Differentiation of opiate and neuroleptic receptor binding in rat brain
For 6 large series of compounds derived from the piperidine moieties of spiperone, pimozide, haloperidol, pethidine, fentanyl and 4-methocarboxyl-fentanyl, IC 50 values were determined in the opiate and neuroleptic binding assay using [ 3H]-fentanyl and [ 3H]-haloperidol as ligands, respectively. Th...
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| Veröffentlicht in: | European journal of pharmacology 1977-06, Vol.43 (3), p.253-267 |
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| container_title | European journal of pharmacology |
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| creator | Leysen, Josee Tollenaere, Jan P. Koch, Michel H.J. Laduron, Pierre |
| description | For 6 large series of compounds derived from the piperidine moieties of spiperone, pimozide, haloperidol, pethidine, fentanyl and 4-methocarboxyl-fentanyl, IC
50 values were determined in the opiate and neuroleptic binding assay using [
3H]-fentanyl and [
3H]-haloperidol as ligands, respectively. The specificity and difference between both receptors were demonstrated on the basis of several criteria (1) the stereospecificity of the binding (2) the significant correlation between the in vitro activity of the drugs and their pharmacological potency in vivo, notwithstanding some discrepancies which are probably of pharmacokinetic and/or metabolic origin (3) the ability to discriminate between morphinomimetic and neuroleptic drugs by the differential affinity for their specific receptor (4) the structure—activity relationships derived from the in vitro data indicating that the structural requirements for high affinity binding in vitro parallel those for high in vivo potency (5) a demonstration, on the basis of physicochemical principles, of the difference in binding mechanism between morphinomimetics and neuroleptics to their respective receptor. |
| doi_str_mv | 10.1016/0014-2999(77)90025-5 |
| format | Article |
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50 values were determined in the opiate and neuroleptic binding assay using [
3H]-fentanyl and [
3H]-haloperidol as ligands, respectively. The specificity and difference between both receptors were demonstrated on the basis of several criteria (1) the stereospecificity of the binding (2) the significant correlation between the in vitro activity of the drugs and their pharmacological potency in vivo, notwithstanding some discrepancies which are probably of pharmacokinetic and/or metabolic origin (3) the ability to discriminate between morphinomimetic and neuroleptic drugs by the differential affinity for their specific receptor (4) the structure—activity relationships derived from the in vitro data indicating that the structural requirements for high affinity binding in vitro parallel those for high in vivo potency (5) a demonstration, on the basis of physicochemical principles, of the difference in binding mechanism between morphinomimetics and neuroleptics to their respective receptor.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(77)90025-5</identifier><identifier>PMID: 194781</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Animals ; Benzimidazoles - metabolism ; Benzimidazoles - pharmacology ; Brain - metabolism ; Female ; Fentanyl - analogs & derivatives ; Fentanyl - metabolism ; Fentanyl - pharmacology ; Haloperidol - metabolism ; Haloperidol - pharmacology ; Meperidine - metabolism ; Meperidine - pharmacology ; Neuroleptic receptor ; Opiate receptor ; Piperidines - metabolism ; Piperidines - pharmacology ; Rats ; Receptors, Drug ; Receptors, Opioid ; Spiro Compounds - metabolism ; Spiro Compounds - pharmacology ; Structure-Activity Relationship</subject><ispartof>European journal of pharmacology, 1977-06, Vol.43 (3), p.253-267</ispartof><rights>1977</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c356t-ec20eee824ed87b280545cfa98446242f1f9200912eb41a3046f5036df50e62e3</citedby><cites>FETCH-LOGICAL-c356t-ec20eee824ed87b280545cfa98446242f1f9200912eb41a3046f5036df50e62e3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/0014299977900255$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/194781$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Leysen, Josee</creatorcontrib><creatorcontrib>Tollenaere, Jan P.</creatorcontrib><creatorcontrib>Koch, Michel H.J.</creatorcontrib><creatorcontrib>Laduron, Pierre</creatorcontrib><title>Differentiation of opiate and neuroleptic receptor binding in rat brain</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>For 6 large series of compounds derived from the piperidine moieties of spiperone, pimozide, haloperidol, pethidine, fentanyl and 4-methocarboxyl-fentanyl, IC
50 values were determined in the opiate and neuroleptic binding assay using [
3H]-fentanyl and [
3H]-haloperidol as ligands, respectively. The specificity and difference between both receptors were demonstrated on the basis of several criteria (1) the stereospecificity of the binding (2) the significant correlation between the in vitro activity of the drugs and their pharmacological potency in vivo, notwithstanding some discrepancies which are probably of pharmacokinetic and/or metabolic origin (3) the ability to discriminate between morphinomimetic and neuroleptic drugs by the differential affinity for their specific receptor (4) the structure—activity relationships derived from the in vitro data indicating that the structural requirements for high affinity binding in vitro parallel those for high in vivo potency (5) a demonstration, on the basis of physicochemical principles, of the difference in binding mechanism between morphinomimetics and neuroleptics to their respective receptor.