Labelling of peripheral-type benzodiazepine binding sites in human brain with [ 3H]PK 11195: Anatomical and subcellular distribution
The peripheral-type benzodiazepine binding site, erstwhile characterized in the rodent and feline brain, has now been characterized in post-mortem human brain using[ 3H]PK 11195. The kinetics and pharmacological properties of the binding of this ligand are similar to peripheral-type benzodiazepine b...
Gespeichert in:
| Veröffentlicht in: | Brain research bulletin 1987, Vol.18 (1), p.49-61 |
|---|---|
| Hauptverfasser: | , , , , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 61 |
|---|---|
| container_issue | 1 |
| container_start_page | 49 |
| container_title | Brain research bulletin |
| container_volume | 18 |
| creator | Doble, A. Malgouris, C. Daniel, M. Daniel, N. Imbault, F. Basbaum, A. Uzan, A. Guérémy, C. Le Fur, G. |
| description | The peripheral-type benzodiazepine binding site, erstwhile characterized in the rodent and feline brain, has now been characterized in post-mortem human brain using[
3H]PK 11195. The kinetics and pharmacological properties of the binding of this ligand are similar to peripheral-type benzodiazepine binding sites elsewhere. The potency of RO5-4864 for this site in human brain is close to that seen in ruminate and carnivore tissues but considerably lower than in rodent tissues. The regional distribution of these binding sites would suggest a neuronal rather than a glial localization. [
3H]PK 11195 bound in a similar fashion to slide-mounted sections of human brain, thus allowing quantitative studies of the regional distribution of peripheral-type benzodiazepine binding sites to be made. The binding sites were distributed heterogeneously, but were restricted to the grey matter. Highest densities of binding sites were found in forebrain structures. The localization was not limited to any functional system, nor did it resemble any previously described transmitter system. The similarities between peripheral-type benzodiazepine binding sites in human and in feline brain in terms of their pharmacological characteristics and their regional and subcellular distribution suggest that the cat, rather than the rat, may be the better model for studying a possible role for this site in human cerebral function. |
| doi_str_mv | 10.1016/0361-9230(87)90033-5 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_77431201</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>0361923087900335</els_id><sourcerecordid>77431201</sourcerecordid><originalsourceid>FETCH-LOGICAL-c386t-e0027f1b63ff23e9a5925cba485f780212f252f9e320479dbc28f9b09dc181e73</originalsourceid><addsrcrecordid>eNp9kE2LFDEQhoMo67j6DxRyENFDaz46nbQHYVnUFQf0oCeRkKQrTklPujfpVnbP_nC7nWGOnipFPVV5eQh5zNlLznjzismGV62Q7LnRL1rGpKzUHbLhRstK6FrfJZsTcp88KOUnY6wxqjkjZ5JJprjYkD9b56HvMf2gQ6QjZBx3kF1fTTcjUA_pdujQ3cKIaWkxdStZcIJCMdHdvHeJ-uyW92-cdvQblVffP3-knPNWvaYXyU3DHoPrqUsdLbMPy2dz7zLtsEwZ_TzhkB6Se9H1BR4d6zn5-u7tl8uravvp_YfLi20VpGmmChgTOnLfyBiFhNapVqjgXW1U1IYJLqJQIrYgBat12_kgTGw9a7vADQctz8mzw90xD9czlMnusayJXIJhLlbrWnLB-ALWBzDkoZQM0Y4Z9y7fWM7sKt-uZu1q1hpt_8m3all7crw_-z10p6Wj7WX-9Dh3ZXESs0sBywnTtVKmXmO-OWCwuPiFkG0JCClAhxnCZLsB_5_jLzpMoEw</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>77431201</pqid></control><display><type>article</type><title>Labelling of peripheral-type benzodiazepine binding sites in human brain with [ 3H]PK 11195: Anatomical and subcellular distribution</title><source>MEDLINE</source><source>Elsevier ScienceDirect Journals</source><creator>Doble, A. ; Malgouris, C. ; Daniel, M. ; Daniel, N. ; Imbault, F. ; Basbaum, A. ; Uzan, A. ; Guérémy, C. ; Le Fur, G.</creator><creatorcontrib>Doble, A. ; Malgouris, C. ; Daniel, M. ; Daniel, N. ; Imbault, F. ; Basbaum, A. ; Uzan, A. ; Guérémy, C. ; Le Fur, G.</creatorcontrib><description>The peripheral-type benzodiazepine binding site, erstwhile characterized in the rodent and feline brain, has now been characterized in post-mortem human brain using[
