Peripheral benzodiazepine binding sites: Effect of PK 11195, 1-(2-chlorophenyl)-n-methyl-n-(1-methylpropyl)-3-isoquinolinecarboxamide: I. In vitro studies
[ 3H] R05-4864 binding sites have been characterized in kidney, heart, brain, adrenals and platelets in the rat. In all these organs the following order of potency in the R05-4864 displacement was found : R05-4864 > diazepam > clonazepam indicating that they correspond to the “peripheral type”...
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| Veröffentlicht in: | Life sciences (1973) 1983-04, Vol.32 (16), p.1839-1847 |
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| container_issue | 16 |
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| container_title | Life sciences (1973) |
| container_volume | 32 |
| creator | Le Fur, G. Perrier, M.L. Vaucher, N. Imbault, F. Flamier, A. Benavides, J. Uzan, A. Renault, C. Dubroeucq, M.C. Guérémy, C. |
| description | [
3H] R05-4864 binding sites have been characterized in kidney, heart, brain, adrenals and platelets in the rat. In all these organs the following order of potency in the R05-4864 displacement was found : R05-4864 > diazepam > clonazepam indicating that they correspond to the “peripheral type” of benzodiazepine binding sites. PK 11195, an isoquinoline carboxamide derivative, displaces [
3H] R05-4864 from its binding sites in all the organs. PK 11195 was as potent as R05-4864 in the platelets, heart, adrenals, kidney and several brain regions (midbrain, hypothalamus, medulla + pons and hippocampus. However it was 5 to 10 times more effective in cortex and striatum. In conclusion PK 11195 might represent a new tool to elucidate the physiological relevance of “peripheral type” benzodiazepine binding sites and might help to discriminate the hypothetical subclasses of these binding sites. |
| doi_str_mv | 10.1016/0024-3205(83)90062-0 |
| format | Article |
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3H] R05-4864 binding sites have been characterized in kidney, heart, brain, adrenals and platelets in the rat. In all these organs the following order of potency in the R05-4864 displacement was found : R05-4864 > diazepam > clonazepam indicating that they correspond to the “peripheral type” of benzodiazepine binding sites. PK 11195, an isoquinoline carboxamide derivative, displaces [
3H] R05-4864 from its binding sites in all the organs. PK 11195 was as potent as R05-4864 in the platelets, heart, adrenals, kidney and several brain regions (midbrain, hypothalamus, medulla + pons and hippocampus. However it was 5 to 10 times more effective in cortex and striatum. In conclusion PK 11195 might represent a new tool to elucidate the physiological relevance of “peripheral type” benzodiazepine binding sites and might help to discriminate the hypothetical subclasses of these binding sites.</description><identifier>ISSN: 0024-3205</identifier><identifier>EISSN: 1879-0631</identifier><identifier>DOI: 10.1016/0024-3205(83)90062-0</identifier><identifier>PMID: 6300588</identifier><language>eng</language><publisher>Netherlands: Elsevier Inc</publisher><subject>Adrenal Glands - metabolism ; Animals ; Benzodiazepinones - metabolism ; Blood Platelets - metabolism ; Brain - metabolism ; Clonazepam - metabolism ; Diazepam - metabolism ; In Vitro Techniques ; Isoquinolines - metabolism ; Kidney - metabolism ; Male ; Myocardium - metabolism ; Rats ; Rats, Inbred Strains ; Receptors, Cell Surface - metabolism ; Receptors, GABA-A ; Tissue Distribution</subject><ispartof>Life sciences (1973), 1983-04, Vol.32 (16), p.1839-1847</ispartof><rights>1983</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0024-3205(83)90062-0$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3548,27922,27923,45993</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/6300588$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Le Fur, G.