</description><subject>Animals</subject><subject>Benzimidazoles - metabolism</subject><subject>Benzimidazoles - pharmacology</subject><subject>Brain - metabolism</subject><subject>Female</subject><subject>Fentanyl - analogs & derivatives</subject><subject>Fentanyl - metabolism</subject><subject>Fentanyl - pharmacology</subject><subject>Haloperidol - metabolism</subject><subject>Haloperidol - pharmacology</subject><subject>Meperidine - metabolism</subject><subject>Meperidine - pharmacology</subject><subject>Neuroleptic receptor</subject><subject>Opiate receptor</subject><subject>Piperidines - metabolism</subject><subject>Piperidines - pharmacology</subject><subject>Rats</subject><subject>Receptors, Drug</subject><subject>Receptors, Opioid</subject><subject>Spiro Compounds - metabolism</subject><subject>Spiro Compounds - pharmacology</subject><subject>Structure-Activity Relationship</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1977</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kEtLAzEQx4P4qtVv4CEn0cPqJJvsbi6CVK1CwYueQzY7kUib1GQr-O3dPtCbl5mB_wPmR8g5g2sGrLoBYKLgSqnLur5SAFwWco-MWFOrAmrG98no13JMTnL-AACpuDwih0yJumEjMr33zmHC0HvT-xhodDQuhxupCR0NuEpxjsveW5rQDkdMtPWh8-Gd-kCT6WmbjA-n5MCZecaz3R6Tt8eH18lTMXuZPk_uZoUtZdUXaDkgYsMFdk3d8gakkNYZ1QhRccEdc4oDKMaxFcyUIConoay6YWLFsRyTi23vMsXPFeZeL3y2OJ-bgHGVdVMqUUloBqPYGm2KOSd0epn8wqRvzUCv8ek1G71mo-tab_BpOcTOd_2rdoHdX2jDa5BvtzIOP355TDpbj8Fi5wc8ve6i_7__B-JPfgk</recordid><startdate>19770601</startdate><enddate>19770601</enddate><creator>Leysen, Josee</creator><creator>Tollenaere, Jan P.</creator><creator>Koch, Michel H.J.</creator><creator>Laduron, Pierre</creator><general>Elsevier B.V</general><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>19770601</creationdate><title>Differentiation of opiate and neuroleptic receptor binding in rat brain</title><author>Leysen, Josee ; Tollenaere, Jan P. ; Koch, Michel H.J. ; Laduron, Pierre</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c356t-ec20eee824ed87b280545cfa98446242f1f9200912eb41a3046f5036df50e62e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1977</creationdate><topic>Animals</topic><topic>Benzimidazoles - metabolism</topic><topic>Benzimidazoles - pharmacology</topic><topic>Brain - metabolism</topic><topic>Female</topic><topic>Fentanyl - analogs & derivatives</topic><topic>Fentanyl - metabolism</topic><topic>Fentanyl - pharmacology</topic><topic>Haloperidol - metabolism</topic><topic>Haloperidol - pharmacology</topic><topic>Meperidine - metabolism</topic><topic>Meperidine - pharmacology</topic><topic>Neuroleptic receptor</topic><topic>Opiate receptor</topic><topic>Piperidines - metabolism</topic><topic>Piperidines - pharmacology</topic><topic>Rats</topic><topic>Receptors, Drug</topic><topic>Receptors, Opioid</topic><topic>Spiro Compounds - metabolism</topic><topic>Spiro Compounds - pharmacology</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Leysen, Josee</creatorcontrib><creatorcontrib>Tollenaere, Jan P.</creatorcontrib><creatorcontrib>Koch, Michel H.J.</creatorcontrib><creatorcontrib>Laduron, Pierre</creatorcontrib><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>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Leysen, Josee</au><au>Tollenaere, Jan P.</au><au>Koch, Michel H.J.</au><au>Laduron, Pierre</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Differentiation of opiate and neuroleptic receptor binding in rat brain</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1977-06-01</date><risdate>1977</risdate><volume>43</volume><issue>3</issue><spage>253</spage><epage>267</epage><pages>253-267</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><abstract>For 6 large series of compounds derived from the piperidine moieties of spiperone, pimozide, haloperidol, pethidine, fentanyl and 4-methocarboxyl-fentanyl, IC
50 values were determined in the opiate and neuroleptic binding assay using [
3H]-fentanyl and [
3H]-haloperidol as ligands, respectively. The specificity and difference between both receptors were demonstrated on the basis of several criteria (1) the stereospecificity of the binding (2) the significant correlation between the in vitro activity of the drugs and their pharmacological potency in vivo, notwithstanding some discrepancies which are probably of pharmacokinetic and/or metabolic origin (3) the ability to discriminate between morphinomimetic and neuroleptic drugs by the differential affinity for their specific receptor (4) the structure—activity relationships derived from the in vitro data indicating that the structural requirements for high affinity binding in vitro parallel those for high in vivo potency (5) a demonstration, on the basis of physicochemical principles, of the difference in binding mechanism between morphinomimetics and neuroleptics to their respective receptor.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>194781</pmid><doi>10.1016/0014-2999(77)90025-5</doi><tpages>15</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0014-2999 |
| ispartof | European journal of pharmacology, 1977-06, Vol.43 (3), p.253-267 |
| issn | 0014-2999 1879-0712 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Benzimidazoles - metabolism Benzimidazoles - pharmacology Brain - metabolism Female Fentanyl - analogs & derivatives Fentanyl - metabolism Fentanyl - pharmacology Haloperidol - metabolism Haloperidol - pharmacology Meperidine - metabolism Meperidine - pharmacology Neuroleptic receptor Opiate receptor Piperidines - metabolism Piperidines - pharmacology Rats Receptors, Drug Receptors, Opioid Spiro Compounds - metabolism Spiro Compounds - pharmacology Structure-Activity Relationship |
| title | Differentiation of opiate and neuroleptic receptor binding in rat brain |
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