Differential effects of sedative and anticonvulsant barbiturates on specific [ 3H]GABA binding to membrane preparations from rat brain cortex
The sensitivity to barbiturates of [ 3H]GABA binding to synaptosomal membrane fractions from rat cortex has been examined. We show that a range of anaesthetic/sedative barbiturates enhance GABA binding in the presence of chloride or other ions that interact with the associated ionophore. Furthermore...
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| Veröffentlicht in: | Biochemical pharmacology 1982-09, Vol.31 (18), p.2891-2895 |
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| container_title | Biochemical pharmacology |
| container_volume | 31 |
| creator | Whittle, Susan R. Turner, Anthony J. |
| description | The sensitivity to barbiturates of [
3H]GABA binding to synaptosomal membrane fractions from rat cortex has been examined. We show that a range of anaesthetic/sedative barbiturates enhance GABA binding in the presence of chloride or other ions that interact with the associated ionophore. Furthermore, picrotoxinin and the anticonvulsant barbiturate phenobarbital antagonise the enhancement produced by pentobarbital. These effects are therefore comparable to those observed at benzodiazepine receptors and may be mediated through the chloride ionophore component of the receptor complex. Other classes of anticonvulsants failed to antagonise pentobarbital activation, suggesting that these interactions may occur at a specific barbiturate site in the membrane. |
| doi_str_mv | 10.1016/0006-2952(82)90260-X |
| format | Article |
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3H]GABA binding to synaptosomal membrane fractions from rat cortex has been examined. We show that a range of anaesthetic/sedative barbiturates enhance GABA binding in the presence of chloride or other ions that interact with the associated ionophore. Furthermore, picrotoxinin and the anticonvulsant barbiturate phenobarbital antagonise the enhancement produced by pentobarbital. These effects are therefore comparable to those observed at benzodiazepine receptors and may be mediated through the chloride ionophore component of the receptor complex. Other classes of anticonvulsants failed to antagonise pentobarbital activation, suggesting that these interactions may occur at a specific barbiturate site in the membrane.</description><subject>Animals</subject><subject>Anticonvulsants - pharmacology</subject><subject>Barbiturates - pharmacology</subject><subject>Brain - metabolism</subject><subject>gamma-Aminobutyric Acid - metabolism</subject><subject>Hypnotics and Sedatives - pharmacology</subject><subject>In Vitro Techniques</subject><subject>Kinetics</subject><subject>Male</subject><subject>Membranes - metabolism</subject><subject>Pentobarbital - pharmacology</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Receptors, Cell Surface - metabolism</subject><subject>Receptors, GABA-A</subject><subject>Synaptosomes - metabolism</subject><issn>0006-2952</issn><issn>1873-2968</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1982</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9UU1LHTEUDVKxT-s_UMiq6GI0yXxlNoWnbVUQumlBKBLycSMpM8k0yTzaH9H_3Ly-h8suQu7NOecmOQehM0quKKHdNSGkq9jQsgvOLgfCOlI9HaAV5X1djjv-Bq1eKW_RcUo_ti3v6BE66thA25as0J-PzlqI4LOTI4ZS65xwsDiBkdltAEtvyspOB79ZxlRKrGRULi9RZihcj9MM2lmn8Xdc3z_frW_WWDlvnH_BOeAJJhWlBzxHmGURueATtjFMuDS4YM5jHWKGX-_QoZVjgtP9foK-ff709fa-evxy93C7fqx03fa5aqwZlLSNapShihvT9pS3zBI-NEBMx3sGfcN0Pah2qC1IoxRRhFrVtCC1rE_Q-93cOYafC6QsJpc0jGN5ZliSKOKedw0rxGZH1DGkFMGKObpJxt-CErFNQWw9FVuLBWfiXwriqcjO9_MXNYF5Fe1tL_iHHQ7lkxsHUSTtwGswLpYAhAnu_xf8BfeUmiw</recordid><startdate>19820915</startdate><enddate>19820915</enddate><creator>Whittle, Susan R.</creator><creator>Turner, Anthony J.</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>19820915</creationdate><title>Differential effects of sedative and anticonvulsant barbiturates on specific [ 3H]GABA binding to membrane preparations from rat brain cortex</title><author>Whittle, Susan R. ; Turner, Anthony J.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c357t-4fd9baf4b4bd1b8dd571852f0894e0d6872e742c39b593feadbb0b01fb45eaca3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1982</creationdate><topic>Animals</topic><topic>Anticonvulsants - pharmacology</topic><topic>Barbiturates - pharmacology</topic><topic>Brain - metabolism</topic><topic>gamma-Aminobutyric Acid - metabolism</topic><topic>Hypnotics and Sedatives - pharmacology</topic><topic>In Vitro Techniques</topic><topic>Kinetics</topic><topic>Male</topic><topic>Membranes - metabolism</topic><topic>Pentobarbital - pharmacology</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Receptors, Cell Surface - metabolism</topic><topic>Receptors, GABA-A</topic><topic>Synaptosomes - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Whittle, Susan R.</creatorcontrib><creatorcontrib>Turner, Anthony J.</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 pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Whittle, Susan R.</au><au>Turner, Anthony J.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Differential effects of sedative and anticonvulsant barbiturates on specific [ 3H]GABA binding to membrane preparations from rat brain cortex</atitle><jtitle>Biochemical pharmacology</jtitle><addtitle>Biochem Pharmacol</addtitle><date>1982-09-15</date><risdate>1982</risdate><volume>31</volume><issue>18</issue><spage>2891</spage><epage>2895</epage><pages>2891-2895</pages><issn>0006-2952</issn><eissn>1873-2968</eissn><abstract>The sensitivity to barbiturates of [
3H]GABA binding to synaptosomal membrane fractions from rat cortex has been examined. We show that a range of anaesthetic/sedative barbiturates enhance GABA binding in the presence of chloride or other ions that interact with the associated ionophore. Furthermore, picrotoxinin and the anticonvulsant barbiturate phenobarbital antagonise the enhancement produced by pentobarbital. These effects are therefore comparable to those observed at benzodiazepine receptors and may be mediated through the chloride ionophore component of the receptor complex. Other classes of anticonvulsants failed to antagonise pentobarbital activation, suggesting that these interactions may occur at a specific barbiturate site in the membrane.</abstract><cop>England</cop><pub>Elsevier Inc</pub><pmid>6291550</pmid><doi>10.1016/0006-2952(82)90260-X</doi><tpages>5</tpages></addata></record> |
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| ispartof | Biochemical pharmacology, 1982-09, Vol.31 (18), p.2891-2895 |
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| language | eng |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Animals Anticonvulsants - pharmacology Barbiturates - pharmacology Brain - metabolism gamma-Aminobutyric Acid - metabolism Hypnotics and Sedatives - pharmacology In Vitro Techniques Kinetics Male Membranes - metabolism Pentobarbital - pharmacology Rats Rats, Inbred Strains Receptors, Cell Surface - metabolism Receptors, GABA-A Synaptosomes - metabolism |
| title | Differential effects of sedative and anticonvulsant barbiturates on specific [ 3H]GABA binding to membrane preparations from rat brain cortex |
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