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

Abstract：

: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.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Bräuner-Osborne H,Hermit MB,Nielsen B,Krogsgaard-Larsen P,Johansen TN

doi

10.1016/s0014-2999(00)00625-7

keywords:

subject

Has Abstract

pub_date

2000-10-06 00:00:00

pages

41-4

issue

1

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(00)00625-7

journal_volume

406

pub_type

杂志文章

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