Skip to main content
SpringerLink
Log in

Competitive and Noncompetitive Antagonism

  • Chapter
Histamine II and Anti-Histaminics

  • 397 Accesses

Abstract

For many purposes it is useful to classify drugs in pharmacologic families. A family includes all drugs which are able to interact with the receptors of a certain receptor-effector system, and which, by doing so, can cause the same kind of effect (Van Den Brink, 1966, 1969a, 1977).

Some observations based on the affinity and in trinsic activity values of a series of 75 compounds with respect to histaminic, cholonergic and metactoid receptors.

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Log in via an institution
Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 84.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 109.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  • Ariëns, E.J.: Receptor theory and structure-action relationships. In: Advances in drug research, Vol. 3, pp.235–285. London-New York: Academic Press 1966.

    Google Scholar 

  • Ariëns, E. J., de Groot, W.M.: Affinity and intrinsic activity in the theory of competitive inhibition, Part III. Homologous decamethonium-derivatives and succinyl-choline-esters. Arch. int. Pharmacodyn. 99, 193–205 (1954).

    PubMed  Google Scholar 

  • Ariëns, E.J., Simonis, A.M.: Autonomic drugs and their receptors. Arch. int. Pharmacodyn. 127, 479–496(1960).

    PubMed  Google Scholar 

  • Ariëns, E.J., Simonis, A.M.: A molecular basis for drug action. J. Pharm. Pharmacol. 16, 137 – 157(1964).

    Article  Google Scholar 

  • Ariëns, E. J., Simonis, A.M.: Cholinergic and anticholinergic drugs, do they act on common receptors? Ann. N.Y. Acad. Sci. 144, 842–868 (1967).

    Article  PubMed  Google Scholar 

  • Ariëns, E.J., Simonis, A.M.: Chemical structure and biological activity. Some general principles. In: Physico-chemical aspects of drug action; Proceedings of the third international pharmacological meeting, Vol.7, pp.271–281. Oxford-London-Edinburgh-New York-Toronto-Sydney-Paris-Braunschweig: Pergamon Press 1968.

    Google Scholar 

  • Ariëns, E.J., Simonis, A.M., van Rossum, J.M.: Drug-receptor interaction: Interaction of one or more drugs with one receptor system. II.A.5.4. Specificity of mimetics and lytics. In: Molecular pharmacology, Vol. 1, pp.225–232. New York-London: Academic Press 1964.

    Google Scholar 

  • Ariëns, E.J., Simonis, A.M., van Rossum, J.M.: Drug-receptor interaction: interaction of one or more drugs with different receptor systems. II.B.4. Functional interaction. In: Molecular pharmacology, Vol. 1, pp. 329–340. New York-London: Academic Press 1964.

    Google Scholar 

  • Bondi, A.: Van der Waals volumes and radii. J. phys. Chem. 68, 441–451 (1964).

    Article  CAS  Google Scholar 

  • Ellenbroek, B. W. J.: Stereoisomerism and biological activity. An investigation into acetylcholine and atropine analogs (in Dutch). Ph.D. Thesis, University of Nijmegen, 1964.

    Google Scholar 

  • Ellenbroek, B.W.J., Nivard, R.J.F., van Rossum, J.M., Ariëns, E.J.: Absolute configuration and parasympathetic action: pharmacodynamics of enantiomorphic and diastereoisomeric esters of β-methylcholine. J. Pharm. Pharmacol. 17, 393–404 (1965).

    Article  PubMed  CAS  Google Scholar 

  • Gould, R.F. (Ed.): Biological correlations—the Hansch approach. Advances in chemistry series, 114. Washington D.C.: Amer. chem. Soc. 1972.

    Google Scholar 

  • Hammett, L.P.: Physical organic chemistry, pp. 184–199. New York: McGraw-Hill 1940.

    Google Scholar 

  • Hansch, C.: Quantitative approaches to pharmacological structure-activity relationship. In: Structure-activity relationships. International encyclopedia of pharmacology and therapeutics, Section 5, Vol.1, pp.75–165. Oxford-New York-Toronto-Sydney-Braunschweig: Pergamon Press 1973.

