Proceedings of the PSK Conference (대한약학회:학술대회논문집)
- 2002.10a
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- Pages.365.1-365.1
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- 2002
DESIGN AND SYNTHESIS OF A3 ADENOSINE RECEPTOR LlGANDS, 2′-FLUORO ANALOGUES OF CI- IB-MECA
- Park, Jae-Gyu (College of Pharmacy, Ewha Womans University) ;
- Kim, Hea-Ok (Division of Chemistry and Molecular Engineering. Seoul national University) ;
- Moon, Hyung-Ryong (Division of Chemistry and Molecular Engineering. Seoul national University) ;
- Jeong, Lak-Shin (Division of Chemistry and Molecular Engineering. Seoul national University)
- Published : 2002.10.01
Abstract
Since adenosine A3 receptor has been cloned from rat brain. a number of compounds have been synthesized and evaluated for the binding affinity to this receptor. Among these. 2-chloro-N6-(3-iodobenzyl)-adenosine-5'-methylcarboxamide (2-CI-IB-MECA) has been found to be one of the most selective agonists (Ki = 1.0 nM) for rat adenosine A3 receptor. On the basis of the high binding affinity of 2-CI-IB-MECA to adenosine A3 receptor. it was interesting to find out whether 2'-hydroxyl group of 2-CI-IB-MECA is essential for the binding affnity to the receptor. (omitted)
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