Analysis of competitive antagonism when this property occurs as part of a pharmacological resultant
1 In this paper, pharmacological resultant is defined as the net effect of a single compound resulting from the simultaneous expression of two or more specific actions. 2 The principles of concentration‐ratio analysis are extended to develop a method for detecting and quantifying competitive antagon...
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| Veröffentlicht in: | British journal of pharmacology 1986-11, Vol.89 (3), p.547-555 |
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| container_title | British journal of pharmacology |
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| creator | Black, J.W. Gerskowitch, V.P. Left, P. Shankley, N. P. |
| description | 1
In this paper, pharmacological resultant is defined as the net effect of a single compound resulting from the simultaneous expression of two or more specific actions.
2
The principles of concentration‐ratio analysis are extended to develop a method for detecting and quantifying competitive antagonism when this property is a component of a pharmacological resultant. The method is general to the extent that it allows analysis of competitive antagonism in combination with all types of post‐receptor intervention. Essentially it depends on the altered expression of competition by a reference antagonist. It incorporates tests for validating its application and it is independent of agonist concentration‐effect curve shape: in these respects the method is analogous to Schild plot‐analysis of simple competition.
3
The methodology for the practical application of the analysis is exemplified by studying the net effect of a combination of a phosphodiesterase inhibitor (isobutylmethylxanthine) and histamine H2‐ receptor antagonist (metiamide) on histamine‐stimulated tachycardia in guinea‐pig, isolated, right atrium. Cimetidine was used as the reference antagonist.
4
The equation used in this analysis is similar in form to one recently described by Hughes & Mackay (1985) to elucidate the situation when competitive antagonism occurs in combination with functional interactions. The relation between their method and the present analysis is discussed. |
| doi_str_mv | 10.1111/j.1476-5381.1986.tb11155.x |
| format | Article |
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In this paper, pharmacological resultant is defined as the net effect of a single compound resulting from the simultaneous expression of two or more specific actions.
2
The principles of concentration‐ratio analysis are extended to develop a method for detecting and quantifying competitive antagonism when this property is a component of a pharmacological resultant. The method is general to the extent that it allows analysis of competitive antagonism in combination with all types of post‐receptor intervention. Essentially it depends on the altered expression of competition by a reference antagonist. It incorporates tests for validating its application and it is independent of agonist concentration‐effect curve shape: in these respects the method is analogous to Schild plot‐analysis of simple competition.
3
The methodology for the practical application of the analysis is exemplified by studying the net effect of a combination of a phosphodiesterase inhibitor (isobutylmethylxanthine) and histamine H2‐ receptor antagonist (metiamide) on histamine‐stimulated tachycardia in guinea‐pig, isolated, right atrium. Cimetidine was used as the reference antagonist.
4
The equation used in this analysis is similar in form to one recently described by Hughes & Mackay (1985) to elucidate the situation when competitive antagonism occurs in combination with functional interactions. The relation between their method and the present analysis is discussed.</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1111/j.1476-5381.1986.tb11155.x</identifier><identifier>PMID: 2432983</identifier><identifier>CODEN: BJPCBM</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>1-Methyl-3-isobutylxanthine - pharmacology ; Animals ; Applied sciences ; Biological and medical sciences ; Cimetidine - pharmacology ; Drug Antagonism ; Exact sciences and technology ; General pharmacology ; Guinea Pigs ; Heart Rate - drug effects ; Imidazoles - pharmacology ; Impromidine ; In Vitro Techniques ; Male ; Medical sciences ; Metiamide - pharmacology ; Models, Biological ; Other techniques and industries ; Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions ; Pharmacology. Drug treatments</subject><ispartof>British journal of pharmacology, 1986-11, Vol.89 (3), p.547-555</ispartof><rights>1986 British Pharmacological Society</rights><rights>1987 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c5365-5ae28fa2b50bf97889a03b8d89b1db29eb9c375fc3c6ad1a03a49f27a7d2e5ff3</citedby><cites>FETCH-LOGICAL-c5365-5ae28fa2b50bf97889a03b8d89b1db29eb9c375fc3c6ad1a03a49f27a7d2e5ff3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1917162/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1917162/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,727,780,784,885,27924,27925,53791,53793</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=8320500$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=8353214$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2432983$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Black, J.W.</creatorcontrib><creatorcontrib>Gerskowitch, V.P.</creatorcontrib><creatorcontrib>Left, P.</creatorcontrib><creatorcontrib>Shankley, N. P.</creatorcontrib><title>Analysis of competitive antagonism when this property occurs as part of a pharmacological resultant</title><title>British journal of pharmacology</title><addtitle>Br J Pharmacol</addtitle><description>1
In this paper, pharmacological resultant is defined as the net effect of a single compound resulting from the simultaneous expression of two or more specific actions.
