SCH 58261 (an adenosine A(2A) receptor antagonist) reduces, only at low doses, K(+)-evoked glutamate release in the striatum.
The aim of the present work was to determine whether systemic administration of the adenosine A(2A) receptor antagonist, SCH 58261 (7-(2-phenylethyl)-5-amino-2-(2-furyl)-pyrazolo-[4,3-e]-1,2,4,triazolo[1,5-c]pyrimidine), could modulate striatal glutamate outflow in the rat. Microdialysis experiments were performed in male Wistar rats implanted with microdialysis probes in the striatum. Pretreatment (15 min before) with SCH 58261 (0.01 and 0.1, but not 1 mg/kg intraperitoneally) significantly prevented K(+)-stimulated glutamate release. These results suggest that SCH 58261 could possess neuroprotective effects in the low dose range, while, at higher doses, the occurrence of additional mechanisms may limit the neuroprotective potential of this drug.
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Department of Pharmacology, Istituto Superiore di Sanità, Viale Regina Elena, 299, 00161, Rome, Italy.
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D000818:Animals; D003342:Corpus Striatum / Q000187:drug effects* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D018698:Glutamic Acid / Q000187:drug effects* / Q000378:metabolism; D008297:Male; D017551:Microdialysis; D018696:Neuroprotective Agents / Q000494:pharmacology*; D011188:Potassium / Q000494:pharmacology*; D058915:Purinergic P1 Receptor Antagonists; D011743:Pyrimidines / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D043705:Receptor, Adenosine A2A; D013997:Time Factors; D014230:Triazoles / Q000494:pharmacology*
C098657:5-amino-7-(2-phenylethyl)-2-(2-furyl)pyrazolo(4,3-e)-1,2,4-triazolo(1,5-c)pyrimidine; D018696:Neuroprotective Agents; D058915:Purinergic P1 Receptor Antagonists; D011743:Pyrimidines; D043705:Receptor, Adenosine A2A; D014230:Triazoles; D018698:Glutamic Acid; D011188:Potassium