Solubilization of convulsant/barbiturate binding activity on the γ-aminobutyric acid/benzodiazepine receptor complex
Binding activity of the radioactive cage convulsant [ 35S] t-butyl-bicyclophosphorothionate was solubilized from rat brain membranes using the zwitterionic detergent 3-[(3-cholamidopropyl)-dimethylammonio] propanesulfonate. Binding (K D = 26 nM, Bmax = 0.4 pmol/mg protein) was inhibited by picrotoxi...
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Veröffentlicht in: | Biochemical and biophysical research communications 1984-03, Vol.119 (2), p.530-536 |
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container_title | Biochemical and biophysical research communications |
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creator | King, Ronnie G. Olsen, Richard W. |
description | Binding activity of the radioactive cage convulsant [
35S]
t-butyl-bicyclophosphorothionate was solubilized from rat brain membranes using the zwitterionic detergent 3-[(3-cholamidopropyl)-dimethylammonio] propanesulfonate. Binding (K
D = 26 nM, Bmax = 0.4 pmol/mg protein) was inhibited by picrotoxin and related convulsants and by barbiturates and related depressants that interact with γ-aminobutyric acid and benzodiazepine receptors via the picrotoxinin binding site. The convulsant/ barbiturate binding activity chromatographed on gel filtration as a single peak coinciding with the benzodiazepine/γ-aminobutyric acid receptor protein complex. |
doi_str_mv | 10.1016/S0006-291X(84)80280-6 |
format | Article |
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35S]
t-butyl-bicyclophosphorothionate was solubilized from rat brain membranes using the zwitterionic detergent 3-[(3-cholamidopropyl)-dimethylammonio] propanesulfonate. Binding (K
D = 26 nM, Bmax = 0.4 pmol/mg protein) was inhibited by picrotoxin and related convulsants and by barbiturates and related depressants that interact with γ-aminobutyric acid and benzodiazepine receptors via the picrotoxinin binding site. The convulsant/ barbiturate binding activity chromatographed on gel filtration as a single peak coinciding with the benzodiazepine/γ-aminobutyric acid receptor protein complex.</description><identifier>ISSN: 0006-291X</identifier><identifier>EISSN: 1090-2104</identifier><identifier>DOI: 10.1016/S0006-291X(84)80280-6</identifier><identifier>PMID: 6324766</identifier><language>eng</language><publisher>United States: Elsevier Inc</publisher><subject>Animals ; Barbiturates - metabolism ; Benzodiazepines - metabolism ; Binding, Competitive ; Bridged Bicyclo Compounds - metabolism ; Bridged Bicyclo Compounds, Heterocyclic ; Bridged-Ring Compounds - metabolism ; Cerebral Cortex - metabolism ; Convulsants - metabolism ; gamma-Aminobutyric Acid - metabolism ; Intracellular Membranes - metabolism ; Rats ; Rats, Inbred Strains ; Receptors, Cell Surface - isolation & purification ; Receptors, Cell Surface - metabolism ; Receptors, GABA-A ; Receptors, Neurotransmitter - isolation & purification ; Receptors, Neurotransmitter - metabolism</subject><ispartof>Biochemical and biophysical research communications, 1984-03, Vol.119 (2), p.530-536</ispartof><rights>1984 Academic Press, Inc. All rights reserved</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c360t-7ae2c5dd60aa88c90742269257fc665b676bbd0f53af8689ab7d0df66e728e5d3</citedby><cites>FETCH-LOGICAL-c360t-7ae2c5dd60aa88c90742269257fc665b676bbd0f53af8689ab7d0df66e728e5d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0006-291X(84)80280-6$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3549,27923,27924,45994</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/6324766$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>King, Ronnie G.</creatorcontrib><creatorcontrib>Olsen, Richard W.</creatorcontrib><title>Solubilization of convulsant/barbiturate binding activity on the γ-aminobutyric acid/benzodiazepine receptor complex</title><title>Biochemical and biophysical research communications</title><addtitle>Biochem Biophys Res Commun</addtitle><description>Binding activity of the radioactive cage convulsant [
35S]
t-butyl-bicyclophosphorothionate was solubilized from rat brain membranes using the zwitterionic detergent 3-[(3-cholamidopropyl)-dimethylammonio] propanesulfonate. Binding (K
D = 26 nM, Bmax = 0.4 pmol/mg protein) was inhibited by picrotoxin and related convulsants and by barbiturates and related depressants that interact with γ-aminobutyric acid and benzodiazepine receptors via the picrotoxinin binding site. The convulsant/ barbiturate binding activity chromatographed on gel filtration as a single peak coinciding with the benzodiazepine/γ-aminobutyric acid receptor protein complex.