3H]PK 11195. The kinetics and pharmacological properties of the binding of this ligand are similar to peripheral-type benzodiazepine binding sites elsewhere. The potency of RO5-4864 for this site in human brain is close to that seen in ruminate and carnivore tissues but considerably lower than in rodent tissues. The regional distribution of these binding sites would suggest a neuronal rather than a glial localization. [
3H]PK 11195 bound in a similar fashion to slide-mounted sections of human brain, thus allowing quantitative studies of the regional distribution of peripheral-type benzodiazepine binding sites to be made. The binding sites were distributed heterogeneously, but were restricted to the grey matter. Highest densities of binding sites were found in forebrain structures. The localization was not limited to any functional system, nor did it resemble any previously described transmitter system. The similarities between peripheral-type benzodiazepine binding sites in human and in feline brain in terms of their pharmacological characteristics and their regional and subcellular distribution suggest that the cat, rather than the rat, may be the better model for studying a possible role for this site in human cerebral function.</description><identifier>ISSN: 0361-9230</identifier><identifier>EISSN: 1873-2747</identifier><identifier>DOI: 10.1016/0361-9230(87)90033-5</identifier><identifier>PMID: 3030512</identifier><identifier>CODEN: BRBUDU</identifier><language>eng</language><publisher>New York, NY: Elsevier Inc</publisher><subject>Animals ; Autoradiography ; Benzodiazepine ; Benzodiazepinones - metabolism ; Biological and medical sciences ; Brain - metabolism ; Cats ; Cerebral Cortex - analysis ; General aspects ; Human brain ; Humans ; Isoquinolines - metabolism ; Medical sciences ; Neuropharmacology ; Pharmacology. Drug treatments ; Radioligand Assay ; Receptors, GABA-A - metabolism ; Subcellular Fractions - analysis</subject><ispartof>Brain research bulletin, 1987, Vol.18 (1), p.49-61</ispartof><rights>1987</rights><rights>1988 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c386t-e0027f1b63ff23e9a5925cba485f780212f252f9e320479dbc28f9b09dc181e73</citedby><cites>FETCH-LOGICAL-c386t-e0027f1b63ff23e9a5925cba485f780212f252f9e320479dbc28f9b09dc181e73</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0361-9230(87)90033-5$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,777,781,3537,4010,27904,27905,27906,45976</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=7455847$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3030512$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Doble, A.</creatorcontrib><creatorcontrib>Malgouris, C.</creatorcontrib><creatorcontrib>Daniel, M.</creatorcontrib><creatorcontrib>Daniel, N.</creatorcontrib><creatorcontrib>Imbault, F.</creatorcontrib><creatorcontrib>Basbaum, A.</creatorcontrib><creatorcontrib>Uzan, A.</creatorcontrib><creatorcontrib>Guérémy, C.</creatorcontrib><creatorcontrib>Le Fur, G.</creatorcontrib><title>Labelling of peripheral-type benzodiazepine binding sites in human brain with [ 3H]PK 11195: Anatomical and subcellular distribution</title><title>Brain research bulletin</title><addtitle>Brain Res Bull</addtitle><description>The peripheral-type benzodiazepine binding site, erstwhile characterized in the rodent and feline brain, has now been characterized in post-mortem human brain using[
3H]PK 11195. The kinetics and pharmacological properties of the binding of this ligand are similar to peripheral-type benzodiazepine binding sites elsewhere. The potency of RO5-4864 for this site in human brain is close to that seen in ruminate and carnivore tissues but considerably lower than in rodent tissues. The regional distribution of these binding sites would suggest a neuronal rather than a glial localization. [
