Implementation of a Radioreceptor Assay for Dexmedetomidine
: We have implemented a radioreceptor assay for dexmedetomidine, a novel α2‐adrenoceptor agonist. Receptor‐bearing membranes were prepared from rat cerebral cortex and 3H‐clonidine, 4 nM, was used as the labeled ligand. Dexmedetomidine displaced 3H‐clonidine in a linear fashion over a concentration...
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| Veröffentlicht in: | Pharmacology & toxicology 1993-11, Vol.73 (5), p.254-256 |
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| creator | Salonen, Markku Maze, Mervyn |
| description | : We have implemented a radioreceptor assay for dexmedetomidine, a novel α2‐adrenoceptor agonist. Receptor‐bearing membranes were prepared from rat cerebral cortex and 3H‐clonidine, 4 nM, was used as the labeled ligand. Dexmedetomidine displaced 3H‐clonidine in a linear fashion over a concentration of 2 × 10‐10 to 2 × 10‐8 M. The detection limit of dexmedetomidine (i.e. 10% of radiolabeled ligand displaced) in this assay was 50 pg.ml‐1 which is comparable to that seen with the reference method which utilizes gas chromotography with mass spectrometer (GC/MS) in series (Vuorilehto et al. 1989). Endogenous catecholamines, which can displace the radiolabeled ligand from its binding site, could easily be eliminated with a one‐step extraction procedure. A comparison was made with the reference method (GC/MS) in 47 human plasma samples; the correlation coefficient (r2) was 0.61 (P |
| doi_str_mv | 10.1111/j.1600-0773.1993.tb00580.x |
| format | Article |
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Receptor‐bearing membranes were prepared from rat cerebral cortex and 3H‐clonidine, 4 nM, was used as the labeled ligand. Dexmedetomidine displaced 3H‐clonidine in a linear fashion over a concentration of 2 × 10‐10 to 2 × 10‐8 M. The detection limit of dexmedetomidine (i.e. 10% of radiolabeled ligand displaced) in this assay was 50 pg.ml‐1 which is comparable to that seen with the reference method which utilizes gas chromotography with mass spectrometer (GC/MS) in series (Vuorilehto et al. 1989). Endogenous catecholamines, which can displace the radiolabeled ligand from its binding site, could easily be eliminated with a one‐step extraction procedure. A comparison was made with the reference method (GC/MS) in 47 human plasma samples; the correlation coefficient (r2) was 0.61 (P<0.001). The radioreceptor assay was also successfully applied for determining dexmedetomidine concentration in rabbit samples. These data indicate that the radioreceptor assay can be utilized for characterizing the pharmacokinetics of novel α2 agonists which are now being introduced into the clinical practice of anaesthesia.</description><identifier>ISSN: 0901-9928</identifier><identifier>EISSN: 1600-0773</identifier><identifier>DOI: 10.1111/j.1600-0773.1993.tb00580.x</identifier><identifier>PMID: 7906879</identifier><identifier>CODEN: PHTOEH</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>Adrenergic alpha-Agonists - analysis ; Adrenergic alpha-Agonists - metabolism ; Analysis ; Animals ; Biological and medical sciences ; Cerebral Cortex - metabolism ; Clonidine - metabolism ; General pharmacology ; Imidazoles - analysis ; Imidazoles - metabolism ; Male ; Medetomidine ; Medical sciences ; Pharmacology. Drug treatments ; Rabbits ; Radioligand Assay - methods ; Rats ; Rats, Sprague-Dawley ; Receptors, Adrenergic, alpha - metabolism</subject><ispartof>Pharmacology & toxicology, 1993-11, Vol.73 (5), p.254-256</ispartof><rights>1993 Nordic Pharmacological Society</rights><rights>1994 INIST-CNRS</rights><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3990-b3859fb034843ad820f7bc3fc4ed8f4662bcb21bb3b8e6f3885497572810f7b53</citedby><cites>FETCH-LOGICAL-c3990-b3859fb034843ad820f7bc3fc4ed8f4662bcb21bb3b8e6f3885497572810f7b53</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1111%2Fj.1600-0773.1993.tb00580.x$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1111%2Fj.1600-0773.1993.tb00580.x$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,776,780,1411,27901,27902,45550,45551</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3876054$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/7906879$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Salonen, Markku</creatorcontrib><creatorcontrib>Maze, Mervyn</creatorcontrib><title>Implementation of a Radioreceptor Assay for Dexmedetomidine</title><title>Pharmacology & toxicology</title><addtitle>Pharmacol Toxicol</addtitle><description>: We have implemented a radioreceptor assay for dexmedetomidine, a novel α2‐adrenoceptor agonist. Receptor‐bearing membranes were prepared from rat cerebral cortex and 3H‐clonidine, 4 nM, was used as the labeled ligand. Dexmedetomidine displaced 3H‐clonidine in a linear fashion over a concentration of 2 × 10‐10 to 2 × 10‐8 M. The detection limit of dexmedetomidine (i.e. 10% of radiolabeled ligand displaced) in this assay was 50 pg.ml‐1 which is comparable to that seen with the reference method which utilizes gas chromotography with mass spectrometer (GC/MS) in series (Vuorilehto et al. 1989). Endogenous catecholamines, which can displace the radiolabeled ligand from its binding site, could easily be eliminated with a one‐step extraction procedure. A comparison was made with the reference method (GC/MS) in 47 human plasma samples; the correlation coefficient (r2) was 0.61 (P<0.001). The radioreceptor assay was also successfully applied for determining dexmedetomidine concentration in rabbit samples. These data indicate that the radioreceptor assay can be utilized for characterizing the pharmacokinetics of novel α2 agonists which are now being introduced into the clinical practice of anaesthesia.