
You have already added 0 works in your ORCID record related to the merged Research product.
You have already added 0 works in your ORCID record related to the merged Research product.
<script type="text/javascript">
<!--
document.write('<div id="oa_widget"></div>');
document.write('<script type="text/javascript" src="https://beta.openaire.eu/index.php?option=com_openaire&view=widget&format=raw&projectId=undefined&type=result"></script>');
-->
</script>
Cerebellar GABAA receptor selective for a behavioural alcohol antagonist

doi: 10.1038/346648a0
Cerebellar GABAA receptor selective for a behavioural alcohol antagonist
Benzodiazepines are widely prescribed anxiolytics and anticonvulsants which bind with high affinity to sites on the GABAA receptor/Cl- channel complex and potentiate the effect of the neurotransmitter GABA (gamma-aminobutyric acid). The heterogeneity of benzodiazepine recognition sites in the central nervous system was revealed by studies showing different classes of GABAA receptor subunits (classes alpha, beta and gamma) and variant subunits in these classes, particularly in the alpha-class. Expression of recombinant subunits produces functional receptors; when certain alpha-variants are coexpressed with beta- and gamma-subunits the resulting receptors have pharmacological properties characteristic of GABAA-benzodiazepine type I or type II receptors. The alpha-variants are differentially expressed in the central nervous system and can be photoaffinity-labelled with benzodiazepines. Here we report a novel alpha-subunit (alpha 6) of cerebellar granule cells. We show that recombinant receptors composed of alpha 6, beta 2 and gamma 2 subunits bind with high affinity to the GABA agonist [3H]muscimol and the benzodiazepine [3H]Ro15-4513 but not the other benzodiazepines or beta-carboniles. The same distinctive pharmacology is observed with GABAA receptors from rat cerebellum immunoprecipitated by an antiserum specific for the alpha 6 subunit. We conclude that this alpha-subunit is part of a cerebellar receptor subtype, selective for Ro15-4513, an antagonist of alcohol-induced motor incoordination and ataxia.
- University of Pennsylvania United States
- Heidelberg University Germany
- Children's Hospital of Philadelphia United States
- Max Planck Institute for Medical Research Germany
- Children's Hospital of Philadelphia United States
Azides, Molecular Sequence Data, Binding, Competitive, Benzodiazepines, Cerebellum, Sequence Homology, Nucleic Acid, Animals, Amino Acid Sequence, Phosphorylation, Immunosorbent Techniques, Binding Sites, Base Sequence, Ethanol, Muscimol, Nucleic Acid Hybridization, DNA, Receptors, GABA-A, Recombinant Proteins, Rats, Cattle
Azides, Molecular Sequence Data, Binding, Competitive, Benzodiazepines, Cerebellum, Sequence Homology, Nucleic Acid, Animals, Amino Acid Sequence, Phosphorylation, Immunosorbent Techniques, Binding Sites, Base Sequence, Ethanol, Muscimol, Nucleic Acid Hybridization, DNA, Receptors, GABA-A, Recombinant Proteins, Rats, Cattle
2 Research products, page 1 of 1
- 2008IsAmongTopNSimilarDocuments
- 2011IsAmongTopNSimilarDocuments
citations This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).635 popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.Top 10% influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).Top 0.1% impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.Top 0.1%
