Results 281 to 290 of about 70,307 (362)
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Noncompetitive excitatory amino acid receptor antagonists
Trends in Pharmacological Sciences, 1990In the first article in this series, Watkins, Krogsgaard-Larsen and Honoré outlined the structure-activity requirements at the receptor sites for excitatory amino acids in the mammalian CNS. The postsynaptic depolarizing actions of glutamate are thought to be mediated by NMDA, AMPA and kainate receptors. Here David Lodge and Kenneth M.
D, Lodge, K M, Johnson
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Isomers of cyclazocine as excitatory amino acid antagonists
Neuropeptides, 1984Abstract As an N-methylaspartate antagonist on cat and frog spinal neurones, (−) cyclazocine was twice as potent as (+) cyclazocine. This stereoselectivity is similar to that of cyclazocine at sigma rather than at mu or kappa opiate receptors. Cyclazocine also reduced synaptic excitation in rat cortex.
D, Lodge +6 more
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Overview: Excitatory Amino Acid Antagonists
Current Opinion on Therapeutic Patents, 1992(1992). Overview: Excitatory Amino Acid Antagonists. Current Opinion on Therapeutic Patents: Vol. 2, No. 8, pp. 1201-1221.
Michael Rowley, Paul D Leeson
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Clinical Experience With Excitatory Amino Acid Antagonist Drugs
Stroke, 1995BackgroundExcitotoxic damage due to excess release of neuronal glutamate is hypothesized to play a pivotal role in the pathogenesis of focal cerebral ischemia. Drugs that antagonize excitatory amino acid function are consistently neuroprotective in preclinical models of stroke, and many are now entering clinical trials.SummaryAntagonists of theN-methyl-
K W, Muir, K R, Lees
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Agonists and antagonists for excitatory amino acid receptors
Trends in Neurosciences, 1987Abstract Behind the recent explosion of interest in the field, there lies a long period of relatively slow progress in the characterization of excitatory amino acid receptors. In this article, Jeff Watkins and Harry Olverman summarize the emergence of current ideas relating to receptor differentiation and describe some of the molecular features of ...
J.C. Watkins, H.J. Olverman
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Antagonists of excitatory amino acids and cyclic guanosine monophosphate in cerebellum
Neuropharmacology, 1982The excitatory amino acid analogues kainate, quisqualate, domoic acid, 4-fluoroglutamate, homocysteic acid and N-methylaspartate as well as the tremor-inducing drugs harmaline and oxotremorine all induced significant elevations in cyclic guanosine monophosphate (cGMP) levels in the cerebellum in vivo. The putative antagonists of excitatory amino acids,
P L, Wood +3 more
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Depression of decerebrate rigidity in the rat by antagonists of excitatory amino acids
Neuropharmacology, 1989Effects of intravenous antagonists of excitatory amino acids on decerebrate rigidity in the rat were examined. Kynurenate, ketamine, (4S, 5R)-4-(2-methylpropyl)-3-[3-(perhydroazepin-1-yl)propyl]-5-phenyl- 1,3- oxazolidin-2-one hydrochloride (MLV-6976), (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d] cyclo-hepten-5,10-imine maleate (MK-801), 3-((/-)-2 ...
H, Shinozaki, M, Ishida, Y, Goto
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Neuroprotective Actions of Excitatory Amino Acid Receptor Antagonists
1994Publisher Summary Postischemic neuronal degeneration is caused in part by overactivity of excitatory amino acid (EAA) neurotransmitter systems. Increases in extracellular glutamate levels result in glutamate receptor-mediated increases in postsynaptic intracellular calcium levels.
V L, Woodburn, G N, Woodruff
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Structure-activity relations of dipeptide antagonists of excitatory amino acids
Neuroscience, 1984Structure-activity relations of dipeptides related to gamma-D-glutamylglycine have been investigated with respect to the ability of these substances to antagonize depolarizing responses of frog motoneurones in vitro to N-methyl-D-aspartate, kainate and quisqualate.
A W, Jones, D A, Smith, J C, Watkins
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Excitatory Amino Acid Antagonists as Novel Anticonvulsants
1986The convulsant effect of application of dicarboxylic amino acids to the cortex was first reported by Hayashi (1954). This observation suggests that antagonists of excitation induced by amino acid neurotransmitters might be anticonvulsant agents in some forms of epilepsy. Some rather weak and indeterminate anticonvulsant effects of glutamic acid diethyl
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