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The effects of distal structural changes on biological activity may be studied, using a “functionalized congener” strategy, in which suitably placed chemically reactive chains lead to biologically active conjugates. Probes for photoaffinity labeling, chemical affinity labeling, spectroscopic characterization and affinity chromatography of adenosine receptors have been derived from purine amine congeners (XAC, ADAC for At-receptors and APEC for Ap-receptors). Also, drug conjugates, including prodrugs and lipids, have been designed as potential Pharmacological agents.
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Jacobson et al. (1991) studied this question.
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