MolPharm xPharm- The Comprehensive Pharmacology Reference

Home Help [Feedback] [For Subscribers] [Archive] [Search] --
QUICK SEARCH:   [advanced]


     

Molecular Pharmacology Fast Forward
First published on July 18, 2005; DOI: 10.1124/mol.105.015313

This Article
Right arrow Full Text (PDF)
Right arrow All Versions of this Article:
mol.105.015313v1
68/4/942    most recent
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Buckingham, S. D
Right arrow Articles by Sattelle, D. B.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Buckingham, S. D
Right arrow Articles by Sattelle, D. B.


Received for publication June 2, 2005.
Revised July 18, 2005.
Accepted for publication July 18, 2005.

Insect GABA receptors: splicing, editing and targeting by antiparasitics and insecticides

Steven D Buckingham 1, Phil C Biggin 1, Benedict Mark Sattelle 1, Laurence Andrew Brown 1, David B. Sattelle 1*

1 University of Oxford

* Address correspondence to: E-mail: david.sattelle{at}anat.ox.ac.uk

Abstract

Ionotropic {gamma}-aminobutyric acid (GABA) receptors are abundant in both vertebrate and invertebrate nervous systems where they mediate rapid, mostly inhibitory synaptic transmission. A GABA-gated chloride channel subunit from Drosophila melanogaster (RDL - Resistant to DieLdrin) has been cloned, functionally expressed and found to exhibit many aspects of the pharmacology of native, bicuculline-insensitive, insect GABA receptors. RDL is the target of the commercially-important insecticide, fipronil. A point mutation in the channel-lining region of the RDL molecule is known to underlie most cases of resistance to insecticides acting on GABA receptors. RDL is widely distributed throughout the insect nervous system, but the subunit composition of RDL-containing in situ receptors is unknown. It is possible that in some instances RDL co-expresses with glutamate-gated chloride channel subunits. Other ionotropic receptor subunits, LCCH3 and GRD form GABA-gated cation channels when heterologously expressed. Interest in RDL as a model ligand-gated anion channel has been enhanced by the recent discovery of pre-mRNA A-to-I editing, which, together with alternative splicing, adds to the functional diversity of this GABA receptor subunit.


Key words: GABAA, GABAC, Structure-activity relationships and modeling, Func. analysis receptor/ion channel mutants, Mutagenesis/Chimeric approaches, Barbiturates, Benzodiazepines


This article has been cited by other articles:


Home page
 J. Neurosci.Home page
D. S. Hekmat-Scafe, M. Y. Lundy, R. Ranga, and M. A. Tanouye
Mutations in the K+/Cl- Cotransporter Gene kazachoc (kcc) Increase Seizure Susceptibility in Drosophila.
J. Neurosci., August 30, 2006; 26(35): 8943 - 8954.
[Abstract] [Full Text] [PDF]


Home Help [Feedback] [For Subscribers] [Archive] [Search] --
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
Molecular Interventions Drug Metabolism and Disposition

Copyright © 2005 by the American Society for Pharmacology and Experimental Therapeutics