N6-Substituted adenosine derivatives: selectivity, efficacy, and species differences at A3 adenosine receptors.

@article{Gao2003N6SubstitutedAD,
  title={N6-Substituted adenosine derivatives: selectivity, efficacy, and species differences at A3 adenosine receptors.},
  author={Zhan-guo Gao and Joshua B. Blaustein and Ariel S Gross and N. Melman and Kenneth A. Jacobson},
  journal={Biochemical pharmacology},
  year={2003},
  volume={65 10},
  pages={1675-84}
}
The activation of the human A(3) adenosine receptor (AR) by a wide range of N(6)-substituted adenosine derivatives was studied in intact CHO cells stably expressing this receptor. Selectivity of binding at rat and human ARs was also determined. Among N(6)-alkyl substitutions, small N(6)-alkyl groups were associated with selectivity for human A(3)ARs vs. rat A(3)ARs, and multiple points of branching were associated with decreased hA(3)AR efficacy. N(6)-Cycloalkyl-substituted adenosines were full… CONTINUE READING

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