View : 96 Download: 0
Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5′-ribofuran-uronamide moiety
- Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5′-ribofuran-uronamide moiety
- Gao Z.-G.; Joshi B.V.; Klutz A.M.; Kim S.-K.; Lee H.W.; Kim H.O.; Jeong L.S.; Jacobson K.A.
- Ewha Authors
- Issue Date
- Journal Title
- Bioorganic and Medicinal Chemistry Letters
- Bioorganic and Medicinal Chemistry Letters vol. 16, no. 3, pp. 596 - 601
- SCIE; SCOPUS
- Document Type
- 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.
- Appears in Collections:
- 약학대학 > 약학과 > Journal papers
- Files in This Item:
There are no files associated with this item.
- RIS (EndNote)
- XLS (Excel)
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.