</description><subject>Animals</subject><subject>Barbiturates - metabolism</subject><subject>Benzodiazepines - metabolism</subject><subject>Binding, Competitive</subject><subject>Bridged Bicyclo Compounds - metabolism</subject><subject>Bridged Bicyclo Compounds, Heterocyclic</subject><subject>Bridged-Ring Compounds - metabolism</subject><subject>Cerebral Cortex - metabolism</subject><subject>Convulsants - metabolism</subject><subject>gamma-Aminobutyric Acid - metabolism</subject><subject>Intracellular Membranes - metabolism</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Receptors, Cell Surface - isolation & purification</subject><subject>Receptors, Cell Surface - metabolism</subject><subject>Receptors, GABA-A</subject><subject>Receptors, Neurotransmitter - isolation & purification</subject><subject>Receptors, Neurotransmitter - metabolism</subject><issn>0006-291X</issn><issn>1090-2104</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1984</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkEuO1DAQhi0EGpqBI4yUFYJF6LKTOM4KodHwkEZiMSCxs_yoQKHEDo7Tovta3IMzkZ5uzZZVLf6X6mPsisMbDlxu7wBAlqLj316p-rUCoaCUj9iGQwel4FA_ZpsHy1P2bJ5_AnBey-6CXchK1K2UG7bcxWGxNNDBZIqhiH3hYtgtw2xC3lqTLOUlmYyFpeApfC-My7SjvC9Wd_6Bxd8_pRkpRLvkfSK36uS3FsMhejIHnChgkdDhlGNau8dpwN_P2ZPeDDO-ON9L9vX9zZfrj-Xt5w-frt_dlq6SkMvWoHCN9xKMUcp10NZCyE40be-kbKxspbUe-qYyvZKqM7b14HspsRUKG19dspen3inFXwvOWY80OxwGEzAus1YcRFULuRqbk9GlOM8Jez0lGk3aaw76iFvf49ZHllrV-h63PuauzgOLHdE_pM58V_3tScf1yx1h0rMjDA49rUyy9pH-s_APYiOUAA</recordid><startdate>19840315</startdate><enddate>19840315</enddate><creator>King, Ronnie G.</creator><creator>Olsen, Richard W.</creator><general>Elsevier Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19840315</creationdate><title>Solubilization of convulsant/barbiturate binding activity on the γ-aminobutyric acid/benzodiazepine receptor complex</title><author>King, Ronnie G. ; Olsen, Richard W.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c360t-7ae2c5dd60aa88c90742269257fc665b676bbd0f53af8689ab7d0df66e728e5d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1984</creationdate><topic>Animals</topic><topic>Barbiturates - metabolism</topic><topic>Benzodiazepines - metabolism</topic><topic>Binding, Competitive</topic><topic>Bridged Bicyclo Compounds - metabolism</topic><topic>Bridged Bicyclo Compounds, Heterocyclic</topic><topic>Bridged-Ring Compounds - metabolism</topic><topic>Cerebral Cortex - metabolism</topic><topic>Convulsants - metabolism</topic><topic>gamma-Aminobutyric Acid - metabolism</topic><topic>Intracellular Membranes - metabolism</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Receptors, Cell Surface - isolation & purification</topic><topic>Receptors, Cell Surface - metabolism</topic><topic>Receptors, GABA-A</topic><topic>Receptors, Neurotransmitter - isolation & purification</topic><topic>Receptors, Neurotransmitter - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>King, Ronnie G.</creatorcontrib><creatorcontrib>Olsen, Richard W.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Biochemical and biophysical research communications</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>King, Ronnie G.</au><au>Olsen, Richard W.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Solubilization of convulsant/barbiturate binding activity on the γ-aminobutyric acid/benzodiazepine receptor complex</atitle><jtitle>Biochemical and biophysical research communications</jtitle><addtitle>Biochem Biophys Res Commun</addtitle><date>1984-03-15</date><risdate>1984</risdate><volume>119</volume><issue>2</issue><spage>530</spage><epage>536</epage><pages>530-536</pages><issn>0006-291X</issn><eissn>1090-2104</eissn><abstract>Binding activity of the radioactive cage convulsant [
35S]
t-butyl-bicyclophosphorothionate was solubilized from rat brain membranes using the zwitterionic detergent 3-[(3-cholamidopropyl)-dimethylammonio] propanesulfonate. Binding (K
D = 26 nM, Bmax = 0.4 pmol/mg protein) was inhibited by picrotoxin and related convulsants and by barbiturates and related depressants that interact with γ-aminobutyric acid and benzodiazepine receptors via the picrotoxinin binding site. The convulsant/ barbiturate binding activity chromatographed on gel filtration as a single peak coinciding with the benzodiazepine/γ-aminobutyric acid receptor protein complex.</abstract><cop>United States</cop><pub>Elsevier Inc</pub><pmid>6324766</pmid><doi>10.1016/S0006-291X(84)80280-6</doi><tpages>7</tpages></addata></record> |
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language | eng |
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source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
subjects | Animals Barbiturates - metabolism Benzodiazepines - metabolism Binding, Competitive Bridged Bicyclo Compounds - metabolism Bridged Bicyclo Compounds, Heterocyclic Bridged-Ring Compounds - metabolism Cerebral Cortex - metabolism Convulsants - metabolism gamma-Aminobutyric Acid - metabolism Intracellular Membranes - metabolism Rats Rats, Inbred Strains Receptors, Cell Surface - isolation & purification Receptors, Cell Surface - metabolism Receptors, GABA-A Receptors, Neurotransmitter - isolation & purification Receptors, Neurotransmitter - metabolism |
title | Solubilization of convulsant/barbiturate binding activity on the γ-aminobutyric acid/benzodiazepine receptor complex |
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