2
The principles of concentration‐ratio analysis are extended to develop a method for detecting and quantifying competitive antagonism when this property is a component of a pharmacological resultant. The method is general to the extent that it allows analysis of competitive antagonism in combination with all types of post‐receptor intervention. Essentially it depends on the altered expression of competition by a reference antagonist. It incorporates tests for validating its application and it is independent of agonist concentration‐effect curve shape: in these respects the method is analogous to Schild plot‐analysis of simple competition.
3
The methodology for the practical application of the analysis is exemplified by studying the net effect of a combination of a phosphodiesterase inhibitor (isobutylmethylxanthine) and histamine H2‐ receptor antagonist (metiamide) on histamine‐stimulated tachycardia in guinea‐pig, isolated, right atrium. Cimetidine was used as the reference antagonist.
4
The equation used in this analysis is similar in form to one recently described by Hughes & Mackay (1985) to elucidate the situation when competitive antagonism occurs in combination with functional interactions. The relation between their method and the present analysis is discussed.</description><subject>1-Methyl-3-isobutylxanthine - pharmacology</subject><subject>Animals</subject><subject>Applied sciences</subject><subject>Biological and medical sciences</subject><subject>Cimetidine - pharmacology</subject><subject>Drug Antagonism</subject><subject>Exact sciences and technology</subject><subject>General pharmacology</subject><subject>Guinea Pigs</subject><subject>Heart Rate - drug effects</subject><subject>Imidazoles - pharmacology</subject><subject>Impromidine</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Metiamide - pharmacology</subject><subject>Models, Biological</subject><subject>Other techniques and industries</subject><subject>Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions</subject><subject>Pharmacology. Drug treatments</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1986</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqVkE2L1DAYx4Mo67j6EYQgXlvzMmkTD-Luoq6woAc9h6dpMpOhbUqS2d359qbOMOhJzCXh-b884YfQG0pqWs67XU3XbVMJLmlNlWzq3JWxEPXjE7Q6S0_RihDSVpRK-Ry9SGlHSBFbcYEu2JozJfkKmasJhkPyCQeHTRhnm3329xbDlGETJp9G_LC1E87b4pljmG3MBxyM2ceEoYwg5iULeN5CHMGEIWy8gQFHm_ZDLj0v0TMHQ7KvTvcl-vn504-b2-ru25evN1d3lRG8EZUAy6QD1gnSOdVKqYDwTvZSdbTvmLKdMrwVznDTQE-LCGvlWAttz6xwjl-iD8feed-Ntjd2yhEGPUc_QjzoAF7_rUx-qzfhXlNFW9qwUvD-WGBiSClad85SohfyeqcXvHrBqxfy-kReP5bw6z-3n6Mn1EV_e9IhFTwuwmR8OtskF5zR9b9tjAhCiu3j0fbgB3v4j3_q6--3v5_8FwKlsY8</recordid><startdate>198611</startdate><enddate>198611</enddate><creator>Black, J.W.</creator><creator>Gerskowitch, V.P.</creator><creator>Left, P.</creator><creator>Shankley, N. P.</creator><general>Blackwell Publishing Ltd</general><general>Nature Publishing</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>5PM</scope></search><sort><creationdate>198611</creationdate><title>Analysis of competitive antagonism when this property occurs as part of a pharmacological resultant</title><author>Black, J.W. ; Gerskowitch, V.P. ; Left, P. ; Shankley, N. P.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c5365-5ae28fa2b50bf97889a03b8d89b1db29eb9c375fc3c6ad1a03a49f27a7d2e5ff3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1986</creationdate><topic>1-Methyl-3-isobutylxanthine - pharmacology</topic><topic>Animals</topic><topic>Applied sciences</topic><topic>Biological and medical sciences</topic><topic>Cimetidine - pharmacology</topic><topic>Drug Antagonism</topic><topic>Exact sciences and technology</topic><topic>General pharmacology</topic><topic>Guinea Pigs</topic><topic>Heart Rate - drug effects</topic><topic>Imidazoles - pharmacology</topic><topic>Impromidine</topic><topic>In Vitro Techniques</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Metiamide - pharmacology</topic><topic>Models, Biological</topic><topic>Other techniques and industries</topic><topic>Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions</topic><topic>Pharmacology. Drug treatments</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Black, J.W.