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  Structural and functional characterization of the gamma 1 subunit of GABAA/benzodiazepine receptors

Ymer, S., Draguhn, A., Wisden, W., Werner, P., Keinänen, K., Schofield, P. R., et al. (1990). Structural and functional characterization of the gamma 1 subunit of GABAA/benzodiazepine receptors. The EMBO Journal, 9(10), 3261-3267. doi:10.1002/j.1460-2075.1990.tb07525.x.

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Item Permalink: http://hdl.handle.net/11858/00-001M-0000-0019-AD59-2 Version Permalink: http://hdl.handle.net/21.11116/0000-0000-8381-9
Genre: Journal Article

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EMBOJ_9_1990_3261.pdf (Any fulltext), 2MB
 
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 Creators:
Ymer, Sanie, Author
Draguhn, Andreas1, Author              
Wisden, William, Author
Werner, Pia2, Author              
Keinänen, Kari, Author
Schofield, Peter R., Author
Sprengel, Rolf2, 3, 4, Author              
Pritchett, Dolan B., Author
Seeburg, Peter H.2, Author              
Affiliations:
1Department of Cell Physiology, Max Planck Institute for Medical Research, Max Planck Society, ou_1497701              
2Department of Molecular Neurobiology, Max Planck Institute for Medical Research, Max Planck Society, ou_1497704              
3Rolf Sprengel Group, Max Planck Institute for Medical Research, Max Planck Society, ou_1497741              
4Olfaction Web, Max Planck Institute for Medical Research, Max Planck Society, ou_1497733              

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Free keywords: ion channels; y subunit variants; receptor subtypes; benzodiazepine
 Abstract: The GABAA receptor gamma 1 subunit of human, rat and bovine origin was molecularly cloned and compared with the gamma 2 subunit in structure and function. Both gamma subunit variants share 74% sequence similarity and are prominently synthesized in often distinct areas of the central nervous system as documented by in situ hybridization. When co-expressed with alpha and beta subunits in Xenopus oocytes and mammalian cells, the gamma variants mediate the potentiation of GABA evoked currents by benzodiazepines and help generate high-affinity binding sites for these drugs. However, these sites show disparate pharmacological properties which, for receptors assembled from alpha 1, beta 1 and gamma 1 subunits, are characterized by the conspicuous loss in affinity for neutral antagonists (e.g. flumazenil) and negative modulators (e.g. DMCM). These findings reveal a pronounced effect of gamma subunit variants on GABAA/benzodiazepine receptor pharmacology.

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Language(s): eng - English
 Dates: 1990-05-221990-07-051990-10
 Publication Status: Published in print
 Pages: 7
 Publishing info: -
 Table of Contents: -
 Rev. Type: Peer
 Degree: -

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Title: The EMBO Journal
Source Genre: Journal
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Publ. Info: Nature Publishing Group
Pages: - Volume / Issue: 9 (10) Sequence Number: - Start / End Page: 3261 - 3267 Identifier: ISSN: 0261-4189
CoNE: https://pure.mpg.de/cone/journals/resource/954925497061_1