Cross-resistance with dieldrin of a novel tricyclic dinitrile GABA receptor antagonist

Authors
Matsuda, K Hosie, AM Holyoke, CW Rauh, JJ Sattelle, DB
Citation
K. Matsuda et al., Cross-resistance with dieldrin of a novel tricyclic dinitrile GABA receptor antagonist, BR J PHARM, 127(6), 1999, pp. 1305-1307
Citations number
11
Categorie Soggetti
Pharmacology & Toxicology
Journal title
BRITISH JOURNAL OF PHARMACOLOGY
ISSN journal
00071188 → ACNP
Volume
127
Issue
6
Year of publication
1999
Pages
1305 - 1307
Database
ISI
SICI code
0007-1188(199907)127:6<1305:CWDOAN>2.0.ZU;2-#
Abstract
A novel tricyclic dinitrile, KN244, blocked the wild-type (dieldrin-sensiti ve) homo-oligomeric gamma-aminobutyric acid (GABA)-gated chloride channel o f Drosophila melanogaster expressed in Xenopus oocytes. Sensitivity to the block by KN244 of the response to 30 mu M GABA (IC50 = 41.6 nM, wildtype RD Lac) was reduced abut 100 fold (IC50=4.5 mu M) in the dieldrin-resistant (R DLacA302S) form of RDL.