</creatorcontrib><creatorcontrib>Gerskowitch, V.P.</creatorcontrib><creatorcontrib>Left, P.</creatorcontrib><creatorcontrib>Shankley, N. P.</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>PubMed Central (Full Participant titles)</collection><jtitle>British journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Black, J.W.</au><au>Gerskowitch, V.P.</au><au>Left, P.</au><au>Shankley, N. P.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Analysis of competitive antagonism when this property occurs as part of a pharmacological resultant</atitle><jtitle>British journal of pharmacology</jtitle><addtitle>Br J Pharmacol</addtitle><date>1986-11</date><risdate>1986</risdate><volume>89</volume><issue>3</issue><spage>547</spage><epage>555</epage><pages>547-555</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><coden>BJPCBM</coden><abstract>1
In this paper, pharmacological resultant is defined as the net effect of a single compound resulting from the simultaneous expression of two or more specific actions.
2
The principles of concentration‐ratio analysis are extended to develop a method for detecting and quantifying competitive antagonism when this property is a component of a pharmacological resultant. The method is general to the extent that it allows analysis of competitive antagonism in combination with all types of post‐receptor intervention. Essentially it depends on the altered expression of competition by a reference antagonist. It incorporates tests for validating its application and it is independent of agonist concentration‐effect curve shape: in these respects the method is analogous to Schild plot‐analysis of simple competition.
3
The methodology for the practical application of the analysis is exemplified by studying the net effect of a combination of a phosphodiesterase inhibitor (isobutylmethylxanthine) and histamine H2‐ receptor antagonist (metiamide) on histamine‐stimulated tachycardia in guinea‐pig, isolated, right atrium. Cimetidine was used as the reference antagonist.
4
The equation used in this analysis is similar in form to one recently described by Hughes & Mackay (1985) to elucidate the situation when competitive antagonism occurs in combination with functional interactions. The relation between their method and the present analysis is discussed.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>2432983</pmid><doi>10.1111/j.1476-5381.1986.tb11155.x</doi><tpages>9</tpages><oa>free_for_read</oa></addata></record> |
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| source | MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; PubMed Central; Alma/SFX Local Collection |
| subjects | 1-Methyl-3-isobutylxanthine - pharmacology Animals Applied sciences Biological and medical sciences Cimetidine - pharmacology Drug Antagonism Exact sciences and technology General pharmacology Guinea Pigs Heart Rate - drug effects Imidazoles - pharmacology Impromidine In Vitro Techniques Male Medical sciences Metiamide - pharmacology Models, Biological Other techniques and industries Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions Pharmacology. Drug treatments |
| title | Analysis of competitive antagonism when this property occurs as part of a pharmacological resultant |
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