</creatorcontrib><creatorcontrib>Perrier, M.L.</creatorcontrib><creatorcontrib>Vaucher, N.</creatorcontrib><creatorcontrib>Imbault, F.</creatorcontrib><creatorcontrib>Flamier, A.</creatorcontrib><creatorcontrib>Benavides, J.</creatorcontrib><creatorcontrib>Uzan, A.</creatorcontrib><creatorcontrib>Renault, C.</creatorcontrib><creatorcontrib>Dubroeucq, M.C.</creatorcontrib><creatorcontrib>Guérémy, C.</creatorcontrib><title>Peripheral benzodiazepine binding sites: Effect of PK 11195, 1-(2-chlorophenyl)-n-methyl-n-(1-methylpropyl)-3-isoquinolinecarboxamide: I. In vitro studies</title><title>Life sciences (1973)</title><addtitle>Life Sci</addtitle><description>[
3H] R05-4864 binding sites have been characterized in kidney, heart, brain, adrenals and platelets in the rat. In all these organs the following order of potency in the R05-4864 displacement was found : R05-4864 > diazepam > clonazepam indicating that they correspond to the “peripheral type” of benzodiazepine binding sites. PK 11195, an isoquinoline carboxamide derivative, displaces [
3H] R05-4864 from its binding sites in all the organs. PK 11195 was as potent as R05-4864 in the platelets, heart, adrenals, kidney and several brain regions (midbrain, hypothalamus, medulla + pons and hippocampus. However it was 5 to 10 times more effective in cortex and striatum. In conclusion PK 11195 might represent a new tool to elucidate the physiological relevance of “peripheral type” benzodiazepine binding sites and might help to discriminate the hypothetical subclasses of these binding sites.</description><subject>Adrenal Glands - metabolism</subject><subject>Animals</subject><subject>Benzodiazepinones - metabolism</subject><subject>Blood Platelets - metabolism</subject><subject>Brain - metabolism</subject><subject>Clonazepam - metabolism</subject><subject>Diazepam - metabolism</subject><subject>In Vitro Techniques</subject><subject>Isoquinolines - metabolism</subject><subject>Kidney - metabolism</subject><subject>Male</subject><subject>Myocardium - metabolism</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Receptors, Cell Surface - metabolism</subject><subject>Receptors, GABA-A</subject><subject>Tissue Distribution</subject><issn>0024-3205</issn><issn>1879-0631</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1983</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9UdFu1DAQtBCoHIU_AMlP6Crhso6T2OkDEqpaOFGJPsCz5dgbziixr3ZScf0UvrY-emJfdqQZ7Y5mCHnL4ZwDbz8CVDUTFTRrJc46gLZi8IysuJIdg1bw52T1X_KSvMr5NwA0jRQn5KQVBSq1In9vMfndFpMZaY_hITpvHnDnA9LeB-fDL5r9jPmCXg0D2pnGgd5-o5zzrvlAOVtXzG7HmGK5EfbjGQtswnm7HwtY8yPeFfrACeZzvFt8iGN5YE3q4x8zeYcXdHNON4He-zlFmufFecyvyYvBjBnfHPcp-Xl99ePyK7v5_mVz-fmGIZftzJTkINFJsLJ3RkjhGmwHp0og2JmubSyWEVC52ra8Mwp64wwaJ0xdiUGIU_L-6W6xebdgnvXks8VxNAHjkrWCuqq5hCJ8dxQu_YRO75KfTNrrY5iF__TEY3F77zHpbD0Gi86nEp120WsO-lCePjSjD81oJfS_8jSIR8kNi7k</recordid><startdate>19830418</startdate><enddate>19830418</enddate><creator>Le Fur, G.</creator><creator>Perrier, M.L.</creator><creator>Vaucher, N.</creator><creator>Imbault, F.</creator><creator>Flamier, A.</creator><creator>Benavides, J.</creator><creator>Uzan, A.</creator><creator>Renault, C.</creator><creator>Dubroeucq, M.C.</creator><creator>Guérémy, C.</creator><general>Elsevier Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>19830418</creationdate><title>Peripheral benzodiazepine binding sites: Effect of PK 11195, 1-(2-chlorophenyl)-n-methyl-n-(1-methylpropyl)-3-isoquinolinecarboxamide: I. In vitro studies</title><author>Le Fur, G. ; Perrier, M.L. ; Vaucher, N. ; Imbault, F. ; Flamier, A. ; Benavides, J. ; Uzan, A. ; Renault, C. ; Dubroeucq, M.C. ; Guérémy, C.