3H]PK 11195 bound in a similar fashion to slide-mounted sections of human brain, thus allowing quantitative studies of the regional distribution of peripheral-type benzodiazepine binding sites to be made. The binding sites were distributed heterogeneously, but were restricted to the grey matter. Highest densities of binding sites were found in forebrain structures. The localization was not limited to any functional system, nor did it resemble any previously described transmitter system. The similarities between peripheral-type benzodiazepine binding sites in human and in feline brain in terms of their pharmacological characteristics and their regional and subcellular distribution suggest that the cat, rather than the rat, may be the better model for studying a possible role for this site in human cerebral function.</description><subject>Animals</subject><subject>Autoradiography</subject><subject>Benzodiazepine</subject><subject>Benzodiazepinones - metabolism</subject><subject>Biological and medical sciences</subject><subject>Brain - metabolism</subject><subject>Cats</subject><subject>Cerebral Cortex - analysis</subject><subject>General aspects</subject><subject>Human brain</subject><subject>Humans</subject><subject>Isoquinolines - metabolism</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Radioligand Assay</subject><subject>Receptors, GABA-A - metabolism</subject><subject>Subcellular Fractions - analysis</subject><issn>0361-9230</issn><issn>1873-2747</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE2LFDEQhoMo67j6DxRyENFDaz46nbQHYVnUFQf0oCeRkKQrTklPujfpVnbP_nC7nWGOnipFPVV5eQh5zNlLznjzismGV62Q7LnRL1rGpKzUHbLhRstK6FrfJZsTcp88KOUnY6wxqjkjZ5JJprjYkD9b56HvMf2gQ6QjZBx3kF1fTTcjUA_pdujQ3cKIaWkxdStZcIJCMdHdvHeJ-uyW92-cdvQblVffP3-knPNWvaYXyU3DHoPrqUsdLbMPy2dz7zLtsEwZ_TzhkB6Se9H1BR4d6zn5-u7tl8uravvp_YfLi20VpGmmChgTOnLfyBiFhNapVqjgXW1U1IYJLqJQIrYgBat12_kgTGw9a7vADQctz8mzw90xD9czlMnusayJXIJhLlbrWnLB-ALWBzDkoZQM0Y4Z9y7fWM7sKt-uZu1q1hpt_8m3all7crw_-z10p6Wj7WX-9Dh3ZXESs0sBywnTtVKmXmO-OWCwuPiFkG0JCClAhxnCZLsB_5_jLzpMoEw</recordid><startdate>1987</startdate><enddate>1987</enddate><creator>Doble, A.</creator><creator>Malgouris, C.</creator><creator>Daniel, M.</creator><creator>Daniel, N.</creator><creator>Imbault, F.</creator><creator>Basbaum, A.</creator><creator>Uzan, A.</creator><creator>Guérémy, C.</creator><creator>Le Fur, G.</creator><general>Elsevier Inc</general><general>Elsevier Science</general><scope>IQODW</scope><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>1987</creationdate><title>Labelling of peripheral-type benzodiazepine binding sites in human brain with [ 3H]PK 11195: Anatomical and subcellular distribution</title><author>Doble, A. ; Malgouris, C. ; Daniel, M. ; Daniel, N. ; Imbault, F. ; Basbaum, A. ; Uzan, A. ; Guérémy, C. ; Le Fur, G.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c386t-e0027f1b63ff23e9a5925cba485f780212f252f9e320479dbc28f9b09dc181e73</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>Animals</topic><topic>Autoradiography</topic><topic>Benzodiazepine</topic><topic>Benzodiazepinones - metabolism</topic><topic>Biological and medical sciences</topic><topic>Brain - metabolism</topic><topic>Cats</topic><topic>Cerebral Cortex - analysis</topic><topic>General aspects</topic><topic>Human brain</topic><topic>Humans</topic><topic>Isoquinolines - metabolism</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Radioligand Assay</topic><topic>Receptors, GABA-A - metabolism</topic><topic>Subcellular Fractions - analysis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Doble, A.</creatorcontrib><creatorcontrib>Malgouris, C.</creatorcontrib><creatorcontrib>Daniel, M.</creatorcontrib><creatorcontrib>Daniel, N.</creatorcontrib><creatorcontrib>Imbault, F.</creatorcontrib><creatorcontrib>Basbaum, A.</creatorcontrib><creatorcontrib>Uzan, A.</creatorcontrib><creatorcontrib>Guérémy, C.