Decavanadate, a P2X receptor antagonist, and its use to study ligand interactions with P2X7 receptors
In this study we have studied decavanadate effects at P2X receptors. Decavanadate competitively blocked 2'- and 3'-O-(4benzoylbenzoyl) ATP (BzATP) stimulated ethidium accumulation in HEK293 cells expressing human recombinant P2X7 receptors (pK(B) 7.5). The effects of decavanadate were rapi...
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| Veröffentlicht in: | European journal of pharmacology 2006-03, Vol.534 (1-3), p.19-29 |
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| container_title | European journal of pharmacology |
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| creator | MICHEL, Anton D MENGLE XING THOMPSON, Kyla M JONES, Clare A HUMPHREY, Patrick P. A |
| description | In this study we have studied decavanadate effects at P2X receptors. Decavanadate competitively blocked 2'- and 3'-O-(4benzoylbenzoyl) ATP (BzATP) stimulated ethidium accumulation in HEK293 cells expressing human recombinant P2X7 receptors (pK(B) 7.5). The effects of decavanadate were rapid (minutes) in both onset and offset and contrasted with the much slower kinetics of pyridoxal 5-phosphate (P5P), Coomassie brilliant blue (CBB) and 1-[N,O-bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine (KN62). Decavanadate competitively blocked the slowly reversible, or irreversible, blockade of the P2X7 receptor produced by P5P and oxidised ATP suggesting competition for a common binding site. However, the interaction between decavanadate and KN62 was non-competitive. Decavanadate also blocked P2X2 and P2X4 receptors but with slightly lower potency. These data demonstrate that decavanadate is the first reversible and competitive antagonist of the P2X7 receptor and is a useful tool for studying the mechanism of interaction of ligands with the P2X7 receptor. |
| doi_str_mv | 10.1016/j.ejphar.2006.01.009 |
| format | Article |
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Decavanadate also blocked P2X2 and P2X4 receptors but with slightly lower potency. These data demonstrate that decavanadate is the first reversible and competitive antagonist of the P2X7 receptor and is a useful tool for studying the mechanism of interaction of ligands with the P2X7 receptor.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/j.ejphar.2006.01.009</identifier><identifier>PMID: 16487507</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier</publisher><subject>Biological and medical sciences ; Calcium Signaling - drug effects ; Cell Line ; Dose-Response Relationship, Drug ; Humans ; Kinetics ; Ligands ; Medical sciences ; Membrane Potentials - drug effects ; Pharmacology. 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A</creatorcontrib><title>Decavanadate, a P2X receptor antagonist, and its use to study ligand interactions with P2X7 receptors</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>In this study we have studied decavanadate effects at P2X receptors. Decavanadate competitively blocked 2'- and 3'-O-(4benzoylbenzoyl) ATP (BzATP) stimulated ethidium accumulation in HEK293 cells expressing human recombinant P2X7 receptors (pK(B) 7.5). The effects of decavanadate were rapid (minutes) in both onset and offset and contrasted with the much slower kinetics of pyridoxal 5-phosphate (P5P), Coomassie brilliant blue (CBB) and 1-[N,O-bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine (KN62). Decavanadate competitively blocked the slowly reversible, or irreversible, blockade of the P2X7 receptor produced by P5P and oxidised ATP suggesting competition for a common binding site. However, the interaction between decavanadate and KN62 was non-competitive. Decavanadate also blocked P2X2 and P2X4 receptors but with slightly lower potency. These data demonstrate that decavanadate is the first reversible and competitive antagonist of the P2X7 receptor and is a useful tool for studying the mechanism of interaction of ligands with the P2X7 receptor.