Agonist versus antagonist action of ATP at the P2Y4 receptor is determined by the second extracellular loop.

@article{Herold2004AgonistVA,
  title={Agonist versus antagonist action of ATP at the P2Y4 receptor is determined by the second extracellular loop.},
  author={Christopher L Herold and A D Qi and T. Kendall Harden and Robert A Nicholas},
  journal={The Journal of biological chemistry},
  year={2004},
  volume={279 12},
  pages={11456-64}
}
UTP is a potent full agonist at both the human P2Y(4) (hP2Y(4)) and rat P2Y(4) (rP2Y(4)) receptor. In contrast, ATP is a potent full agonist at the rP2Y(4) receptor but is a similarly potent competitive antagonist at the hP2Y(4) receptor. To delineate the structural determinants of agonism versus antagonism in these species homologues, we expressed a series of human/rat P2Y(4) receptor chimeras in 1321N1 human astrocytoma cells and assessed the capacity of ATP and UTP to mobilize intracellular… CONTINUE READING

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