</creatorcontrib><creatorcontrib>Le Fur, G.</creatorcontrib><collection>Pascal-Francis</collection><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>Brain research bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Doble, A.</au><au>Malgouris, C.</au><au>Daniel, M.</au><au>Daniel, N.</au><au>Imbault, F.</au><au>Basbaum, A.</au><au>Uzan, A.</au><au>Guérémy, C.</au><au>Le Fur, G.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Labelling of peripheral-type benzodiazepine binding sites in human brain with [ 3H]PK 11195: Anatomical and subcellular distribution</atitle><jtitle>Brain research bulletin</jtitle><addtitle>Brain Res Bull</addtitle><date>1987</date><risdate>1987</risdate><volume>18</volume><issue>1</issue><spage>49</spage><epage>61</epage><pages>49-61</pages><issn>0361-9230</issn><eissn>1873-2747</eissn><coden>BRBUDU</coden><abstract>The peripheral-type benzodiazepine binding site, erstwhile characterized in the rodent and feline brain, has now been characterized in post-mortem human brain using[
3H]PK 11195. The kinetics and pharmacological properties of the binding of this ligand are similar to peripheral-type benzodiazepine binding sites elsewhere. The potency of RO5-4864 for this site in human brain is close to that seen in ruminate and carnivore tissues but considerably lower than in rodent tissues. The regional distribution of these binding sites would suggest a neuronal rather than a glial localization. [
3H]PK 11195 bound in a similar fashion to slide-mounted sections of human brain, thus allowing quantitative studies of the regional distribution of peripheral-type benzodiazepine binding sites to be made. The binding sites were distributed heterogeneously, but were restricted to the grey matter. Highest densities of binding sites were found in forebrain structures. The localization was not limited to any functional system, nor did it resemble any previously described transmitter system. The similarities between peripheral-type benzodiazepine binding sites in human and in feline brain in terms of their pharmacological characteristics and their regional and subcellular distribution suggest that the cat, rather than the rat, may be the better model for studying a possible role for this site in human cerebral function.</abstract><cop>New York, NY</cop><pub>Elsevier Inc</pub><pmid>3030512</pmid><doi>10.1016/0361-9230(87)90033-5</doi><tpages>13</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0361-9230 |
| ispartof | Brain research bulletin, 1987, Vol.18 (1), p.49-61 |
| issn | 0361-9230 1873-2747 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_77431201 |
| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Autoradiography Benzodiazepine Benzodiazepinones - metabolism Biological and medical sciences Brain - metabolism Cats Cerebral Cortex - analysis General aspects Human brain Humans Isoquinolines - metabolism Medical sciences Neuropharmacology Pharmacology. Drug treatments Radioligand Assay Receptors, GABA-A - metabolism Subcellular Fractions - analysis |
| title | Labelling of peripheral-type benzodiazepine binding sites in human brain with [ 3H]PK 11195: Anatomical and subcellular distribution |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-19T09%3A36%3A16IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Labelling%20of%20peripheral-type%20benzodiazepine%20binding%20sites%20in%20human%20brain%20with%20%5B%203H%5DPK%2011195:%20Anatomical%20and%20subcellular%20distribution&rft.jtitle=Brain%20research%20bulletin&rft.au=Doble,%20A.&rft.date=1987&rft.volume=18&rft.issue=1&rft.spage=49&rft.epage=61&rft.pages=49-61&rft.issn=0361-9230&rft.eissn=1873-2747&rft.coden=BRBUDU&rft_id=info:doi/10.1016/0361-9230(87)90033-5&rft_dat=%3Cproquest_cross%3E77431201%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=77431201&rft_id=info:pmid/3030512&rft_els_id=0361923087900335&rfr_iscdi=true |