Format

Send to

Choose Destination
See comment in PubMed Commons below
Bioorg Med Chem. 1995 Feb;3(2):129-41.

Structure-activity relationships in a series of 3-sulfonylamino-2-(1H)-quinolones, as new AMPA/kainate and glycine antagonists.

Author information

1
Institut de Recherches Servier, Suresnes, France.

Abstract

This paper describes the design and synthesis of a new class of molecules, the 3-sulfonylamino-2-(1H)-quinolones, which are potent and selective antagonists at both the AMPA/kainate site as well as at the NMDA-associated glycine site. The molecules were characterized by their binding affinities to rat cortical membranes and by electrophysiology on Xenopus oocytes injected with mRNA isolated from rat cerebral cortex. The most potent compound 61 has an IC50 of 0.09 microM for binding at the AMPA/kainate site, and 0.16 microM in oocyte electrophysiology.

PMID:
7540921
[Indexed for MEDLINE]
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science
    Loading ...
    Support Center