Evaluation of the interactions of serotonergic and adrenergic drugs with μ, δ, and κ opioid binding sites
Several serotonergic and adrenergic agents were tested for an ability to interact with μ, δ, and κ opioid binding sites. Spiroxatrine interacted nearly equipotently with all three opioid subtypes, yielding K i values near 110 nM. A number of other serotonergic and adrenergic agents interacted with a...
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| Veröffentlicht in: | Neuroscience letters 1991-12, Vol.133 (2), p.229-232 |
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| container_title | Neuroscience letters |
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| creator | Monroe, Philip J. Perschke, Scott E. Crisp, Terriann Smith, David J. |
| description | Several serotonergic and adrenergic agents were tested for an ability to interact with μ, δ, and κ opioid binding sites. Spiroxatrine interacted nearly equipotently with all three opioid subtypes, yielding
K
i values near 110 nM. A number of other serotonergic and adrenergic agents interacted with affinities in the 1–50 μM range. Most of the other compounds tested in this study were found to compete for opioid binding to some degree, though not achieving a 50% inhibition of binding at concentrations up to 100 μM. If this interaction between monoaminergic agents and opioid receptors is found to have functional significance, it must be considered in the interpretation of results from studies using these agents to evaluate the contribution of monoaminergic systems to opioid-mediated events. |
| doi_str_mv | 10.1016/0304-3940(91)90576-F |
| format | Article |
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K
i values near 110 nM. A number of other serotonergic and adrenergic agents interacted with affinities in the 1–50 μM range. Most of the other compounds tested in this study were found to compete for opioid binding to some degree, though not achieving a 50% inhibition of binding at concentrations up to 100 μM. If this interaction between monoaminergic agents and opioid receptors is found to have functional significance, it must be considered in the interpretation of results from studies using these agents to evaluate the contribution of monoaminergic systems to opioid-mediated events.</description><identifier>ISSN: 0304-3940</identifier><identifier>EISSN: 1872-7972</identifier><identifier>DOI: 10.1016/0304-3940(91)90576-F</identifier><identifier>PMID: 1687758</identifier><identifier>CODEN: NELED5</identifier><language>eng</language><publisher>Shannon: Elsevier Ireland Ltd</publisher><subject>Adrenergic ; Animals ; Binding, Competitive ; Biological and medical sciences ; Cell Membrane - metabolism ; Cerebellum - metabolism ; Dopamine Agents - pharmacology ; Fundamental and applied biological sciences. Psychology ; Guinea Pigs ; Kinetics ; Male ; Phentolamine ; Prosencephalon - metabolism ; Rats ; Rats, Inbred Strains ; Receptors, Opioid - drug effects ; Receptors, Opioid - metabolism ; Receptors, Opioid, delta ; Receptors, Opioid, kappa ; Receptors, Opioid, mu ; Serotonergic ; Serotonin - physiology ; Somesthesis and somesthetic pathways (proprioception, exteroception, nociception); interoception; electrolocation. Sensory receptors ; Spiroxatrine ; Sympathomimetics - pharmacology ; Vertebrates: nervous system and sense organs ; δOpioid ; κOpioid ; μOpioid</subject><ispartof>Neuroscience letters, 1991-12, Vol.133 (2), p.229-232</ispartof><rights>1991</rights><rights>1992 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c386t-e278166efb5981c502cafd89b1f82e44acf47c16fda3bfa05e3c72375e0718013</citedby><cites>FETCH-LOGICAL-c386t-e278166efb5981c502cafd89b1f82e44acf47c16fda3bfa05e3c72375e0718013</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/030439409190576F$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,65309</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=5013125$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/1687758$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Monroe, Philip J.