Vinburnine decelerates [3H]N-methylscopolamine binding to recombinant human muscarinic M1-M4 acetylcholine receptors
The kinetics of [3H]N-methylscopolamine binding to membranes of Chinese hamster ovary (CHO) cells expressing muscarinic M(1)-M(4) acetylcholine receptors was studied. [3H]N-methylscopolamine dissociation was used for the "single-point" analysis of allosteric modulation by vinburnine (L-ebu...
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| Veröffentlicht in: | European journal of pharmacology 2004-01, Vol.483 (2-3), p.229-232 |
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| creator | MAKSAY, Gabor BIRO, Timea KISS, Béla |
| description | The kinetics of [3H]N-methylscopolamine binding to membranes of Chinese hamster ovary (CHO) cells expressing muscarinic M(1)-M(4) acetylcholine receptors was studied. [3H]N-methylscopolamine dissociation was used for the "single-point" analysis of allosteric modulation by vinburnine (L-eburnamonine). [3H]N-methylscopolamine dissociation was decelerated by vinburnine with EC(50) values of 29.5, 4.1, 9.5 and 15.0 microM for muscarinic M(1)-M(4) receptors, respectively. Acetylcholine doubled the EC(50) of vinburnine for muscarinic M(3) receptors. These kinetic EC(50) values correlated with equilibrium binding constants, supporting the ternary allosteric model. Vinburnine also decelerated the association of [3H]N-methylscopolamine binding, resulting in opposite cooperativity for muscarinic M(1) and M(2) receptors. |
| doi_str_mv | 10.1016/j.ejphar.2003.10.039 |
| format | Article |
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[3H]N-methylscopolamine dissociation was used for the "single-point" analysis of allosteric modulation by vinburnine (L-eburnamonine). [3H]N-methylscopolamine dissociation was decelerated by vinburnine with EC(50) values of 29.5, 4.1, 9.5 and 15.0 microM for muscarinic M(1)-M(4) receptors, respectively. Acetylcholine doubled the EC(50) of vinburnine for muscarinic M(3) receptors. These kinetic EC(50) values correlated with equilibrium binding constants, supporting the ternary allosteric model. 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[3H]N-methylscopolamine dissociation was used for the "single-point" analysis of allosteric modulation by vinburnine (L-eburnamonine). [3H]N-methylscopolamine dissociation was decelerated by vinburnine with EC(50) values of 29.5, 4.1, 9.5 and 15.0 microM for muscarinic M(1)-M(4) receptors, respectively. Acetylcholine doubled the EC(50) of vinburnine for muscarinic M(3) receptors. These kinetic EC(50) values correlated with equilibrium binding constants, supporting the ternary allosteric model. Vinburnine also decelerated the association of [3H]N-methylscopolamine binding, resulting in opposite cooperativity for muscarinic M(1) and M(2) receptors.</description><subject>Allosteric Regulation - drug effects</subject><subject>Allosteric Regulation - physiology</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>CHO Cells</subject><subject>Cricetinae</subject><subject>Humans</subject><subject>Medical sciences</subject><subject>N-Methylscopolamine - antagonists & inhibitors</subject><subject>N-Methylscopolamine - metabolism</subject><subject>Pharmacology. Drug treatments</subject><subject>Protein Binding - drug effects</subject><subject>Protein Binding - physiology</subject><subject>Receptor, Muscarinic M1 - metabolism</subject><subject>Receptor, Muscarinic M2 - metabolism</subject><subject>Receptor, Muscarinic M3 - metabolism</subject><subject>Receptor, Muscarinic M4 - metabolism</subject><subject>Receptors, Muscarinic - metabolism</subject><subject>Recombinant Proteins - metabolism</subject><subject>Tritium - metabolism</subject><subject>Vinca Alkaloids - pharmacology</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkMFq3DAQhkVoaTZJ3yAUX9qbNyPJiq1jCWkTSNJLm0spZiyPu1psyZXkw759ZXYhp2Fmvn9gPsauOWw58Nub_Zb28w7DVgDIPNqC1Gdsw5tal1Bz8Y5tAHhVCq31ObuIcQ8ASgv1gZ3zqhaac75h6dW6bgnOOip6MjRSwESx-C0f_ryUE6XdYYzGz37EaWU663rr_hbJF4GMn3KPLhW7ZUJXTEs0GKyzpnjm5XNVoKF0GM3Oj2s2B2hOPsQr9n7AMdLHU71kv77d_7x7KJ9-fH-8-_pUGlE1qUSpK9kL4ELXRg2oFPagmtsBsEfq6rxTSGQ06apWxhjRCAKstOgISCt5yb4c787B_1sopnayMf84oiO_xLaBbJIrkcHqCJrgYww0tHOwE4ZDy6Fdbbf79mi7XW2v02w7xz6d7i_dRP1b6KQ3A59PAGYz4xDQGRvfOCUb3Wgp_wMPlYyo</recordid><startdate>20040112</startdate><enddate>20040112</enddate><creator>MAKSAY, Gabor</creator><creator>BIRO, Timea</creator><creator>KISS, Béla</creator><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>20040112</creationdate><title>Vinburnine decelerates [3H]N-methylscopolamine binding to recombinant human muscarinic M1-M4 acetylcholine receptors</title><author>MAKSAY, Gabor ; BIRO, Timea ; KISS, Béla</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c248t-a3943d201297c5fa55ad0586f0adaeb73d25aeec9e9475ccc282e0a492be0e953</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><topic>Allosteric Regulation - drug effects</topic><topic>Allosteric Regulation - physiology</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>CHO Cells</topic><topic>Cricetinae</topic><topic>Humans</topic><topic>Medical sciences</topic><topic>N-Methylscopolamine - antagonists & inhibitors</topic><topic>N-Methylscopolamine - metabolism</topic><topic>Pharmacology. Drug treatments</topic><topic>Protein Binding - drug effects</topic><topic>Protein Binding - physiology</topic><topic>Receptor, Muscarinic M1 - metabolism</topic><topic>Receptor, Muscarinic M2 - metabolism</topic><topic>Receptor, Muscarinic M3 - metabolism</topic><topic>Receptor, Muscarinic M4 - metabolism</topic><topic>Receptors, Muscarinic - metabolism</topic><topic>Recombinant Proteins - metabolism</topic><topic>Tritium - metabolism</topic><topic>Vinca Alkaloids - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>MAKSAY, Gabor</creatorcontrib><creatorcontrib>BIRO, Timea</creatorcontrib><creatorcontrib>KISS, Béla</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>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>MAKSAY, Gabor</au><au>BIRO, Timea</au><au>KISS, Béla</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Vinburnine decelerates [3H]N-methylscopolamine binding to recombinant human muscarinic M1-M4 acetylcholine receptors</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>2004-01-12</date><risdate>2004</risdate><volume>483</volume><issue>2-3</issue><spage>229</spage><epage>232</epage><pages>229-232</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>The kinetics of [3H]N-methylscopolamine binding to membranes of Chinese hamster ovary (CHO) cells expressing muscarinic M(1)-M(4) acetylcholine receptors was studied. [3H]N-methylscopolamine dissociation was used for the "single-point" analysis of allosteric modulation by vinburnine (L-eburnamonine). [3H]N-methylscopolamine dissociation was decelerated by vinburnine with EC(50) values of 29.5, 4.1, 9.5 and 15.0 microM for muscarinic M(1)-M(4) receptors, respectively. Acetylcholine doubled the EC(50) of vinburnine for muscarinic M(3) receptors. These kinetic EC(50) values correlated with equilibrium binding constants, supporting the ternary allosteric model. Vinburnine also decelerated the association of [3H]N-methylscopolamine binding, resulting in opposite cooperativity for muscarinic M(1) and M(2) receptors.</abstract><cop>Amsterdam</cop><pub>Elsevier</pub><pmid>14729111</pmid><doi>10.1016/j.ejphar.2003.10.039</doi><tpages>4</tpages></addata></record> |
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| subjects | Allosteric Regulation - drug effects Allosteric Regulation - physiology Animals Biological and medical sciences CHO Cells Cricetinae Humans Medical sciences N-Methylscopolamine - antagonists & inhibitors N-Methylscopolamine - metabolism Pharmacology. Drug treatments Protein Binding - drug effects Protein Binding - physiology Receptor, Muscarinic M1 - metabolism Receptor, Muscarinic M2 - metabolism Receptor, Muscarinic M3 - metabolism Receptor, Muscarinic M4 - metabolism Receptors, Muscarinic - metabolism Recombinant Proteins - metabolism Tritium - metabolism Vinca Alkaloids - pharmacology |
| title | Vinburnine decelerates [3H]N-methylscopolamine binding to recombinant human muscarinic M1-M4 acetylcholine receptors |
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