</description><subject>Biological and medical sciences</subject><subject>Calcium Signaling - drug effects</subject><subject>Cell Line</subject><subject>Dose-Response Relationship, Drug</subject><subject>Humans</subject><subject>Kinetics</subject><subject>Ligands</subject><subject>Medical sciences</subject><subject>Membrane Potentials - drug effects</subject><subject>Pharmacology. Drug treatments</subject><subject>Purinergic P2 Receptor Antagonists</subject><subject>Pyridoxal Phosphate - pharmacology</subject><subject>Receptors, Purinergic P2 - genetics</subject><subject>Receptors, Purinergic P2X2</subject><subject>Receptors, Purinergic P2X4</subject><subject>Receptors, Purinergic P2X7</subject><subject>Rosaniline Dyes - pharmacology</subject><subject>Transfection</subject><subject>Vanadates - pharmacology</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2006</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkMtu2zAQAImiQeO4_YMg4KU9ReqS4kM8FknzAAwkhwTojVhRlC1DllySSuC_r1wb8WmB3dk5DCGXDHIGTP1c5369XWHIOYDKgeUA5hOZsVKbDDTjn8kMgImMG2POyUWMawCQhssv5JwpUWoJekb8rXf4hj3WmPw1RfrM_9Dgnd-mIVDsEy6Hvo1pOvU1bVOkY_Q0DTSmsd7Rrl3-3_fJB3SpHfpI39u02mv0hyd-JWcNdtF_O845eb37_XLzkC2e7h9vfi0yVxQyZUYoo5ngoIVhCFoJDUo7U9bCNHUjVV2ZRnmFUmimZF1wKKQxFfCqrLioijn5cfBuw_B39DHZTRud7zrs_TBGq7QuSlByAsUBdGGIMfjGbkO7wbCzDOw-r13bQ167z2uB2Snv9HZ19I_Vxtenp2PPCfh-BDA67JqAvWvjidOy5JwVxT9Q8oPB</recordid><startdate>20060318</startdate><enddate>20060318</enddate><creator>MICHEL, Anton D</creator><creator>MENGLE XING</creator><creator>THOMPSON, Kyla M</creator><creator>JONES, Clare A</creator><creator>HUMPHREY, Patrick P. 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A</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c335t-9469714207491a07647067c98d49fdf56db9f6e6a547165d3203599b02b8b24b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2006</creationdate><topic>Biological and medical sciences</topic><topic>Calcium Signaling - drug effects</topic><topic>Cell Line</topic><topic>Dose-Response Relationship, Drug</topic><topic>Humans</topic><topic>Kinetics</topic><topic>Ligands</topic><topic>Medical sciences</topic><topic>Membrane Potentials - drug effects</topic><topic>Pharmacology. Drug treatments</topic><topic>Purinergic P2 Receptor Antagonists</topic><topic>Pyridoxal Phosphate - pharmacology</topic><topic>Receptors, Purinergic P2 - genetics</topic><topic>Receptors, Purinergic P2X2</topic><topic>Receptors, Purinergic P2X4</topic><topic>Receptors, Purinergic P2X7</topic><topic>Rosaniline Dyes - pharmacology</topic><topic>Transfection</topic><topic>Vanadates - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>MICHEL, Anton D</creatorcontrib><creatorcontrib>MENGLE XING</creatorcontrib><creatorcontrib>THOMPSON, Kyla M</creatorcontrib><creatorcontrib>JONES, Clare A</creatorcontrib><creatorcontrib>HUMPHREY, Patrick P. 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A</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Decavanadate, a P2X receptor antagonist, and its use to study ligand interactions with P2X7 receptors</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>2006-03-18</date><risdate>2006</risdate><volume>534</volume><issue>1-3</issue><spage>19</spage><epage>29</epage><pages>19-29</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>In this study we have studied decavanadate effects at P2X receptors. Decavanadate competitively blocked 2'- and 3'-O-(4benzoylbenzoyl) ATP (BzATP) stimulated ethidium accumulation in HEK293 cells expressing human recombinant P2X7 receptors (pK(B) 7.5). The effects of decavanadate were rapid (minutes) in both onset and offset and contrasted with the much slower kinetics of pyridoxal 5-phosphate (P5P), Coomassie brilliant blue (CBB) and 1-[N,O-bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine (KN62). Decavanadate competitively blocked the slowly reversible, or irreversible, blockade of the P2X7 receptor produced by P5P and oxidised ATP suggesting competition for a common binding site. However, the interaction between decavanadate and KN62 was non-competitive. Decavanadate also blocked P2X2 and P2X4 receptors but with slightly lower potency. These data demonstrate that decavanadate is the first reversible and competitive antagonist of the P2X7 receptor and is a useful tool for studying the mechanism of interaction of ligands with the P2X7 receptor.</abstract><cop>Amsterdam</cop><pub>Elsevier</pub><pmid>16487507</pmid><doi>10.1016/j.ejphar.2006.01.009</doi><tpages>11</tpages></addata></record> |
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| subjects | Biological and medical sciences Calcium Signaling - drug effects Cell Line Dose-Response Relationship, Drug Humans Kinetics Ligands Medical sciences Membrane Potentials - drug effects Pharmacology. Drug treatments Purinergic P2 Receptor Antagonists Pyridoxal Phosphate - pharmacology Receptors, Purinergic P2 - genetics Receptors, Purinergic P2X2 Receptors, Purinergic P2X4 Receptors, Purinergic P2X7 Rosaniline Dyes - pharmacology Transfection Vanadates - pharmacology |
| title | Decavanadate, a P2X receptor antagonist, and its use to study ligand interactions with P2X7 receptors |
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