Competitive antagonism at metabotropic glutamate receptors by (S)-4-carboxyphenylglycine and (RS)-alpha-methyl-4-carboxyphenylglycine.
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. The same phenylglycine derivatives selectively antagonized ACPD-induced depolarization in neonatal rat spinal motoneurones and rate thalamic neurones relative to depolarization or excitation induced by N-methyl-D-aspartate (NMDA) or alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA). Both phenylglycine derivatives also selectively depressed synaptic excitation in thalamic neurones evoked by noxious thermal stimuli, without affecting the synaptic stimulation of the same cells by non-noxious stimuli.
Eaton
S A
SA
Department of Visual Science, Institute of Ophthalmology, London, UK.
Jane
D E
DE
Jones
P L
PL
Porter
R H
RH
Pook
P C
PC
Sunter
D C
DC
Udvarhelyi
P M
PM
Roberts
P J
PJ
Salt
T E
TE
Watkins
J C
JC
D000818:Animals; D000831:Animals, Newborn; D001565:Benzoates / Q000494:pharmacology*; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D003515:Cycloleucine / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors / Q000494:pharmacology; D018691:Excitatory Amino Acid Antagonists; D005998:Glycine / Q000031:analogs & derivatives* / Q000494:pharmacology; D066298:In Vitro Techniques; D009046:Motor Neurons / Q000187:drug effects; D016202:N-Methylaspartate / Q000494:pharmacology; D010716:Phosphatidylinositols / Q000378:metabolism; D051381:Rats; D013116:Spinal Cord / Q000166:cytology / Q000187:drug effects; D013569:Synapses / Q000187:drug effects; D013788:Thalamus / Q000166:cytology / Q000187:drug effects
D001565:Benzoates; D018691:Excitatory Amino Acid Antagonists; D010716:Phosphatidylinositols; D003515:Cycloleucine; C036361:1-amino-1,3-dicarboxycyclopentane; C079694:alpha-methyl-4-carboxyphenylglycine; D016202:N-Methylaspartate; C079693:4-carboxyphenylglycine; D005998:Glycine