</creatorcontrib><creatorcontrib>Perschke, Scott E.</creatorcontrib><creatorcontrib>Crisp, Terriann</creatorcontrib><creatorcontrib>Smith, David J.</creatorcontrib><title>Evaluation of the interactions of serotonergic and adrenergic drugs with μ, δ, and κ opioid binding sites</title><title>Neuroscience letters</title><addtitle>Neurosci Lett</addtitle><description>Several serotonergic and adrenergic agents were tested for an ability to interact with μ, δ, and κ opioid binding sites. Spiroxatrine interacted nearly equipotently with all three opioid subtypes, yielding
K
i values near 110 nM. A number of other serotonergic and adrenergic agents interacted with affinities in the 1–50 μM range. Most of the other compounds tested in this study were found to compete for opioid binding to some degree, though not achieving a 50% inhibition of binding at concentrations up to 100 μM. If this interaction between monoaminergic agents and opioid receptors is found to have functional significance, it must be considered in the interpretation of results from studies using these agents to evaluate the contribution of monoaminergic systems to opioid-mediated events.</description><subject>Adrenergic</subject><subject>Animals</subject><subject>Binding, Competitive</subject><subject>Biological and medical sciences</subject><subject>Cell Membrane - metabolism</subject><subject>Cerebellum - metabolism</subject><subject>Dopamine Agents - pharmacology</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Guinea Pigs</subject><subject>Kinetics</subject><subject>Male</subject><subject>Phentolamine</subject><subject>Prosencephalon - metabolism</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Receptors, Opioid - drug effects</subject><subject>Receptors, Opioid - metabolism</subject><subject>Receptors, Opioid, delta</subject><subject>Receptors, Opioid, kappa</subject><subject>Receptors, Opioid, mu</subject><subject>Serotonergic</subject><subject>Serotonin - physiology</subject><subject>Somesthesis and somesthetic pathways (proprioception, exteroception, nociception); interoception; electrolocation. Sensory receptors</subject><subject>Spiroxatrine</subject><subject>Sympathomimetics - pharmacology</subject><subject>Vertebrates: nervous system and sense organs</subject><subject>δOpioid</subject><subject>κOpioid</subject><subject>μOpioid</subject><issn>0304-3940</issn><issn>1872-7972</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1991</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMGKFDEQhoMo6-zqGyjkIKKwrUk66aQvgiw7Kix40XNIJ5XZSE8yJuldfC9P4jPMM233zrDePBVV9VXx8yH0gpJ3lNDuPWkJb9qekzc9fdsTIbtm_QitqJKskb1kj9HqAXmKTkv5QQgRVPATdEI7JaVQKzRe3phxMjWkiJPH9RpwiBWyscuoLLMCOdUUIW-CxSY6bFyGY-vytCn4NtRrvP97jve_z--J_R-cdiEFh4cQXYgbXEKF8gw98WYs8PxYz9D39eW3i8_N1ddPXy4-XjW2VV1tgElFuw78IHpFrSDMGu9UP1CvGHBurOfS0s470w7eEAGtlayVAoikitD2DL0-_N3l9HOCUvU2FAvjaCKkqWjJJOeMLyA_gDanUjJ4vctha_IvTYleJOvFoF4M6p7qe8l6PZ-9PP6fhi24f0cHq_P-1XFvijWjzybaUB4wMUekTMzYhwMGs4ubAFkXGyBacCGDrdql8P8cdyDLmxo</recordid><startdate>19911209</startdate><enddate>19911209</enddate><creator>Monroe, Philip J.</creator><creator>Perschke, Scott E.</creator><creator>Crisp, Terriann</creator><creator>Smith, David J.</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>7X8</scope></search><sort><creationdate>19911209</creationdate><title>Evaluation of the interactions of serotonergic and adrenergic drugs with μ, δ, and κ opioid binding sites</title><author>Monroe, Philip J. ; Perschke, Scott E. ; Crisp, Terriann ; Smith, David J.