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  Type I and type II GABAA-benzodiazepine receptors produced in transfected cells

Pritchett, D. B., Lüddens, H., & Seeburg, P. H. (1989). Type I and type II GABAA-benzodiazepine receptors produced in transfected cells. Science, 245(4924), 1389-1392. Retrieved from http://www.jstor.org/stable/1704278.

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Item Permalink: http://hdl.handle.net/21.11116/0000-0000-8529-C Version Permalink: http://hdl.handle.net/21.11116/0000-0000-852A-B
Genre: Journal Article

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Science_245_1989_1389.pdf (Any fulltext), 787KB
 
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Pritchett, Dolan B., Author
Lüddens, Hartmut, Author
Seeburg, Peter H.1, Author              
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1External Organizations, ou_persistent22              

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 Abstract: GABAA (gamma-aminobutyric acid A)-benzodiazepine receptors expressed in mammalian cells and assembled from one of three different alpha subunit variants (alpha 1, alpha 2, or alpha 3) in combination with a beta 1 and a gamma 2 subunit display the pharmacological properties of either type I or type II receptor subtypes. These receptors contain high-affinity binding sites for benzodiazepines. However, CL 218 872, 2-oxoquazepam, and methyl beta-carboline-3-carboxylate (beta-CCM) show a temperature-modulated selectivity for alpha 1 subunit-containing receptors. There were no significant differences in the binding of clonazepam, diazepam, Ro 15-1788, or dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM) to all three recombinant receptors. Receptors containing the alpha 3 subunit show greater GABA potentiation of benzodiazepine binding than receptors containing the alpha 1 or alpha 2 subunit, indicating that there are subtypes within the type II class. Thus, diversity in benzodiazepine pharmacology is generated by heterogeneity of the alpha subunit of the GABAA receptor.

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Language(s): eng - English
 Dates: 1989-05-241989-08-111989-09-22
 Publication Status: Published in print
 Pages: 4
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 Rev. Method: Peer
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Title: Science
Source Genre: Journal
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Publ. Info: Washington, D.C. : American Association for the Advancement of Science
Pages: - Volume / Issue: 245 (4924) Sequence Number: - Start / End Page: 1389 - 1392 Identifier: ISSN: 0036-8075
CoNE: /journals/resource/991042748276600_1