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Fundamental difference between the molecular interactions of agonists and antagonists with the β-adrenergic receptor

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Abstract

Antagonist binding to the β-adrenergic receptor is largely entropy driven, with only a small enthalpy component. The binding of agonists, on the other hand, is associated with a large decrease in enthalpy which permits a highly unfavourable decrease in entropy. The thermodynamic differences between the binding of agonists and antagonists may provide new insights into the molecular basis for hormone stimulation of adenylate cyclase activity.

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Authors and Affiliations

  1. Department of Pharmacology, University of Colorado Medical Center, 4200 East Ninth Avenue, Denver, Colorado, 80262

    Gregory A. Weiland, Kenneth P. Minneman & Perry B. Molinoff

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  1. Gregory A. Weiland
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  2. Kenneth P. Minneman
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  3. Perry B. Molinoff
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Weiland, G., Minneman, K. & Molinoff, P. Fundamental difference between the molecular interactions of agonists and antagonists with the β-adrenergic receptor. Nature 281, 114–117 (1979). https://doi.org/10.1038/281114a0

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