No evidence for specific opioid effects on batrachotoxin-modified sodium channels from human brain synaptosomes
Human central nervous system (CNS) sodium channels modified by batrachotoxin and incorporated inter voltage-clamped lipid bilayers, were exposed to various concentrations of the opioid alfentanil (0.2–8.0 mM). Alfentanil caused a concentration-dependent and membrane potential independent reduction o...
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| Veröffentlicht in: | Neuroscience letters 1997-06, Vol.229 (1), p.41-44 |
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| creator | Frenkel, Christian Gerhard, Alexander Wartenberg, Hans C Benno Rehberg Urban, Bernd W |
| description | Human central nervous system (CNS) sodium channels modified by batrachotoxin and incorporated inter voltage-clamped lipid bilayers, were exposed to various concentrations of the opioid alfentanil (0.2–8.0 mM). Alfentanil caused a concentration-dependent and membrane potential independent reduction of the single channel amplitude and the fractional channel open-time. The weighted computer fit of the dose-response curve yielded a maximal conductance block of 50% with an EC
50 of 1.3 mM. These effects occurred at levels beyond clinically relevant human serum/brain levels (0.003 mM) but within the predicted concentration range using the Meyer–Overton (lipid solubility/anaesthetic potency) correlation. Thus, human CNS sodium channels are probably not a main target site for the clinical effects of alfentanil but they provide a model system to estimate the proportion of the lipophilic interactions contributing to its overall effect. |
| doi_str_mv | 10.1016/S0304-3940(97)00408-4 |
| format | Article |
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50 of 1.3 mM. These effects occurred at levels beyond clinically relevant human serum/brain levels (0.003 mM) but within the predicted concentration range using the Meyer–Overton (lipid solubility/anaesthetic potency) correlation. Thus, human CNS sodium channels are probably not a main target site for the clinical effects of alfentanil but they provide a model system to estimate the proportion of the lipophilic interactions contributing to its overall effect.</description><identifier>ISSN: 0304-3940</identifier><identifier>EISSN: 1872-7972</identifier><identifier>DOI: 10.1016/S0304-3940(97)00408-4</identifier><identifier>PMID: 9224797</identifier><identifier>CODEN: NELED5</identifier><language>eng</language><publisher>Shannon: Elsevier Ireland Ltd</publisher><subject>Alfentanil ; Alfentanil - pharmacology ; Anaesthesia ; Analgesics ; Analgesics, Opioid - pharmacology ; Batrachotoxins - pharmacology ; Biological and medical sciences ; Brain Chemistry - drug effects ; Electrophysiology ; Human brain ; Humans ; In Vitro Techniques ; Lipid bilayer ; Lipid Bilayers ; Mechanism of action ; Medical sciences ; Membrane Potentials - physiology ; Neuropharmacology ; Opioid ; Patch-Clamp Techniques ; Pharmacology. Drug treatments ; Receptors, Opioid - drug effects ; Sodium Channels - drug effects ; Sodium Channels - metabolism ; Synaptosomes - drug effects ; Synaptosomes - metabolism ; Voltage-clamp</subject><ispartof>Neuroscience letters, 1997-06, Vol.229 (1), p.41-44</ispartof><rights>1997 Elsevier Science Ireland Ltd</rights><rights>1997 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c467t-c8dcc490510634892615ffbd4a88a5130e311a341bf1bea9278004b048278baf3</citedby><cites>FETCH-LOGICAL-c467t-c8dcc490510634892615ffbd4a88a5130e311a341bf1bea9278004b048278baf3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0304-3940(97)00408-4$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2754179$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9224797$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Frenkel, Christian</creatorcontrib><creatorcontrib>Gerhard, Alexander</creatorcontrib><creatorcontrib>Wartenberg, Hans