    Google Scholar 

  • Hansch, C., Clayton, J.M.: Lipophilic character and biological activity of drugs, II. The parabolic case. J. pharm. Sci. 62, 1–21 (1973).

    Article  PubMed  CAS  Google Scholar 

  • Hansch, C., Dunn, W.J. III: Linear relationships between lipophilic character and biological activity of drugs. J. pharm. Sci. 61, 1–19 (1972).

    Article  PubMed  CAS  Google Scholar 

  • Hansch, C., Leo, A., Unger, S.H., Kim, K.H., Nikaitani, D., Lien, E.J.: “Aromatic” substituent constants for structure-activity correlations. J. med. Chem. 16, 1207–1216 (1973).

    Article  PubMed  CAS  Google Scholar 

  • Hansch, C., Lien, E.J.: An analysis of the structure-activity relationship in the adrenergic blocking activity of the β-haloalkylamines. Biochem. Pharmacol. 17, 709–720 (1968).

    Article  PubMed  CAS  Google Scholar 

  • Kutter, E., Hansch, C.: Steric parameters in drug design. Monoamine oxidase inhibitors and antihistamines. J. med. Chem. 12, 647–652 (1969).

    Article  PubMed  CAS  Google Scholar 

  • Lehmann, P.A., Rodrigues de Miranda, J.F., Ariëns, E.J.: Stereoselectivity and affinity in molecular pharmacology. In: Progress in drug research, Vol.20. Basel-Stuttgart: Birkhäuser Verlag 1976.

    Google Scholar 

  • Leo, A., Hansch, C., Elkins, D.: Partition coefficients and their uses. Chem. Rev. 71, 525–616 (1971).

    Article  CAS  Google Scholar 

  • Lien, E.J., Rodrigues de Miranda, J.F., Ariëns, E.J.: Quantitative structure-activity correlation of optical isomers: a molecular basis for Pfeiffer’s rule. Mol. Pharmacol. 12, 598–604 (1976).

    PubMed  CAS  Google Scholar 

  • Lien, E. J., Tong, G.L.: Structure-activity correlations of anticancer agents: diaminopyrimidines, N-acyltriamines, bis-(l-aziridinyl)-pnosphinyl carbamates, and aromatic nitrogen mustards. Cancer Chemother. Rep. Part 1, 57, 251–261 (1973).

    CAS  Google Scholar 

  • Offermeier, J., Van den Brink, F.G.: The antagonism between cholinomimetic agonists and ß-adrenoceptor stimulants. The differentiation between functional and metaffinoid antagonism. Europ. J. Pharmacol. 27, 206–213 (1974).

    Article  CAS  Google Scholar 

  • Pfeiffer, C. C.: Optical isomerism and pharmacological action, a generalization. Science 124, 29–31(1956).

    Article  PubMed  CAS  Google Scholar 

  • Rekker, R.F.: New developments in the design of bioactive compounds. In: The design of bioactive compounds. Symposium organized by the Section of Medicinal Chemistry of the Royal Netherlands Chemical Society, Maastricht 1970, pp.32–51.

    Google Scholar 

  • Simonis, A.M., Ariëns, E.J.: Eine Molekulargrundlage für die Wirkung von Pharmaka. II. Verschiedene Typen von Antagonisten. Arzneimittel-Forsch. 16, 1393–1403 (1966).

    CAS  Google Scholar 

  • Simonis, A.M., Ariëns, E. J.: Kritische und nicht-kritische Struktur-Elemente in Pharmaka. Nau-nyn-Schmiedebergs Arch. Pharmak. exp. Path. 257, 65–66 (1967).

    CAS  Google Scholar 

  • Stubbins, J.F., Hudgins, P.M., Andrako, J., Beebe, A.J.: Anticholinergic agents based on Ariëns’ dual receptor site theory. J. pharm. Sci. 57, 534–536 (1968).

    Article  PubMed  CAS  Google Scholar 

  • van den Brink, F.G.: Eine Molekulargrundlage für die Wirkung von Pharmaka. Arzneimittel-Forsch. 16, 1403–1412 (1966).

