4422e5a6789e47a409d6681a5a872
https://doi.org/10.1021/jm9605492

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5,6,7,8-Tetrahydroquinolones as antagonists at the glycine site of the NMDA receptor

Autor: Paul D. Leeson, George R. Marshall, Sarah Grimwood, K. L. Saywell, Michael Rowley

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:2089-2092

The effect of reducing the benzo ring of a series of 4-hydroxyquinolone Glycine/NMDA antagonists is described. It is important that the ring be present, but not that it is aromatic. Provided that the correct lipophilic interactions are present, high

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::87596aac8ed7910ecd82551e334ba993
https://doi.org/10.1016/0960-894x(95)00374-3

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Identification of 3,5-Dihydro-2-aryl-1H-pyrazolo[3,4-c]quinoline-1,4(2H)-diones as Novel High-Affinity Glycine Site N-Methyl-D-aspartate Antagonists

Autor: K. L. Saywell, Richard G. Ball, Sarah Grimwood, Angus Murray Macleod, Cheryl L. Barton, Linda J. Bristow, George R. Marshall

Publikováno v: Journal of Medicinal Chemistry. 38:2239-2243

Almost all of the existing known antagonists at the glycine site of the N-methyl-D-aspartate (NMDA) receptor have a low propensity for crossing the blood-brain barrier. It has been suggested that in many cases this may be due to the presence of a car

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a47166e055bac940de710603f313c8d
https://doi.org/10.1021/jm00012a024

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The anticonvulsant and behavioural profile of L-687,414, a partial agonist acting at the glycine modulatory site on the N-methyl-D-aspartate (NMDA) receptor complex

Autor: L. Singh, Linda J. Bristow, Paul D. Leeson, Brian John Williams, Peter H. Hutson, Mark D. Tricklebank, F. D. Tattersall, Michael Rowley, L. Thorn, K. L. Saywell

Publikováno v: British Journal of Pharmacology. 113:729-736

1. The anticonvulsant and behavioural effects of the glycine/NMDA receptor partial agonist, L-687,414 (R(+)-cis-beta-methyl-3-amino-1-hydroxypyrrolid-2-one) have been investigated in rodents. 2. L-687,414 dose-dependently antagonized seizures induced

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b0008ac0b50d7ca3fca8462b14ada314
https://doi.org/10.1111/j.1476-5381.1994.tb17054.x

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Anticonvulsant activity of glycine-site NMDA antagonists. 2. trans 2-carboxy-4-substituted tetrahydroquinolines

Autor: A M Moseley, John A. Kemp, Paul D. Leeson, Mark D. Tricklebank, George R. Marshall, Sarah Grimwood, Robert W. Carling, K. L. Saywell, Alan C. Foster, Julian D. Smith

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 3:65-70

Anticonvulsant activity has been optimized in a series of glycine-site NMDA antagonists based on 2-carboxy tetrahydroquinoline, leading to the benzylamine 7 (L-690,590), its methyl ester prodrug 13 (L-691,470) and the phenylalanine 8 (L-696,833) whic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a89e339452c78232fba8d73424c70a2a
https://doi.org/10.1016/s0960-894x(00)80093-1

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ChemInform Abstract: 4-Substituted-3-phenylquinolin-2(1H)-ones: Acidic and Nonacidic Glycine Site N-Methyl-D-aspartate Antagonists with in vivo Activity

Autor: Martin L. Hudson, George R. Marshall, Robert W. Carling, Mark D. Tricklebank, Alan C. Foster, Raymond Baker, John A. Kemp, Christopher Moyes, Kevin W. Moore, K. L. Saywell, Sarah Grimwood, Duncton Matthew A J, Paul D. Leeson

Publikováno v: ChemInform. 28

4-Substituted-3-phenylquinolin-2(1H)-ones have been synthesized and evaluated in vitro for antagonist activity at the glycine site on the NMDA (N-methyl-d-aspartate) receptor and in vivo for anticonvulsant activity in the DBA/2 strain of mouse in an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e097bcb311bb4807369ad9879fe38042
https://doi.org/10.1002/chin.199725135

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2-carboxy indolines and indoles as potential glycine/NMDA antagonists: effect of five-membered ring conformation on affinity

Autor: Michael Rowley, K. L. Saywell, Paul D. Leeson, Sarah Grimwood, Alan C. Foster

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 2:1627-1630

2-Carboxy indolines were synthesised as potential antagonists at the glycine site of the NMDA receptor, based on a pharmacophore developed from other series. None of the indolines had significant potency, possibly due to the lack of coplanarity of th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::571ad44da95df30a9e357041301c0f80
https://doi.org/10.1016/s0960-894x(00)80444-8

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Rat Strain Differences in the Ability to Disrupt Sensorimotor Gating Are Limited to the Dopaminergic System, Specific to Prepulse Inhibition, and Unrelated to Changes in Startle Amplitude or Nucleus Accumbens Dopamine Receptor Sensitivity

Autor: Mark D. Tricklebank, Gene G. Kinney, Lynn O. Wilkinson, K. L. Saywell

Previous studies indicate that a variety of pharmacological agents interfere with the prepulse inhibition of the acoustic startle (PPI) response including phencyclidine (PCP), 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), amphetamine, and apomo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61db410d58fe4fd3b5c69dbd5c111724
https://europepmc.org/articles/PMC6782328/

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Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists

Autor: John A. Kemp, K. L. Saywell, Alan P. Watt, Robert W. Carling, George R. Marshall, Alan C. Foster, Mark D. Tricklebank, Denise Rathbone, Raymond Baker, Michael Rowley, Janusz Jozef Kulagowski, Sarah Grimwood, Paul D. Leeson, Richard Hargreaves, Catherine Hurley, Graeme Irvine Stevenson

Publikováno v: Journal of medicinal chemistry. 40(25)

A major issue in designing drugs as antagonists at the glycine site of the NMDA receptor has been to achieve good in vivo activity. A series of 4-hydroxyquinolone glycine antagonists was found to be active in the DBA/2 mouse anticonvulsant assay, but

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::493ab3997ed9b6463372b3fdb43bb830
https://pubmed.ncbi.nlm.nih.gov/9406596

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