Elsevier

Life Sciences

Volume 44, Issue 4, 1989, Pages 245-258
Life Sciences

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Thermodynamic analysis of the drug-receptor interaction

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Abstract

Thermodynamic analysis of pharmacologic data potentially offers an insight into the molecular events underlying drug-receptor interactions not obtainable by other techniques. Embodied in thermodynamics are the laws governing the interconvertibility of heat and work and, hence, it is a particularly apt framework for the analysis of the transduction of information from ligand to biological tissue during the initiation of a drug effect. Implicit in thermodynamic analysis of pharmacologic data is quantitative measurement of the driving forces involved in the drug-receptor interaction (in place of less precise terms such as “affinity”). In addition, the cautious interpretation of thermodynamic analysis can give clues to the underlying mechanisms of the drug-receptor interaction that is beyond the resolving power of other parameters, such as the dissociation constant. The present review is an attempt to identify repsresentative reports that have overtly analyzed pharmacologic data with thermodynamic analysis, to summarize the findings within and across studies (particularly regarding enthapy - versus entropy-driven binding of agonists and antagonists), to point out and address some apparent inconsistencies that can arise, and to consider the application of thermodynamic analysis to data obtained using isolated tissue preparations.

References (56)

  • T.J. Franklin

    Biochem. Pharmacol.

    (1980)
  • G.A. Weiland et al.

    Life Sci.

    (1981)
  • E.P. Duarte et al.

    Eur. J. Pharmacol.

    (1988)
  • A. Maelicke et al.

    J. Biol. Chem,

    (1977)
  • J-P. Gies et al.

    Biochim. Biophys. Acta

    (1986)
  • G. Le Fur et al.

    Life Sci.

    (1983)
  • P. Nicolas et al.

    Arch. Biochem. Biophys.

    (1982)
  • R. Hitzemann et al.

    Eur. J. Pharmacol.

    (1985)
  • P.A. Borea et al.

    Eur. J. Pharmacol.

    (1988)
  • M.E.A. Reith et al.

    Biochem. Pharmacol.

    (1984)
  • B.P. Schaumburg et al.

    Biochim. Biophys. Acta

    (1968)
  • M. Koblinsky et al.

    J. Biol. Chem.

    (1972)
  • T.T. Andersen et al.

    Mol. Cell. Endocrinol.

    (1983)
  • C.Y. Liu et al.

    J. Biol. Chem.

    (1980)
  • R.M. Gilli et al.

    Biochim. Biophys. Acta

    (1988)
  • S. Seelig et al.

    J. Biol. Chem.

    (1982)
  • A.R. Saltiel et al.

    Mol. Cell. Endocrinol.

    (1982)
  • M. Waelbroeck et al.

    J. Biol. Chem.

    (1979)
  • B. Testa et al.

    Biochem. Pharmacol.

    (1987)
  • S.J. Ward et al.

    Eur. J. Pharmacol.

    (1982)
  • L. Miller et al.

    Eur. J. Pharmacol.

    (1983)
  • A.L. Lehninger

    Biochemistry

  • INTERUNION COMMISSION ON BIOTHERMODYNAMICS

    Quart. Rev. Biophys.

    (1976)
  • T.P. Kenakin

    Pharmacol. Rev.

    (1984)
  • T.P. Kenakin

    Pharmacologic Analysis of Drug-Receptor Interaction

    (1987)
  • R.J. Tallarida et al.

    Principles in General Pharmacology

    (1988)
  • G.A. Weiland et al.

    Nature (London)

    (1979)
  • A. Gero

    Arch. int. Pharmacodyn.

    (1973)

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