C</creatorcontrib><creatorcontrib>Benno Rehberg</creatorcontrib><creatorcontrib>Urban, Bernd W</creatorcontrib><title>No evidence for specific opioid effects on batrachotoxin-modified sodium channels from human brain synaptosomes</title><title>Neuroscience letters</title><addtitle>Neurosci Lett</addtitle><description>Human central nervous system (CNS) sodium channels modified by batrachotoxin and incorporated inter voltage-clamped lipid bilayers, were exposed to various concentrations of the opioid alfentanil (0.2–8.0 mM). Alfentanil caused a concentration-dependent and membrane potential independent reduction of the single channel amplitude and the fractional channel open-time. The weighted computer fit of the dose-response curve yielded a maximal conductance block of 50% with an EC
50 of 1.3 mM. These effects occurred at levels beyond clinically relevant human serum/brain levels (0.003 mM) but within the predicted concentration range using the Meyer–Overton (lipid solubility/anaesthetic potency) correlation. Thus, human CNS sodium channels are probably not a main target site for the clinical effects of alfentanil but they provide a model system to estimate the proportion of the lipophilic interactions contributing to its overall effect.</description><subject>Alfentanil</subject><subject>Alfentanil - pharmacology</subject><subject>Anaesthesia</subject><subject>Analgesics</subject><subject>Analgesics, Opioid - pharmacology</subject><subject>Batrachotoxins - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Brain Chemistry - drug effects</subject><subject>Electrophysiology</subject><subject>Human brain</subject><subject>Humans</subject><subject>In Vitro Techniques</subject><subject>Lipid bilayer</subject><subject>Lipid Bilayers</subject><subject>Mechanism of action</subject><subject>Medical sciences</subject><subject>Membrane Potentials - physiology</subject><subject>Neuropharmacology</subject><subject>Opioid</subject><subject>Patch-Clamp Techniques</subject><subject>Pharmacology. Drug treatments</subject><subject>Receptors, Opioid - drug effects</subject><subject>Sodium Channels - drug effects</subject><subject>Sodium Channels - metabolism</subject><subject>Synaptosomes - drug effects</subject><subject>Synaptosomes - metabolism</subject><subject>Voltage-clamp</subject><issn>0304-3940</issn><issn>1872-7972</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1997</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkcFu1DAQhi0EKtvCI1TyASE4BOzYie0TQhUUpAoOwNlynLHWKLGDJ0H07fF2V3vtySPN949H8xFyzdk7znj__gcTTDbCSPbGqLeMSaYb-YTsuFZto4xqn5LdGXlOLhF_M8Y63skLcmHaVlZmR_K3TOFvHCF5oCEXigv4GKKneYk5jhRCAL8izYkObi3O7_Oa_8XUzHmsHIwUa7HN1O9dSjAhDSXPdL_NriaKi4nifXLLmjHPgC_Is-AmhJen94r8-vzp582X5u777debj3eNl71aG69H76Wp67JeSG3annchDKN0WruOCwaCcyckHwIfwJlW6XqBgUldq8EFcUVeH-cuJf_ZAFc7R_QwTS5B3tAqw0XXavUoyHuhBO-7CnZH0JeMWCDYpcTZlXvLmT0YsQ9G7OHc1ij7YMTKmrs-fbANM4zn1ElB7b869R16N4Xiko94xlrVSa5MxT4csXriKgyKRR8P1sZYqiA75vjIIv8BWsWooQ</recordid><startdate>19970620</startdate><enddate>19970620</enddate><creator>Frenkel, Christian</creator><creator>Gerhard, Alexander</creator><creator>Wartenberg, Hans C</creator><creator>Benno Rehberg</creator><creator>Urban, Bernd W</creator><general>Elsevier Ireland Ltd</general><general>Elsevier</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>7TK</scope><scope>7X8</scope></search><sort><creationdate>19970620</creationdate><title>No evidence for specific opioid effects on batrachotoxin-modified sodium channels from human brain synaptosomes</title><author>Frenkel, Christian ; Gerhard, Alexander ; Wartenberg, Hans C ; Benno Rehberg ; Urban, Bernd W</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c467t-c8dcc490510634892615ffbd4a88a5130e311a341bf1bea9278004b048278baf3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1997</creationdate><topic>Alfentanil</topic><topic>Alfentanil - pharmacology</topic><topic>Anaesthesia</topic><topic>Analgesics</topic><topic>Analgesics, Opioid - pharmacology</topic><topic>Batrachotoxins - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Brain Chemistry - drug effects</topic><topic>Electrophysiology</topic><topic>Human brain</topic><topic>Humans</topic><topic>In Vitro Techniques</topic><topic>Lipid bilayer</topic><topic>Lipid Bilayers</topic><topic>Mechanism of action</topic><topic>Medical sciences</topic><topic>Membrane Potentials - physiology</topic><topic>Neuropharmacology</topic><topic>Opioid</topic><topic>Patch-Clamp Techniques</topic><topic>Pharmacology. Drug treatments</topic><topic>Receptors, Opioid - drug effects</topic><topic>Sodium Channels - drug effects</topic><topic>Sodium Channels - metabolism</topic><topic>Synaptosomes - drug effects</topic><topic>Synaptosomes - metabolism</topic><topic>Voltage-clamp</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Frenkel, Christian</creatorcontrib><creatorcontrib>Gerhard, Alexander</creatorcontrib><creatorcontrib>Wartenberg, Hans C</creatorcontrib><creatorcontrib>Benno Rehberg</creatorcontrib><creatorcontrib>Urban, Bernd W</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>Neurosciences Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Neuroscience letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Frenkel, Christian</au><au>Gerhard, Alexander</au><au>Wartenberg, Hans C</au><au>Benno Rehberg</au><au>Urban, Bernd W</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>No evidence for specific opioid effects on batrachotoxin-modified sodium channels from human brain synaptosomes</atitle><jtitle>Neuroscience letters</jtitle><addtitle>Neurosci Lett</addtitle><date>1997-06-20</date><risdate>1997</risdate><volume>229</volume><issue>1</issue><spage>41</spage><epage>44</epage><pages>41-44</pages><issn>0304-3940</issn><eissn>1872-7972</eissn><coden>NELED5</coden><abstract>Human central nervous system (CNS) sodium channels modified by batrachotoxin and incorporated inter voltage-clamped lipid bilayers, were exposed to various concentrations of the opioid alfentanil (0.2–8.0 mM). Alfentanil caused a concentration-dependent and membrane potential independent reduction of the single channel amplitude and the fractional channel open-time. The weighted computer fit of the dose-response curve yielded a maximal conductance block of 50% with an EC
50 of 1.3 mM. These effects occurred at levels beyond clinically relevant human serum/brain levels (0.003 mM) but within the predicted concentration range using the Meyer–Overton (lipid solubility/anaesthetic potency) correlation. Thus, human CNS sodium channels are probably not a main target site for the clinical effects of alfentanil but they provide a model system to estimate the proportion of the lipophilic interactions contributing to its overall effect.</abstract><cop>Shannon</cop><pub>Elsevier Ireland Ltd</pub><pmid>9224797</pmid><doi>10.1016/S0304-3940(97)00408-4</doi><tpages>4</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | Neuroscience letters, 1997-06, Vol.229 (1), p.41-44 |
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| subjects | Alfentanil Alfentanil - pharmacology Anaesthesia Analgesics Analgesics, Opioid - pharmacology Batrachotoxins - pharmacology Biological and medical sciences Brain Chemistry - drug effects Electrophysiology Human brain Humans In Vitro Techniques Lipid bilayer Lipid Bilayers Mechanism of action Medical sciences Membrane Potentials - physiology Neuropharmacology Opioid Patch-Clamp Techniques Pharmacology. Drug treatments Receptors, Opioid - drug effects Sodium Channels - drug effects Sodium Channels - metabolism Synaptosomes - drug effects Synaptosomes - metabolism Voltage-clamp |
| title | No evidence for specific opioid effects on batrachotoxin-modified sodium channels from human brain synaptosomes |
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