Benzodiazepine receptors in rat brain
HIGH affinity binding of tritium labelled morphine and morphine-like drugs to membranes in brain homogenates 1–3 was a decisive advance in the characterisation of opiate receptors and the discovery of enkephalines and endorphines. We report here experiments which suggest that another important group...
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Veröffentlicht in: | Nature (London) 1977-04, Vol.266 (5604), p.732-734 |
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description | HIGH affinity binding of tritium labelled morphine and morphine-like drugs to membranes in brain homogenates
1–3
was a decisive advance in the characterisation of opiate receptors and the discovery of enkephalines and endorphines. We report here experiments which suggest that another important group of psychoactive drugs, the benzodiazepines, bind to specific receptors on the membranes of rat brain cells. This suggests that there may be an unknown endogenous neurotransmitter which is the natural ligand for the benzodiazepine receptor. The binding sites are distributed unevenly through the brain, and displacement potencies of benzodiazepines correlate with pharmacological effects predictive of anxiolytic activity. |
doi_str_mv | 10.1038/266732a0 |
format | Article |
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1–3
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1–3
was a decisive advance in the characterisation of opiate receptors and the discovery of enkephalines and endorphines. We report here experiments which suggest that another important group of psychoactive drugs, the benzodiazepines, bind to specific receptors on the membranes of rat brain cells. This suggests that there may be an unknown endogenous neurotransmitter which is the natural ligand for the benzodiazepine receptor. The binding sites are distributed unevenly through the brain, and displacement potencies of benzodiazepines correlate with pharmacological effects predictive of anxiolytic activity.</description><subject>Animals</subject><subject>Benzodiazepines - metabolism</subject><subject>Binding, Competitive</subject><subject>Brain - metabolism</subject><subject>Cerebral Cortex - metabolism</subject><subject>Diazepam - metabolism</subject><subject>Hippocampus - metabolism</subject><subject>Humanities and Social Sciences</subject><subject>letter</subject><subject>Membranes - metabolism</subject><subject>multidisciplinary</subject><subject>Rats</subject><subject>Receptors, Drug - metabolism</subject><subject>Science</subject><subject>Science (multidisciplinary)</subject><subject>Synaptosomes - metabolism</subject><issn>0028-0836</issn><issn>1476-4687</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1977</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNplkDtPwzAURi3EqxQkfgBDFhAMATt-ZoSKl1SJBWbLj2uUqnWCnQz01xMUYGG6wzk60v0QOiX4mmCqbiohJK0M3kEzwqQomVByF80wrlSJFRWH6CjnFcaYE8kO0L6SgnI2Q-d3ELetb8wWuiZCkcBB17cpF00skukLm0wTj9FeMOsMJz93jt4e7l8XT-Xy5fF5cbssHSWkL2VljbIEaitwUIyDERJCMKyiDuqKYB9YoBTz2lEO3gbDnbHcecm8D76mc3QxdbvUfgyQe71psoP12kRoh6wVrZWSEo_i5SS61OacIOguNRuTPjXB-nsQ_TvIqJ79NAe7Af8nTguM-GrCeQTxHZJetUOK45f_U1_kjWe6</recordid><startdate>19770421</startdate><enddate>19770421</enddate><creator>SQUIRES, RICHARD F.</creator><creator>BRAESTRUP, CLAUS</creator><general>Nature Publishing Group UK</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>19770421</creationdate><title>Benzodiazepine receptors in rat brain</title><author>SQUIRES, RICHARD F. ; BRAESTRUP, CLAUS</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c311t-72ba8b1e9b60f845ea67effa423ce9210df4f33059c35edbfa5cab5cd74ddfd93</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1977</creationdate><topic>Animals</topic><topic>Benzodiazepines - metabolism</topic><topic>Binding, Competitive</topic><topic>Brain - metabolism</topic><topic>Cerebral Cortex - metabolism</topic><topic>Diazepam - metabolism</topic><topic>Hippocampus - metabolism</topic><topic>Humanities and Social Sciences</topic><topic>letter</topic><topic>Membranes - metabolism</topic><topic>multidisciplinary</topic><topic>Rats</topic><topic>Receptors, Drug - metabolism</topic><topic>Science</topic><topic>Science (multidisciplinary)</topic><topic>Synaptosomes - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>SQUIRES, RICHARD F.</creatorcontrib><creatorcontrib>BRAESTRUP, CLAUS</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>Nature (London)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>SQUIRES, RICHARD F.</au><au>BRAESTRUP, CLAUS</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Benzodiazepine receptors in rat brain</atitle><jtitle>Nature (London)</jtitle><stitle>Nature</stitle><addtitle>Nature</addtitle><date>1977-04-21</date><risdate>1977</risdate><volume>266</volume><issue>5604</issue><spage>732</spage><epage>734</epage><pages>732-734</pages><issn>0028-0836</issn><eissn>1476-4687</eissn><abstract>HIGH affinity binding of tritium labelled morphine and morphine-like drugs to membranes in brain homogenates
1–3
was a decisive advance in the characterisation of opiate receptors and the discovery of enkephalines and endorphines. We report here experiments which suggest that another important group of psychoactive drugs, the benzodiazepines, bind to specific receptors on the membranes of rat brain cells. This suggests that there may be an unknown endogenous neurotransmitter which is the natural ligand for the benzodiazepine receptor. The binding sites are distributed unevenly through the brain, and displacement potencies of benzodiazepines correlate with pharmacological effects predictive of anxiolytic activity.</abstract><cop>London</cop><pub>Nature Publishing Group UK</pub><pmid>876354</pmid><doi>10.1038/266732a0</doi><tpages>3</tpages></addata></record> |
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subjects | Animals Benzodiazepines - metabolism Binding, Competitive Brain - metabolism Cerebral Cortex - metabolism Diazepam - metabolism Hippocampus - metabolism Humanities and Social Sciences letter Membranes - metabolism multidisciplinary Rats Receptors, Drug - metabolism Science Science (multidisciplinary) Synaptosomes - metabolism |
title | Benzodiazepine receptors in rat brain |
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