The Hill equation and the origin of quantitative pharmacology

Archive for History of Exact Sciences

Volumn 66, Issue 4, 2012, Pages 427-438

  Gesztelyi, Rudolf ^a   Zsuga, Judit ^b   Kemeny Beke, Adam ^b   Varga, Balazs ^a   Juhasz, Bela ^a   Tosaki, Arpad ^a  

^a UNIVERSITY OF DEBRECEN   (Hungary)

^b UNIVERSITY OF DEBRECEN   (Hungary)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 84863308963     PISSN: 00039519     EISSN: 14320657     Source Type: Journal    
DOI: 10.1007/s00407-012-0098-5     Document Type: Review

References (33)

1. Black J. W., Leff P. (1983) Operational models of pharmacological agonism. Proceedings of the Royal Society B: Biological Sciences 220: 141-162.
2. Clark A. J. (1926) The antagonism of acetylcholine by atropine. Journal of Physiology (London) 61: 547-556.
3. Colquhoun D. (1998) Binding, gating, affinity and efficacy: The interpretation of structure-activity relationships for agonists and of the effects of mutating receptors. British Journal of Pharmacology 125: 924-947.
4. Colquhoun D. (2006) The quantitative analysis of drug-receptor interactions: A short history. Trends in Pharmacological Sciences 27: 149-157.
5. Danhof M., de Jongh J., De Lange E. C., Della Pasqua O., Ploeger B. A., Voskuyl R. A. (2007) Mechanism-based pharmacokinetic-pharmacodynamic modeling: Biophase distribution, receptor theory, and dynamical systems analysis. Annual Review of Pharmacology and Toxicology 47: 357-400.
6. Del Castillo J., Katz B. (1957) Interaction at end-plate receptors between different choline derivatives. Proceedings of the Royal Society B: Biological Sciences 146: 369-381.
7. Furchgott R. F., Bursztyn P. (1967) Comparison of dissociation constants and of relative efficacies of selected agonists acting on parasympathetic receptors. Annals of the New York Academy of Sciences 144: 882-899.
8. Giraldo J., Vivas N. M., Vila E., Badia A. (2002) Assessing the (a)symmetry of concentration-effect curves: Empirical versus mechanistic models. Pharmacol Ther 95: 21-45.
9. Goutelle S., Maurin M., Rougier F., Barbaut X., Bourguignon L., Ducher M., Maire P. (2008) The Hill equation: A review of its capabilities in pharmacological modelling. Fundamental and Clinical Pharmacology 22: 633-648.
10. Hill A. V. (1909) The mode of action of nicotine and curari, determined by the form of the contraction curve and the method of temperature coefficients. Journal of Physiology (London) 39: 361-373.
11. A. V. Hill. 1910. The possible effects of the aggregation of the molecules of haemoglobin on its dissociation curves. Journal of Physiology (London) 40: Proceedings iv-vii.
12. Keller F., Giehl M., Czock D., Zellner D. (2002) PK-PD curve-fitting problems with the Hill equation? Try one of the 1-exp functions derived from Hodgkin, Douglas or Gompertz. International Journal of Clinical Pharmacology and Therapeutics 40: 23-29.
13. Kenakin T. (2006) Data-driven analysis in drug discovery. Journal of Receptors and Signal Transduction Research 26: 299-327.
14. Kenakin T. (2004) Principles: Receptor theory in pharmacology. Trends in Pharmacological Sciences 25: 186-192.
15. Kenakin T. (2009) Quantifying biological activity in chemical terms: A pharmacology primer to describe drug effect. ACS Chemical Biology 4: 249-260.
16. Langmuir I. (1918) The adsorption of gases on plane surfaces of glass, mica and platinum. Journal of the American Chemical Society 40: 1361.
17. Maehle A. H. (2004) Receptive substances": John Newport Langley (1852-1925) and his path to a receptor theory of drug action. Medical History 48: 153-174.
18. Maehle A. H. (2009) A binding question: The evolution of the receptor concept. Endeavour 33: 135-140.
19. Mager D. E., Wyska E., Jusko W. J. (2003) Diversity of mechanism-based pharmacodynamic models. Drug Metabolism and Disposition 31: 510-518.
20. Michaelis L., Menten M. L. (1913) Die Kinetik der Intertinwerkung. Biochemische Zeitschrift 49: 333-369.
21. Motulsky, H. J., and A. Christopoulos. 2003. Fitting models to biological data using linear and nonlinear regression. A practical guide to curve fitting. Oxford: Oxford Press (Corrected online version: http://www. graphpad. com/manuals/Prism4/RegressionBook. pdf).
22. Neubig R. R., Spedding M., Kenakin T., Christopoulos A. (2003) International union of pharmacology committee on receptor nomenclature and drug classification. XXXVIII. update on terms and symbols in quantitative pharmacology. Pharmacological Reviews 55: 597-606.
23. Pelner L. (1972) Corpora non agunt nisi fixata. Maxim behind all of Ehrlich's great discoveries. New York State Journal of Medicine 72: 620-624.
24. Rang, H. P. 2006. The receptor concept: Pharmacology's big idea. British Journal of Pharmacology 147: S9-16.
25. Richards F. J. (1959) A flexible growth function for empirical use. Journal of Experimental Botany 10: 290-300.
26. Ruffolo R. R. Jr. (1982) Review important concepts of receptor theory. Journal of Autonomic Pharmacology 2: 277-295.
27. Scheindlin S. (2001) A brief history of pharmacology. Modern Drug Discovery 4: 87-88.
28. Stephenson R. P. (1956) A modification of receptor theory. British Journal of Pharmacology 11: 379-393.
29. van der Graaf P. H., Danhof M. (1997) Analysis of drug-receptor interactions in vivo: A new approach in pharmacokinetic-pharmacodynamic modelling. International Journal of Clinical Pharmacology and Therapeutics 35: 442-446.
30. van der Graaf P. H., Schoemaker R. C. (1999) Analysis of asymmetry of agonist concentration-effect curves. Journal of Pharmacological and Toxicological Methods 41: 107-115.
31. van der Graaf P. H., Stam W. B. (1999) Analysis of receptor inactivation experiments with the operational model of agonism yields correlated estimates of agonist affinity and efficacy. Journal of Pharmacological and Toxicological Methods 41: 117-125.
32. Weiss J. N. (1997) The Hill equation revisited: Uses and misuses. FASEB Journal 11: 835-841.
33. Zimmer, H. G. (1996) Carl Ludwig: the man, his time, his influence. Pflugers Archiv 432: R9-22.