Cross‐resistance with dieldrin of a novel tricyclic dinitrile GABA receptor antagonist
Open Access
- 1 July 1999
- journal article
- Published by Wiley in British Journal of Pharmacology
- Vol. 127 (6) , 1305-1307
- https://doi.org/10.1038/sj.bjp.0702663
Abstract
A novel tricyclic dinitrile, KN244, blocked the wild-type (dieldrin-sensitive) homo-oligomeric gamma-aminobutyric acid (GABA)-gated chloride channel of Drosophila melanogaster expressed in Xenopus oocytes. Sensitivity to the block by KN244 of the response to 30 microM GABA (IC50=41.6 nM, wild-type RDLac) was reduced abut 100 fold (IC50=4.5 microM) in the dieldrin-resistant (RDLacA302S) form of RDL.Keywords
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