NDLI: Cloning and functional expression of a Drosophila gamma-aminobutyric acid receptor.

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Cloning and functional expression of a Drosophila gamma-aminobutyric acid receptor.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Lambert, J. J. Reyes, A. Chen, R. Lan, N. C. Belelli, D. Peters, J. A.
Description	Author Affiliation: Chen R ( CoCensys, Inc., Irvine, CA 92718.);
Abstract	A cDNA encoding a functional gamma-aminobutyric (GABA)-activated Cl- channel has been isolated from an adult Drosophila head cDNA library. When expressed in Xenopus laevis oocytes, the subunit functions efficiently, presumably as a homooligomeric complex and is activated by GABA or muscimol. GABA-evoked currents are highly sensitive to antagonism by picrotoxin but are insensitive to bicuculline, RU 5135, or zinc. Pentobarbitone greatly enhances GABA-evoked currents, whereas the neurosteroid 5 alpha-pregnan-3 alpha-ol-20-one demonstrates a large reduction in both the potency and maximal effect when compared with its actions upon vertebrate GABA type A receptors. Although zinc-insensitive, the subunit is also insensitive to flunitrazepam. Hence, the GABA receptors formed by this subunit exhibit a unique pharmacology when compared with vertebrate GABA type A receptors or those composed of rho subunits. Because the receptor-channel complex functions as a homooligomer, this subunit may be of value in mutagenesis studies aiming to define drug-binding sites.
ISSN	00278424
e-ISSN	10916490
Journal	Proceedings of the National Academy of Sciences of the United States of America
Issue Number	13
Volume Number	91
Language	English
Publisher	National Academy of Sciences
Publisher Date	1994-07-01
Publisher Place	United States
Access Restriction	Open
Subject Keyword	Bicyclo Compounds, Heterocyclic Drosophila Melanogaster Metabolism Receptors, GABA-A Physiology Receptors, GABA Gamma-Aminobutyric Acid Pharmacology Amino Acid Sequence Animals Bicuculline Bicyclo Compounds Cloning, Molecular Convulsants DNA Primers DNA, Complementary Genetics Flunitrazepam Gene Expression Macromolecular Substances Molecular Sequence Data Muscimol Oocytes Drug Effects Pentobarbital Picrotoxin Polymerase Chain Reaction Biosynthesis Transcription, Genetic Xenopus Laevis Comparative Study Multidisciplinary
Content Type	Text
Resource Type	Article
Subject	Multidisciplinary

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