Mepyramine, a histamine H1 receptor inverse agonist, binds preferentially to a G protein-coupled form of the receptor and sequesters G protein.

@article{Fitzsimons2004MepyramineAH,
  title={Mepyramine, a histamine H1 receptor inverse agonist, binds preferentially to a G protein-coupled form of the receptor and sequesters G protein.},
  author={Carlos Patricio Fitzsimons and Federico Monczor and Natalia Cristina Fern{\'a}ndez and Carina Shayo and Carlos A. Davio},
  journal={The Journal of biological chemistry},
  year={2004},
  volume={279 33},
  pages={
          34431-9
        }
}
Accurate characterization of the molecular mechanisms of the action of ligands is an extremely important issue for their appropriate research, pharmacological, and therapeutic uses. In view of this fact, the aim of the present work was to investigate the mechanisms involved in the actions of mepyramine at the guinea pig H(1) receptor stably expressed in Chinese hamster ovary cells. We found that mepyramine is able to decrease the basal constitutive activity of the guinea pig H(1) receptor, to… CONTINUE READING
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Mechanisms Associated with Mepyramine Inverse Agonism

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