Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors
A novel series of antagonists of the human P2X7 receptor is described. Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful pharmacological tools for evaluation of the role of P2X7 in disease.
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| Veröffentlicht in: | Journal of medicinal chemistry 2007-11, Vol.50 (24), p.5882-5885 |
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| container_end_page | 5885 |
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| container_issue | 24 |
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| container_title | Journal of medicinal chemistry |
| container_volume | 50 |
| creator | Furber, Mark Alcaraz, Lilian Bent, Janice E Beyerbach, Armin Bowers, Keith Braddock, Martin Caffrey, Moya V Cladingboel, David Collington, John Donald, David K Fagura, Malbinder Ince, Frank Kinchin, Elizabeth C Laurent, Celine Lawson, Mandy Luker, Timothy J Mortimore, Michael M P Pimm, Austen D Riley, Robert J Roberts, Nicola Robertson, Mark Theaker, Jill Thorne, Philip V Weaver, Richard Webborn, Peter Willis, Paul |
| description | A novel series of antagonists of the human P2X7 receptor is described. Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful pharmacological tools for evaluation of the role of P2X7 in disease. |
| format | Article |
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Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful pharmacological tools for evaluation of the role of P2X7 in disease.</description><subject>Adamantane - analogs & derivatives</subject><subject>Adamantane - chemical synthesis</subject><subject>Adamantane - pharmacology</subject><subject>Animals</subject><subject>Benzamides - chemical synthesis</subject><subject>Benzamides - pharmacology</subject><subject>Blood Proteins - metabolism</subject><subject>Crystallography, X-Ray</subject><subject>Humans</subject><subject>In Vitro Techniques</subject><subject>Interleukin-1beta - antagonists & inhibitors</subject><subject>Molecular Conformation</subject><subject>Monocytes - metabolism</subject><subject>Protein Binding</subject><subject>Purinergic P2 Receptor Antagonists</subject><subject>Rats</subject><subject>Receptors, Purinergic P2X7</subject><subject>Structure-Activity Relationship</subject><issn>0022-2623</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo10D1PwzAQBmAPIFoKfwF5QjBE-CONkxGVT6kSDB3YIic-g8Gxg-1UKr8eV5Tphnv0nt47QnNCGCtYxfgMncb4SQjhlPETNKOiqTgXfI5-7kzs_RbCDnuNR5_AJSydwhEs9MlsAUslB-mSdFB0MkJeDdLaYvAZTBbwK3u7Etc4QA9j8gHv7bt3JqZ4Y1yCYGH6Mq6gHSSJjfswnckunqFjLW2E88NcoM3D_Wb1VKxfHp9Xt-tiXJa84B1vtKoFUUoSoKxRWpak4bQHRgUoseR1DUIq3Wude5WV6pdal7KEvar5Al3-xY7Bf08QUzvkymBtLuSn2FZ1PsNKmuHFAU7dAKodgxlk2LX_z-K_72dngg</recordid><startdate>20071129</startdate><enddate>20071129</enddate><creator>Furber, Mark</creator><creator>Alcaraz, Lilian</creator><creator>Bent, Janice E</creator><creator>Beyerbach, Armin</creator><creator>Bowers, Keith</creator><creator>Braddock, Martin</creator><creator>Caffrey, Moya V</creator><creator>Cladingboel, David</creator><creator>Collington, John</creator><creator>Donald, David K</creator><creator>Fagura, Malbinder</creator><creator>Ince, Frank</creator><creator>Kinchin, Elizabeth C</creator><creator>Laurent, Celine</creator><creator>Lawson, Mandy</creator><creator>Luker, Timothy J</creator><creator>Mortimore, Michael M P</creator><creator>Pimm, Austen D</creator><creator>Riley, Robert J</creator><creator>Roberts, Nicola</creator><creator>Robertson, Mark</creator><creator>Theaker, Jill</creator><creator>Thorne, Philip V</creator><creator>Weaver, Richard</creator><creator>Webborn, Peter</creator><creator>Willis, Paul</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>20071129</creationdate><title>Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors</title><author>Furber, Mark ; 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| ispartof | Journal of medicinal chemistry, 2007-11, Vol.50 (24), p.5882-5885 |
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| source | American Chemical Society; MEDLINE |
| subjects | Adamantane - analogs & derivatives Adamantane - chemical synthesis Adamantane - pharmacology Animals Benzamides - chemical synthesis Benzamides - pharmacology Blood Proteins - metabolism Crystallography, X-Ray Humans In Vitro Techniques Interleukin-1beta - antagonists & inhibitors Molecular Conformation Monocytes - metabolism Protein Binding Purinergic P2 Receptor Antagonists Rats Receptors, Purinergic P2X7 Structure-Activity Relationship |
| title | Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors |
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