Negative antagonists promote an inactive conformation of the beta 2-adrenergic receptor.

@article{Samama1994NegativeAP,
  title={Negative antagonists promote an inactive conformation of the beta 2-adrenergic receptor.},
  author={Philippe Samama and Gang Pei and T. V. V. Costa and Susanna Cotecchia and Robert J Lefkowitz},
  journal={Molecular pharmacology},
  year={1994},
  volume={45 3},
  pages={390-4}
}
The beta 2-adrenergic receptor undergoes isomerization between an inactive conformation (R) and an active conformation (R*). The formation of the active conformation of the receptor molecule can be promoted by adrenergic agonists or by mutations in the third cytoplasmic domain that constitutively activate the receptor. Here we show that, of several beta-adrenergic receptor-blocking drugs tested, only two, ICI 118551 and betaxolol, inhibit the basal signaling activity of the beta 2-adrenergic… CONTINUE READING

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