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• W2073572009 abstract "The present commentary surveys the methods for obtaining the thermodynamic parameters of the drug–receptor binding equilibrium, ΔG°, ΔH°, ΔS°, and ΔC°p (standard free energy, enthalpy, entropy, and heat capacity, respectively). Moreover, it reviews the available thermodynamic data for the binding of agonists and antagonists to several G-protein coupled receptors (GPCRs) and ligand-gated ion channel receptors (LGICRs). In particular, thermodynamic data for five GPCRs (β-adrenergic, adenosine A1, adenosine A2A, dopamine D2, and 5-HT1A) and four LGICRs (glycine, GABAA, 5-HT3, and nicotinic) have been collected and analyzed. Among these receptor systems, seven (three GPCRs and all LGICRs) show “thermodynamic agonist–antagonist discrimination”: when the agonist binding to a given receptor is entropy-driven, the binding of its antagonist is enthalpy-driven, or vice versa. A scatter plot of all entropy versus enthalpy values of the database gives a regression line with the equation TΔS° (kJ mol−1; T = 298.15 K) = 40.3 (± 0.7) + 1.00 (±0.01) ΔH° (kJ mol−1); N = 184; r = 0.981; P < 0.0001 – which is of the form ΔH° = β · ΔS°, revealing the presence of the “enthalpy–entropy compensation” phenomenon. This means that any decrease of binding enthalpy is compensated for by a parallel decrease of binding entropy, and vice versa, in such a manner that affinity constant values (KA) of drug–receptor equilibrium (ΔG° = −RT ln KA = ΔH° − TΔS°) cannot be greater than 1011 M−1. According to the most recent hypotheses concerning drug–receptor interaction mechanisms, these thermodynamic phenomena appear to be a consequence of the rearrangement of solvent molecules that occurs during the binding." @default.
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• W2073572009 date "2000-12-01" @default.
• W2073572009 modified "2023-09-27" @default.
• W2073572009 title "Can thermodynamic measurements of receptor binding yield information on drug affinity and efficacy?" @default.
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• W2073572009 doi "https://doi.org/10.1016/s0006-2952(00)00368-3" @default.
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