Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins.

@article{Costa1989AntagonistsWN,
  title={Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins.},
  author={T. V. V. Costa and A. Herz},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={1989},
  volume={86 19},
  pages={7321-5}
}
According to classical models of drug-receptor interactions, competitive antagonists share with agonists the ability to bind to a common site on the receptor molecule. However, they are different from agonists, as they cannot trigger the "stimulus" that leads to biological responses--i.e., they lack intrinsic activity. For those receptors whose signals are transduced to effector systems by GTP-binding regulatory proteins (G proteins), a mechanistic equivalent of such a stimulus is an increased… CONTINUE READING
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