@article{c633b3a06e8f11df928f000ea68e967b,
title = "Agonist discrimination between AMPA receptor subtypes",
abstract = "The lack of subtype-selective compounds for AMPA receptors (AMPA-R) led us to search for compounds with such selectivity. Homoibotenic acid analogues were investigated at recombinant GluR1o, GluR2o(R), GluR3o and GluR1o + 3o receptors expressed in Sf9 insect cells and affinities determined in [3H]AMPA radioligand binding experiments. (S)-4-bromohomoibotenic acid (BrHIBO) exhibited a 126-fold selectivity for GluR1o compared to GluR3o. Xenopus laevis oocytes were used to express functional homomeric and heteromeric recombinant AMPA-R and to determine BrHIBO potency (EC50) at these channels. (R,S)-BrHIBO exhibited a 37-fold selectivity range amongst the AMPA-R. It is hoped that BrHIBO can be used as a lead structure for the development of other subtype-selective compounds.",
author = "T Coquelle and Christensen, {J K} and Banke, {T G} and U Madsen and A Schousboe and Darryl Pickering",
note = "Keywords: Animals; Binding, Competitive; Cell Line; Dose-Response Relationship, Drug; Female; Ibotenic Acid; Insects; Ion Channels; Oocytes; Protein Isoforms; Receptors, AMPA; Recombinant Proteins; Xenopus laevis",
year = "2000",
language = "English",
volume = "11",
pages = "2643--8",
journal = "NeuroReport",
issn = "0959-4965",
publisher = "Lippincott Williams & Wilkins",
number = "12",
}