    Google Scholar 

  • van den Brink, F.G.: Influence of combined cooling and aging on the response of the guinea-pig ileum to histamine. Europ. J. Pharmacol. 2, 224–228 (1967).

    Article  Google Scholar 

  • van den Brink, F.G.: Classification of drugs in families. In: Histamine and antihistamines, pp.28–29. Nijmegen: Gebr. Janssen N.V. 1969a.

    Google Scholar 

  • van den Brink, F.G.: Discussion of the presuppositions in the agonistic model. In: Histamine and antihistamines, pp.43–45. Nijmegen: Gebr. Janssen N.V. 1969b.

    Google Scholar 

  • van den Brink, F.G.: The making of concentration-effect curves with the cumulative concentration technique. Determination of the α E-, pD2-, α S-, pK SA -, pA2-, and pD2’-value. The statistical handling of these values. In: Histamine and antihistamines, pp.66–91. Nijmegen: Gebr. Janssen N.V. 1969 c.

    Google Scholar 

  • van den Brink, F.G.: Influence of some molecular modifications on the affinity values. In: Histamine and antihistamines, pp. 119–125. Nijmegen: Gebr. Janssen N.V. 1969d.

    Google Scholar 

  • van den Brink, F.G.: The model of functional interaction. I. Development and first check of a new model of functional synergism and antagonism. Europ. J. Pharmacol. 22, 270–278 (1973 a).

    Article  Google Scholar 

  • van den Brink, F.G.: The model of functional interaction. II. Experimental verification of a new model: the antagonism of β-adrenoceptor stimulants and other agonists. Europ. J. Pharmacol. 22, 279–286 (1973b).

    Article  Google Scholar 

  • van den Brink, F.G.: General theory of drug-receptor interactions. Drug-receptor interaction models. Calculation of drug parameters. In: Kinetics of drug action. Handbook of experimental pharmacology, Vol. 47, pp. 169–254. Berlin-Heidelberg-New York: Springer 1977.

    Google Scholar 

  • van Rossum, J.M.: Cumulative dose-response curves. II. Technique for the making of dose-response curves in isolated organs and the evaluation of drug parameters. Arch. int. Pharma -codyn. 143, 299–330(1963).

    Google Scholar 

  • van Rossum J.M.: Limitations of molecular pharmacology. In: Advances in drug research, Vol. 3, pp. 189–234. London-New York: Academic Press 1966 a.

    Google Scholar 

  • van Rossum J.M.: Die Pharmakon-Rezeptor-Theorie als Grundlage der Wirkung von Arzneimitteln; Möglichkeiten und Beschränkungen. Arzneimittel-Forsch. 16, 1412–1426 (1966 b).

    Google Scholar 

  • van Rossum J.M., van den Brink, F.G.: Cumulative dose-response curves. I. Introduction to the technique. Arch. int. Pharmacodyn. 143, 240–247 (1963).

    PubMed  Google Scholar 

  • Verloop, A., Hoogenstraaten, W., Tipker J.: Development and application of new steric substituent parameters in drug design. In: Drug design, Vol. 7, pp. 165–207. New York-San Francisco-London: Academic Press 1876.

    Google Scholar 

Download references

Authors
  1. Frans G. Van Den Brink
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Eric J. Lien
    View author publications

    You can also search for this author in PubMed Google Scholar

Editor information

Editors and Affiliations

  1. Department of Pharmacology, Faculty of Medicine of Ribeirão Preto, University of São Paulo, 14.100, Ribeirão Preto, S.P., Brazil

    Mauricio Rocha e Silva

Rights and permissions

Reprints and permissions

Copyright information

© 1978 Springer-Verlag Berlin Heidelberg

About this chapter

Cite this chapter

Van Den Brink, F.G., Lien, E.J. (1978). Competitive and Noncompetitive Antagonism. In: Rocha e Silva, M. (eds) Histamine II and Anti-Histaminics. Handbuch der experimentellen Pharmakologie / Handbook of Experimental Pharmacology, vol 18 / 2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-66445-8_8

Download citation

  • DOI: https://doi.org/10.1007/978-3-642-66445-8_8

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-642-66447-2

  • Online ISBN: 978-3-642-66445-8

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics

Search

Navigation