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New base-altered adenosine analogues: Synthesis and affinity at adenosine A1 and A2A receptors |
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| Authors: | Seung B Ha Neli Melman Kenneth A Jacobson Vasu Nair |
| Institution: | a Department of Chemistry, The University of Iowa, Iowa City, Iowa 52242, U.S.A. b Molecular Recognition Section, Laboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, Bethesda, MD 20892, U.S.A. |
| Abstract: | N6-Substituted adenosine analogues containing cyclic hydrazines or chiral hydroxy (ar)alkyl groups, designed to interact with the S2 and S3 receptor subregions, have been synthesized and their binding to the adenosine A1 and A2A receptors have been investigated. Examples of both types of compounds were found to exhibit highly selective binding (Ki in low nM range) to the rat A1 receptor. |
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