Full metadata record
DC Field | Value | Language |
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dc.contributor.author | 정낙신 | - |
dc.date.accessioned | 2018-05-30T08:14:15Z | - |
dc.date.available | 2018-05-30T08:14:15Z | - |
dc.date.issued | 2006 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.other | OAK-3120 | - |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/243572 | - |
dc.description.abstract | The highly selective agonists of the A3 adenosine receptor (AR), Cl-IB-MECA (2-chloro-N6-(3-iodobenzyl)-5′-N- methylcarboxamidoadenosine), and its 4′-thio analogue, were successfully converted into selective antagonists simply by appending a second N-methyl group on the 5′-uronamide position. The 2-chloro-5′-(N,N-dimethyl) uronamido analogues bound to, but did not activate, the human A3AR, with Ki values of 29 nM (4′-O) and 15 nM (4′-S), showing >100-fold selectivity over A1, A2A, and A 2BARs. Competitive antagonism was demonstrated by Schild analysis. The 2-(dimethylamino)-5′-(N,N-dimethyl)uronamido substitution also retained A3AR selectivity but lowered affinity. © 2005 Elsevier Ltd. All rights reserved. | - |
dc.language | English | - |
dc.title | Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5′-ribofuran-uronamide moiety | - |
dc.type | Article | - |
dc.relation.issue | 3 | - |
dc.relation.volume | 16 | - |
dc.relation.index | SCI | - |
dc.relation.index | SCIE | - |
dc.relation.index | SCOPUS | - |
dc.relation.startpage | 596 | - |
dc.relation.lastpage | 601 | - |
dc.relation.journaltitle | Bioorganic and Medicinal Chemistry Letters | - |
dc.identifier.doi | 10.1016/j.bmcl.2005.10.054 | - |
dc.identifier.wosid | WOS:000234641000023 | - |
dc.identifier.scopusid | 2-s2.0-29544432554 | - |
dc.author.google | Gao Z.-G. | - |
dc.author.google | Joshi B.V. | - |
dc.author.google | Klutz A.M. | - |
dc.author.google | Kim S.-K. | - |
dc.author.google | Lee H.W. | - |
dc.author.google | Kim H.O. | - |
dc.author.google | Jeong L.S. | - |
dc.author.google | Jacobson K.A. | - |
dc.contributor.scopusid | 정낙신(16028528200) | - |
dc.date.modifydate | 20211210153610 | - |