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Synthesis and receptor binding affinity of new selective GluR5 ligands.

Abstract：

:Two hybrid analogues of the kainic acid receptor agonists, 2-amino-3-(5-tert-butyl-3-hydroxy-4-isoxazolyl)propionic acid (ATPA) and (2S,4R)-4-methylglutamic acid ((2S,4R)-4-Me-Glu), were designed, synthesized, and characterized in radioligand binding assays using cloned ionotropic and metabotropic glutamic acid receptors. The (S)-enantiomers of E-4-(2,2-dimethylpropylidene)glutamic acid ((S)-1) and E-4-(3,3-dimethylbutylidene)glutamic acid ((S)-2) were shown to be selective and high affinity GluR5 ligands, with Ki values of 0.024 and 0.39 microM, respectively, compared to Ki values at GluR2 of 3.0 and 2.0 microM. respectively. Their affinities in the [3H]AMPA binding assay on native cortical receptors were shown to correlate with their GluR2 affinity rather than their GluR5 affinity. No affinity for GluR6 was detected (IC50 > 100 microM).

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Bunch L,Johansen TH,Bräuner-Osborne H,Stensbøl TB,Johansen TN,Krogsgaard-Larsen P,Madsen U

doi

10.1016/s0968-0896(00)00304-7

subject

Has Abstract

pub_date

2001-04-01 00:00:00

pages

875-9

issue

4

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(00)00304-7

journal_volume

9

pub_type

杂志文章

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