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-e176t-87107ed70c7bda373d5e6fd8006e9a965ceeee302d4c619a80badaead3a423f33</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1983</creationdate><topic>Adrenal Glands - metabolism</topic><topic>Animals</topic><topic>Benzodiazepinones - metabolism</topic><topic>Blood Platelets - metabolism</topic><topic>Brain - metabolism</topic><topic>Clonazepam - metabolism</topic><topic>Diazepam - metabolism</topic><topic>In Vitro Techniques</topic><topic>Isoquinolines - metabolism</topic><topic>Kidney - metabolism</topic><topic>Male</topic><topic>Myocardium - metabolism</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Receptors, Cell Surface - metabolism</topic><topic>Receptors, GABA-A</topic><topic>Tissue Distribution</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Le Fur, G.</creatorcontrib><creatorcontrib>Perrier, M.L.</creatorcontrib><creatorcontrib>Vaucher, N.</creatorcontrib><creatorcontrib>Imbault, F.</creatorcontrib><creatorcontrib>Flamier, A.</creatorcontrib><creatorcontrib>Benavides, J.</creatorcontrib><creatorcontrib>Uzan, A.</creatorcontrib><creatorcontrib>Renault, C.</creatorcontrib><creatorcontrib>Dubroeucq, M.C.</creatorcontrib><creatorcontrib>Guérémy, C.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><jtitle>Life sciences (1973)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Le Fur, G.</au><au>Perrier, M.L.</au><au>Vaucher, N.</au><au>Imbault, F.</au><au>Flamier, A.</au><au>Benavides, J.</au><au>Uzan, A.</au><au>Renault, C.</au><au>Dubroeucq, M.C.</au><au>Guérémy, C.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Peripheral benzodiazepine binding sites: Effect of PK 11195, 1-(2-chlorophenyl)-n-methyl-n-(1-methylpropyl)-3-isoquinolinecarboxamide: I. In vitro studies</atitle><jtitle>Life sciences (1973)</jtitle><addtitle>Life Sci</addtitle><date>1983-04-18</date><risdate>1983</risdate><volume>32</volume><issue>16</issue><spage>1839</spage><epage>1847</epage><pages>1839-1847</pages><issn>0024-3205</issn><eissn>1879-0631</eissn><abstract>[
3H] R05-4864 binding sites have been characterized in kidney, heart, brain, adrenals and platelets in the rat. In all these organs the following order of potency in the R05-4864 displacement was found : R05-4864 > diazepam > clonazepam indicating that they correspond to the “peripheral type” of benzodiazepine binding sites. PK 11195, an isoquinoline carboxamide derivative, displaces [
3H] R05-4864 from its binding sites in all the organs. PK 11195 was as potent as R05-4864 in the platelets, heart, adrenals, kidney and several brain regions (midbrain, hypothalamus, medulla + pons and hippocampus. However it was 5 to 10 times more effective in cortex and striatum. In conclusion PK 11195 might represent a new tool to elucidate the physiological relevance of “peripheral type” benzodiazepine binding sites and might help to discriminate the hypothetical subclasses of these binding sites.</abstract><cop>Netherlands</cop><pub>Elsevier Inc</pub><pmid>6300588</pmid><doi>10.1016/0024-3205(83)90062-0</doi><tpages>9</tpages></addata></record> |
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| subjects | Adrenal Glands - metabolism Animals Benzodiazepinones - metabolism Blood Platelets - metabolism Brain - metabolism Clonazepam - metabolism Diazepam - metabolism In Vitro Techniques Isoquinolines - metabolism Kidney - metabolism Male Myocardium - metabolism Rats Rats, Inbred Strains Receptors, Cell Surface - metabolism Receptors, GABA-A Tissue Distribution |
| title | Peripheral benzodiazepine binding sites: Effect of PK 11195, 1-(2-chlorophenyl)-n-methyl-n-(1-methylpropyl)-3-isoquinolinecarboxamide: I. In vitro studies |
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