Results 251 to 260 of about 75,386 (292)
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Bioorganic & Medicinal Chemistry Letters, 1997
Abstract The synthesis of three novel 4-carboxyphenylglycine derivatives is described. 2-Methyl substituents increase the antagonist potency compared to (S)-4CPG at mGluR1 receptors. Resolution of compound 1 showed that the activity resided in the (+)-isomer LY367385.
Barry P. Clark +4 more
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Abstract The synthesis of three novel 4-carboxyphenylglycine derivatives is described. 2-Methyl substituents increase the antagonist potency compared to (S)-4CPG at mGluR1 receptors. Resolution of compound 1 showed that the activity resided in the (+)-isomer LY367385.
Barry P. Clark +4 more
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The Journal of Pharmacology and Experimental Therapeutics, 1997
Metabotropic glutamate receptors (mGluRs) are a family of glutamate receptors that are coupled to a variety of second messenger systems through GTP-binding proteins. Of the eight subtypes cloned to date, mGluR1 and mGluR5 are coupled to phosphoinositide hydrolysis in expression systems, and both are activated by the glutamate analogue 1 ...
D S, Chung +3 more
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Metabotropic glutamate receptors (mGluRs) are a family of glutamate receptors that are coupled to a variety of second messenger systems through GTP-binding proteins. Of the eight subtypes cloned to date, mGluR1 and mGluR5 are coupled to phosphoinositide hydrolysis in expression systems, and both are activated by the glutamate analogue 1 ...
D S, Chung +3 more
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Acta Crystallographica Section C Crystal Structure Communications, 1997
The title compound, (+)-MCPG [(+)-alpha-(4-carboxyphenyl)-alpha-methylglycine, C10H11NO4], is an antagonist at certain subtypes of metabotropic glutamate (mGlu) receptors. (+)-MCPG has gained widespread acceptance as a tool for probing the physiological role of mGlu receptors in the central nervous system.
C, Wilson +4 more
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The title compound, (+)-MCPG [(+)-alpha-(4-carboxyphenyl)-alpha-methylglycine, C10H11NO4], is an antagonist at certain subtypes of metabotropic glutamate (mGlu) receptors. (+)-MCPG has gained widespread acceptance as a tool for probing the physiological role of mGlu receptors in the central nervous system.
C, Wilson +4 more
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Neuroscience, 1998
Previous work has shown that responses of thalamic neurons in vivo to the metabotropic glutamate receptor agonists 1S,3R-aminocyclopentane-1,3-dicarboxylate and S-3,5-dihydroxyphenylglycine can be reduced by a variety of phenylglycine antagonists. Responses of thalamic neurons to noxious thermal somatosensory stimuli were reduced in parallel by these ...
Salt, T. E., Turner, J. P.
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Previous work has shown that responses of thalamic neurons in vivo to the metabotropic glutamate receptor agonists 1S,3R-aminocyclopentane-1,3-dicarboxylate and S-3,5-dihydroxyphenylglycine can be reduced by a variety of phenylglycine antagonists. Responses of thalamic neurons to noxious thermal somatosensory stimuli were reduced in parallel by these ...
Salt, T. E., Turner, J. P.
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European Journal of Pharmacology: Molecular Pharmacology, 1993
Two phenylglycine derivates, (S)-4-carboxyphenylglycine and (RS)-alpha-methyl-4-carboxyphenylglycine, competitively antagonised (1S,3R)-1-aminocyclopentane-1,3-dicarboxylate (ACPD)-stimulated phosphoinositide hydrolysis in rat cerebral cortical slices.
S A, Eaton +9 more
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Two phenylglycine derivates, (S)-4-carboxyphenylglycine and (RS)-alpha-methyl-4-carboxyphenylglycine, competitively antagonised (1S,3R)-1-aminocyclopentane-1,3-dicarboxylate (ACPD)-stimulated phosphoinositide hydrolysis in rat cerebral cortical slices.
S A, Eaton +9 more
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Neuropharmacology, 2017
In cerebellar cortex, mGlu4 receptors located on parallel fibers play an essential role in normal motor function, but the molecular mechanisms involved are not yet completely understood. Using a strategy combining biochemical and electrophysiological approaches in the rodent cerebellum, we demonstrate that presynaptic mGlu4 receptors control synaptic ...
Chardonnet, Solenne +14 more
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In cerebellar cortex, mGlu4 receptors located on parallel fibers play an essential role in normal motor function, but the molecular mechanisms involved are not yet completely understood. Using a strategy combining biochemical and electrophysiological approaches in the rodent cerebellum, we demonstrate that presynaptic mGlu4 receptors control synaptic ...
Chardonnet, Solenne +14 more
openaire +3 more sources
An mGlu4‐Positive Allosteric Modulator Alleviates Parkinsonism in Primates
Movement Disorders, 2018Background: Levodopa remains the gold‐standard treatment for PD. However, it becomes less effective as the disease progresses and produces debilitating side effects, such as motor fluctuations and l‐dopa‐induced dyskinesia.
D. Charvin +9 more
semanticscholar +1 more source
European Journal of Pharmacology, 1999
Agonists at group III glutamate metabotropic receptors, such as L-serine-O-phosphate, have pro- and anti-convulsant activities in rodent models. We have used intracerebroventricular administration to test a novel group III agonist, (R,S)-4-phosphonophenylglycine (PPG), that is preferential for mglu(8), against sound-induced seizures in DBA/2 mice ...
A G, Chapman +3 more
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Agonists at group III glutamate metabotropic receptors, such as L-serine-O-phosphate, have pro- and anti-convulsant activities in rodent models. We have used intracerebroventricular administration to test a novel group III agonist, (R,S)-4-phosphonophenylglycine (PPG), that is preferential for mglu(8), against sound-induced seizures in DBA/2 mice ...
A G, Chapman +3 more
openaire +2 more sources