Vinpocetine preferentially antagonizes quisqualate/AMPA receptor responses: evidence from release and ligand binding studies.
The effect of vinpocetine on excitatory amino acid receptors was examined in the rat brain by two different biochemical approaches. In release experiments with striatal slices, vinpocetine reduced the efflux of dopamine and acetylcholine evoked by glutamate, quisqualate and N-methyl-D-aspartate (NMDA), but not that evoked by kainate. In binding experiments with cortical membranes, vinpocetine reduced the binding of [3H]2-amino-3-3-hydroxy-s-methylisoxasole-4-yl-propionic acid ([3H]AMPA), a quisqualate partial agonist, in an incomplete manner, but failed to influence the binding of [3H]kainate and [3H]3-(2-carboxypyperazine-4-yl)-propyl-1-phosphonic acid ([3H]CPP), an NMDA agonist. These findings suggest that vinpocetine is a quisqualate/AMPA antagonist of some specificity and selectivity.
Pharmacological Research Centre, Gedeon Richter Ltd., Budapest, Hungary.
B
B
Kiss
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NS
Cai
S L
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Erdö
D000109:Acetylcholine / Q000378:metabolism; D000818:Animals; D001667:Binding, Competitive; D002540:Cerebral Cortex / Q000378:metabolism / Q000648:ultrastructure; D003342:Corpus Striatum / Q000033:anatomy & histology / Q000187:drug effects / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism; D005971:Glutamates / Q000494:pharmacology; D018698:Glutamic Acid; D007051:Ibotenic Acid / Q000031:analogs & derivatives / Q000378:metabolism; D066298:In Vitro Techniques; D007608:Kainic Acid / Q000378:metabolism / Q000494:pharmacology; D008297:Male; D008566:Membranes / Q000378:metabolism / Q000648:ultrastructure; D016202:N-Methylaspartate / Q000494:pharmacology; D016318:Quisqualic Acid / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D018091:Receptors, AMPA; D017459:Receptors, Amino Acid; D011956:Receptors, Cell Surface / Q000037:antagonists & inhibitors / Q000145:classification / Q000378:metabolism; D018092:Kainic Acid Receptors; D016194:Receptors, N-Methyl-D-Aspartate / Q000378:metabolism; D017981:Receptors, Neurotransmitter / Q000037:antagonists & inhibitors* / Q000378:metabolism / Q000502:physiology; D014316:Tritium; D014748:Vinca Alkaloids / Q000378:metabolism / Q000494:pharmacology*; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
D000109:Acetylcholine; D004298:Dopamine; D005971:Glutamates; D018698:Glutamic Acid; D007051:Ibotenic Acid; D007608:Kainic Acid; D016202:N-Methylaspartate; D016318:Quisqualic Acid; D018091:Receptors, AMPA; D017459:Receptors, Amino Acid; D011956:Receptors, Cell Surface; D018092:Kainic Acid Receptors; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter; D014316:Tritium; D014748:Vinca Alkaloids; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid; C013983:vinpocetine