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c386t-e278166efb5981c502cafd89b1f82e44acf47c16fda3bfa05e3c72375e0718013</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1991</creationdate><topic>Adrenergic</topic><topic>Animals</topic><topic>Binding, Competitive</topic><topic>Biological and medical sciences</topic><topic>Cell Membrane - metabolism</topic><topic>Cerebellum - metabolism</topic><topic>Dopamine Agents - pharmacology</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Guinea Pigs</topic><topic>Kinetics</topic><topic>Male</topic><topic>Phentolamine</topic><topic>Prosencephalon - metabolism</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Receptors, Opioid - drug effects</topic><topic>Receptors, Opioid - metabolism</topic><topic>Receptors, Opioid, delta</topic><topic>Receptors, Opioid, kappa</topic><topic>Receptors, Opioid, mu</topic><topic>Serotonergic</topic><topic>Serotonin - physiology</topic><topic>Somesthesis and somesthetic pathways (proprioception, exteroception, nociception); interoception; electrolocation. Sensory receptors</topic><topic>Spiroxatrine</topic><topic>Sympathomimetics - pharmacology</topic><topic>Vertebrates: nervous system and sense organs</topic><topic>δOpioid</topic><topic>κOpioid</topic><topic>μOpioid</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Monroe, Philip J.</creatorcontrib><creatorcontrib>Perschke, Scott E.</creatorcontrib><creatorcontrib>Crisp, Terriann</creatorcontrib><creatorcontrib>Smith, David J.</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>Neuroscience letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Monroe, Philip J.</au><au>Perschke, Scott E.</au><au>Crisp, Terriann</au><au>Smith, David J.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Evaluation of the interactions of serotonergic and adrenergic drugs with μ, δ, and κ opioid binding sites</atitle><jtitle>Neuroscience letters</jtitle><addtitle>Neurosci Lett</addtitle><date>1991-12-09</date><risdate>1991</risdate><volume>133</volume><issue>2</issue><spage>229</spage><epage>232</epage><pages>229-232</pages><issn>0304-3940</issn><eissn>1872-7972</eissn><coden>NELED5</coden><abstract>Several serotonergic and adrenergic agents were tested for an ability to interact with μ, δ, and κ opioid binding sites. Spiroxatrine interacted nearly equipotently with all three opioid subtypes, yielding
K
i values near 110 nM. A number of other serotonergic and adrenergic agents interacted with affinities in the 1–50 μM range. Most of the other compounds tested in this study were found to compete for opioid binding to some degree, though not achieving a 50% inhibition of binding at concentrations up to 100 μM. If this interaction between monoaminergic agents and opioid receptors is found to have functional significance, it must be considered in the interpretation of results from studies using these agents to evaluate the contribution of monoaminergic systems to opioid-mediated events.</abstract><cop>Shannon</cop><pub>Elsevier Ireland Ltd</pub><pmid>1687758</pmid><doi>10.1016/0304-3940(91)90576-F</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0304-3940 |
| ispartof | Neuroscience letters, 1991-12, Vol.133 (2), p.229-232 |
| issn | 0304-3940 1872-7972 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Adrenergic Animals Binding, Competitive Biological and medical sciences Cell Membrane - metabolism Cerebellum - metabolism Dopamine Agents - pharmacology Fundamental and applied biological sciences. Psychology Guinea Pigs Kinetics Male Phentolamine Prosencephalon - metabolism Rats Rats, Inbred Strains Receptors, Opioid - drug effects Receptors, Opioid - metabolism Receptors, Opioid, delta Receptors, Opioid, kappa Receptors, Opioid, mu Serotonergic Serotonin - physiology Somesthesis and somesthetic pathways (proprioception, exteroception, nociception) interoception electrolocation. Sensory receptors Spiroxatrine Sympathomimetics - pharmacology Vertebrates: nervous system and sense organs δOpioid κOpioid μOpioid |
| title | Evaluation of the interactions of serotonergic and adrenergic drugs with μ, δ, and κ opioid binding sites |
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