Diazepam enhancement of low affinity GABA binding to rat brain membranes
Diazepam (3 nM–3 μM) enhanced GABA binding to well-washed synaptosomal membranes in a concentration-dependent manner. Half maximal enhancement occurred at 20 nM diazepam. Kinetic analysis by non-linear Scatchard analysis revealed that the primary action of diazepam was to increase the affinity of GA...
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Veröffentlicht in: | Neuroscience letters 1982-03, Vol.29 (1), p.63-66 |
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creator | Skerritt, John H. Willow, Max Johnston, Graham A.R. |
description | Diazepam (3 nM–3 μM) enhanced GABA binding to well-washed synaptosomal membranes in a concentration-dependent manner. Half maximal enhancement occurred at 20 nM diazepam. Kinetic analysis by non-linear Scatchard analysis revealed that the primary action of diazepam was to increase the affinity of GABA binding to a low affinity site. These results support electrophysiological and other biochemical observations of benzodiazepine-GABA interactions. |
doi_str_mv | 10.1016/0304-3940(82)90365-2 |
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Half maximal enhancement occurred at 20 nM diazepam. Kinetic analysis by non-linear Scatchard analysis revealed that the primary action of diazepam was to increase the affinity of GABA binding to a low affinity site. 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Half maximal enhancement occurred at 20 nM diazepam. Kinetic analysis by non-linear Scatchard analysis revealed that the primary action of diazepam was to increase the affinity of GABA binding to a low affinity site. These results support electrophysiological and other biochemical observations of benzodiazepine-GABA interactions.</description><subject>Animals</subject><subject>Binding Sites - drug effects</subject><subject>Brain - anatomy & histology</subject><subject>Brain - metabolism</subject><subject>Cell Membrane - metabolism</subject><subject>Diazepam - pharmacology</subject><subject>gamma-Aminobutyric Acid - metabolism</subject><subject>Kinetics</subject><subject>Rats</subject><subject>Synaptosomes - metabolism</subject><subject>Synaptosomes - ultrastructure</subject><issn>0304-3940</issn><issn>1872-7972</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1982</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1PwzAMhiMEgjH4ByDlhOBQiJukbS5IY3xKk7jAOUpTB4LWdiQdCH49GZs4Ih9s2a-_HkKOgJ0Dg-KCcSYyrgQ7rfIzxXghs3yLjKAq86xUZb5NRn-SPbIf4xtjTIIUu2S3ZMlAjMj9tTffuDAtxe7VdBZb7AbaOzrvP6lxznd--KJ3k6sJrX3X-O6FDj0NZqB1ML6jLbYp6DAekB1n5hEPN35Mnm9vnqb32ezx7mE6mWWWy3LIpJNWOqiVa7BgKWVrzqFQFRhRQcErrsCoAlzprABAYIIBGGcrlRslGz4mJ-u5i9C_LzEOuvXR4nyejuiXUZeCydXbSSjWQhv6GAM6vQi-NeFLA9MrgHol0ys6usr1L0Cdp7bjzfxl3WLz17QhluqX6zqmJz88Bh2txwSu8QHtoJve_7_gB6hFfXE</recordid><startdate>19820317</startdate><enddate>19820317</enddate><creator>Skerritt, John H.</creator><creator>Willow, Max</creator><creator>Johnston, Graham A.R.</creator><general>Elsevier Ireland Ltd</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>19820317</creationdate><title>Diazepam enhancement of low affinity GABA binding to rat brain membranes</title><author>Skerritt, John H. ; Willow, Max ; Johnston, Graham A.R.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c357t-5f5c5f1b9fde60357cb3316981a481638391a961f7fc411e104011afc892a95d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1982</creationdate><topic>Animals</topic><topic>Binding Sites - drug effects</topic><topic>Brain - anatomy & histology</topic><topic>Brain - metabolism</topic><topic>Cell Membrane - metabolism</topic><topic>Diazepam - pharmacology</topic><topic>gamma-Aminobutyric Acid - metabolism</topic><topic>Kinetics</topic><topic>Rats</topic><topic>Synaptosomes - metabolism</topic><topic>Synaptosomes - ultrastructure</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Skerritt, John H.</creatorcontrib><creatorcontrib>Willow, Max</creatorcontrib><creatorcontrib>Johnston, Graham A.R.</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>Neuroscience letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Skerritt, John H.</au><au>Willow, Max</au><au>Johnston, Graham A.R.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Diazepam enhancement of low affinity GABA binding to rat brain membranes</atitle><jtitle>Neuroscience letters</jtitle><addtitle>Neurosci Lett</addtitle><date>1982-03-17</date><risdate>1982</risdate><volume>29</volume><issue>1</issue><spage>63</spage><epage>66</epage><pages>63-66</pages><issn>0304-3940</issn><eissn>1872-7972</eissn><abstract>Diazepam (3 nM–3 μM) enhanced GABA binding to well-washed synaptosomal membranes in a concentration-dependent manner. Half maximal enhancement occurred at 20 nM diazepam. Kinetic analysis by non-linear Scatchard analysis revealed that the primary action of diazepam was to increase the affinity of GABA binding to a low affinity site. These results support electrophysiological and other biochemical observations of benzodiazepine-GABA interactions.</abstract><cop>Ireland</cop><pub>Elsevier Ireland Ltd</pub><pmid>7070714</pmid><doi>10.1016/0304-3940(82)90365-2</doi><tpages>4</tpages></addata></record> |
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language | eng |
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source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
subjects | Animals Binding Sites - drug effects Brain - anatomy & histology Brain - metabolism Cell Membrane - metabolism Diazepam - pharmacology gamma-Aminobutyric Acid - metabolism Kinetics Rats Synaptosomes - metabolism Synaptosomes - ultrastructure |
title | Diazepam enhancement of low affinity GABA binding to rat brain membranes |
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