Forskning ved Københavns Universitet - Københavns Universitet

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A new structural class of subtype-selective inhibitor of cloned excitatory amino acid transporter, EAAT2

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We have studied the pharmacological effects of (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) and the enantiomers of (RS)-2-amino-3-(3-hydroxy-1,2, 5-thiadiazol-4-yl)propionic acid (TDPA) on cloned human excitatory amino acid transporter subtypes 1, 2 and 3 (EAAT1-3) expressed in Cos-7 cells. Whereas AMPA and (R)-TDPA were both inactive as inhibitors of [3H]-(R)-aspartic acid uptake on all three EAAT subtypes, (S)-TDPA was shown to selectively inhibit uptake by EAAT2 with a potency equal to that of the endogenous ligand (S)-glutamic acid. (S)-TDPA thus represents a new structural class of EAAT2 inhibitor that will serve as a lead for the design of EAAT selective inhibitors.
OriginalsprogEngelsk
TidsskriftEuropean Journal of Pharmacology
Vol/bind406
Udgave nummer1
Sider (fra-til)41-4
ISSN0014-2999
StatusUdgivet - 6 okt. 2000

ID: 45596078