</description><subject>Adrenergic alpha-Agonists - analysis</subject><subject>Adrenergic alpha-Agonists - metabolism</subject><subject>Analysis</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cerebral Cortex - metabolism</subject><subject>Clonidine - metabolism</subject><subject>General pharmacology</subject><subject>Imidazoles - analysis</subject><subject>Imidazoles - metabolism</subject><subject>Male</subject><subject>Medetomidine</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Rabbits</subject><subject>Radioligand Assay - methods</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Receptors, Adrenergic, alpha - metabolism</subject><issn>0901-9928</issn><issn>1600-0773</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1993</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqVkF1LwzAUhoMoc8z9BKGIeNeaNE2T6IXM-TUYKDKvQ5ImEOmXTYfbvzdlZffmJgfe5-ScPABcIZigcG6_E5RDGENKcYI4x0mvICQMJrsTMD1Gp2AKOUQx5yk7B3PvnYKYUIZQlk_AhHKYM8qn4H5VtaWpTN3L3jV11NhIRp-ycE1ntGn7posW3st9ZEP1ZHaVKUzfVK5wtbkAZ1aW3szHewa-Xp43y7d4_f66Wi7Wscacw1hhRrgN4zOWYVmwFFqqNLY6MwWzWZ6nSqsUKYUVM7nFjJGMU0JThgaS4Bm4Obzbds3P1vheVM5rU5ayNs3WC5qnGSIEBfDuAOqu8b4zVrSdq2S3FwiKQZ74FoMhMRgSgzwxyhO70Hw5Ttmq8Mtj66gq5NdjLr2Wpe1krZ0_YpjRHJIsYA8H7NeVZv-PBcTj8mMTKvwHvwCLKw</recordid><startdate>199311</startdate><enddate>199311</enddate><creator>Salonen, Markku</creator><creator>Maze, Mervyn</creator><general>Blackwell Publishing Ltd</general><general>Blackwell</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>199311</creationdate><title>Implementation of a Radioreceptor Assay for Dexmedetomidine</title><author>Salonen, Markku ; Maze, Mervyn</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3990-b3859fb034843ad820f7bc3fc4ed8f4662bcb21bb3b8e6f3885497572810f7b53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1993</creationdate><topic>Adrenergic alpha-Agonists - analysis</topic><topic>Adrenergic alpha-Agonists - metabolism</topic><topic>Analysis</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cerebral Cortex - metabolism</topic><topic>Clonidine - metabolism</topic><topic>General pharmacology</topic><topic>Imidazoles - analysis</topic><topic>Imidazoles - metabolism</topic><topic>Male</topic><topic>Medetomidine</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Rabbits</topic><topic>Radioligand Assay - methods</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Receptors, Adrenergic, alpha - metabolism</topic><toplevel>online_resources</toplevel><creatorcontrib>Salonen, Markku</creatorcontrib><creatorcontrib>Maze, Mervyn</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>Pharmacology & toxicology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Salonen, Markku</au><au>Maze, Mervyn</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Implementation of a Radioreceptor Assay for Dexmedetomidine</atitle><jtitle>Pharmacology & toxicology</jtitle><addtitle>Pharmacol Toxicol</addtitle><date>1993-11</date><risdate>1993</risdate><volume>73</volume><issue>5</issue><spage>254</spage><epage>256</epage><pages>254-256</pages><issn>0901-9928</issn><eissn>1600-0773</eissn><coden>PHTOEH</coden><abstract>: We have implemented a radioreceptor assay for dexmedetomidine, a novel α2‐adrenoceptor agonist. Receptor‐bearing membranes were prepared from rat cerebral cortex and 3H‐clonidine, 4 nM, was used as the labeled ligand. Dexmedetomidine displaced 3H‐clonidine in a linear fashion over a concentration of 2 × 10‐10 to 2 × 10‐8 M. The detection limit of dexmedetomidine (i.e. 10% of radiolabeled ligand displaced) in this assay was 50 pg.ml‐1 which is comparable to that seen with the reference method which utilizes gas chromotography with mass spectrometer (GC/MS) in series (Vuorilehto et al. 1989). Endogenous catecholamines, which can displace the radiolabeled ligand from its binding site, could easily be eliminated with a one‐step extraction procedure. A comparison was made with the reference method (GC/MS) in 47 human plasma samples; the correlation coefficient (r2) was 0.61 (P<0.001). The radioreceptor assay was also successfully applied for determining dexmedetomidine concentration in rabbit samples. These data indicate that the radioreceptor assay can be utilized for characterizing the pharmacokinetics of novel α2 agonists which are now being introduced into the clinical practice of anaesthesia.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>7906879</pmid><doi>10.1111/j.1600-0773.1993.tb00580.x</doi><tpages>3</tpages></addata></record> |
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| ispartof | Pharmacology & toxicology, 1993-11, Vol.73 (5), p.254-256 |
| issn | 0901-9928 1600-0773 |
| language | eng |
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| subjects | Adrenergic alpha-Agonists - analysis Adrenergic alpha-Agonists - metabolism Analysis Animals Biological and medical sciences Cerebral Cortex - metabolism Clonidine - metabolism General pharmacology Imidazoles - analysis Imidazoles - metabolism Male Medetomidine Medical sciences Pharmacology. Drug treatments Rabbits Radioligand Assay - methods Rats Rats, Sprague-Dawley Receptors, Adrenergic, alpha - metabolism |
| title | Implementation of a Radioreceptor Assay for Dexmedetomidine |
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