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. 1979 Sep 13;281(5727):114-7.
doi: 10.1038/281114a0.

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

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

G A Weiland et al. Nature. .

Abstract

Antagonist binding to the beta-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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