| Literature DB >> 10976936 |
T Coquelle1, J K Christensen, T G Banke, U Madsen, A Schousboe, D S Pickering.
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.Entities:
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Year: 2000 PMID： 10976936 DOI： 10.1097/00001756-200008210-00008
Source DB: PubMed Journal: Neuroreport ISSN： 0959-4965 Impact factor: 1.837