2,6-diisopropylphenol, a general anesthetic, inhibits glutamate action on rat synaptosomes.
2,6-diisopropylphenol (propofol), a general intravenous anesthetic, inhibits the glutamate-dependent Ca2+ entry in rat synaptosomes with an approximate IC50 of 3.0 x 10(-5) M. Propofol, at concentrations above 10(-6) M, also inhibits the ATP-dependent uptake of glutamate in the presence of Ca2+, with an approximate IC50 of 3.5 x 10(-5) M, while it only has a slight inhibitory effect on the release of glutamate. The ouabain-insensitive synaptosomal ATPase is strongly inhibited by propofol, with an IC50 of about 2.5 x 10(-6) M, at concentrations which do not affect the luciferase system.
Department of Biological Chemistry, University of Padova, Italy.
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Bianchi
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Battistin
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Galzigna
D000251:Adenosine Triphosphatases / Q000037:antagonists & inhibitors*; D000818:Animals; D001921:Brain / Q000378:metabolism*; D002118:Calcium / Q000378:metabolism* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005971:Glutamates / Q000378:metabolism / Q000494:pharmacology*; D018698:Glutamic Acid; D007700:Kinetics; D008297:Male; D010042:Ouabain / Q000494:pharmacology; D015742:Propofol / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism*
D005971:Glutamates; D018698:Glutamic Acid; D010042:Ouabain; D000251:Adenosine Triphosphatases; D002118:Calcium; D015742:Propofol