Drug Receptors in the Lung Especially Histamine Receptors

  • Noemi Eiser
Part of the Ettore Majorana International Science Series book series (EMISS, volume 14)


Drugs produce their actions by combining with receptors. A specific response is produced when an agonist binds to a receptor. In contrast, when an antagonist combines with that receptor, it produces either no response or a decrease in the expected response of the agonist. Pre-treatment with the antagonist will shift the dose-response curve of the agonist to the right. This is known as competitive inhibition. Thus, while agonists have affinity and efficacy, antagonists have affinity only. In many cases the precise nature and location of the receptor is unknown but the properties of established agonists and antagonists have been utilized to investigate receptors both in vitro and in vivo. In this paper I shall concentrate on the findings of recent research into histamine receptors in the lung and then consider, briefly, the evidence concerning cholinergic, adrenergic and noncholinergic, nonadrenergic receptors.


Histamine Release Human Airway Histamine Receptor Asthmatic Subject Disodium Cromoglycate 
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  1. Ash, A. S. F. and Schild, H. O.(1966). Receptors mediating some actions of histamine. Br. J. Pharmacol., 27, 427–439.Google Scholar
  2. Barnes, P. J., Karliner, J. S. and Dollery, C. T. (1980). Human lung adrenoreceptors studied by radioligand bind ing. Clin. Sci., 58, 457–461.Google Scholar
  3. Black, J. W., Duncan, W. A. M., Durant, G. J., Ganellin, C. R. and Parsons, M. E. (1972). Definition and antagonism of histamine H2-receptors. Nature, London, 236, 385–390.ADSCrossRefGoogle Scholar
  4. Boe, J. and Simonsson, B. G. (1980). Histamine H1- and H2-receptors in human pulmonary arteries. Bull. Europ. Physiopathol. Resp. 16, 108–109p.Google Scholar
  5. Booij-Noord, H. O., Orie, N. G. M., Berg, W. and de Vries, K. (1970). Protection tests on bronchial allergen challenge with disodium cromoglycate and thiazinamium. J. Allergy, 46, 1–11.CrossRefGoogle Scholar
  6. Casterline, C. L. and Evans, R. (1977). Further studies on the mechanism of human histamine-induced asthma. J. Allergy Clin. Immunol., 59, 420–424.CrossRefGoogle Scholar
  7. Chakrin, L. W. and Krell, R. D. (1980). Histamine receptors in the respiratory system: a review of current evidence. H2-Antagonists in Peptic Ulcer Disease and Progress in Histamine Research. (Ed. Torsoli, A., Lucchelli, P. E., Brimblecombe, R.E.W.: Excerpta Med ica). 338–346.Google Scholar
  8. Chand, N. (1980). Distribution and classification of airway histamine receptors: The physiological significance of histamine H2-receptors. Advances in Pharmacology and Chemotherapy. 17, 103–131.CrossRefGoogle Scholar
  9. Church, M. K. and Gradidge, C. F. (1979). Histamine H1-antagonists and histamine release from human lung in vitro. Br. J. Pharmacol., 66, 68p.Google Scholar
  10. Curry, J. J. (1946). The action of histamine on the respiratory tract in normal and asthmatic patients. J. Clin. Invest. 25, 785–799.CrossRefGoogle Scholar
  11. Dunlop, L. S. and Smith, A. P. (1977). The effect of histamine antagonists on antigen-induced contractions of sensitised human bronchus in vitro. Br. J. Pharmacol., 59, 475p.Google Scholar
  12. Eiser, N. M., Mills, J., McRae, K. D., Snashall, P. D. and Guz, A. (1980). Histamine receptors in normal human bronchi. Clin. Sci., 58, 537–544.Google Scholar
  13. Eiser, N. M., Mills, J., Snashall, P. D. and Guz, A. (1981). The role of histamine receptors in asthma. Clin. Sci., 60, 363–370.Google Scholar
  14. Gaddie, J., Legge, J. S., Petrie, G., and Palmer, K. N. V. (1972). The effect of an alpha-adrenergic receptor blocking drug on histamine sensitivity in bronchial asthma. Br. J. Dis. Chest., 66, 141–146.CrossRefGoogle Scholar
  15. Hartley, J. P. R. and Nogrady, S. G. (1980). Effect of an inhaled antihistamine on exercise-induced asthma. Thorax, 35, 675–680.CrossRefGoogle Scholar
  16. Herxheimer, H. (1949). Antihistamines in bronchial asthma. Brit. Med. J., ii: 901–905.CrossRefGoogle Scholar
  17. Kaliner, M. (1978). Human lung tissue and anaphylaxis. The effect of histamine on the immunological release of mediators. Am. Rev. Resp. Dis, 118, 1015–1023.Google Scholar
  18. Leopold, J. D., Hartley, J. P. R. and Smith, A. P.(1979). Effects of oral H1- and H2-receptor antagonists in asthma. Br. J. Clin. Pharmacol., 8, 249–251.CrossRefGoogle Scholar
  19. Lichtenstein, L. M. and Gillespie, E. (1973). Inhibition of histamine release by histamine controlled by H2-receptor. Nature, 244, 287–288.ADSCrossRefGoogle Scholar
  20. Lowhagen, O. and Lindholm, N. B.(1979f). Clinical evaluation of some anti-allergic drugs by the use of antigen challenge test. The Mast Cell: its role in Health and Disease. (Pitman Medical Publishers) (Ed: Pepys, J. and Edwards, A. M.) 332–336.Google Scholar
  21. Maconochie, J. G., Woodings, E. P. and Richards, D. A. (1979). Effects of H1- and H2-receptor blocking agents on histamine-ind uced bronchoconstriction in non-asthmatic subjects. Br. J. Clin. Pharmacol., 7, 231–236.CrossRefGoogle Scholar
  22. Muittari, A. (1968). The value of the Metacholine test as a diagnostic method in bronchospastic disorders. Ann. Med. Int. Fenn, 57, 197–203.Google Scholar
  23. Nadel, J. A. (1980). Autonomic regulation of airway submucosal gland secretion. In: Airway Reactivity: mechanisms and clinical relevance. Ed: Hargreave, F. E. (Astra Pharmaceuticals, Canada Ltd.), 54–58.Google Scholar
  24. Nogrady, S. G. and Bevan, C. (1978). Inhaled antihistamines, bronchodilatation and effects on histamine and methacholine-induced bronchoconstriction. Thorax, 33, 700–704.CrossRefGoogle Scholar
  25. Nogrady, S. G. and Bevan, C. (1981). H2-receptor blockade and bronchial hyper-reactivity to histamine in asthma. Thorax, 36, 268–271.CrossRefGoogle Scholar
  26. Patel, K. R. and Kerr, J. W. (1975). Effect of alpha receptor blocking drug, thymoxamine, on allergen induced bronchoconstriction in extrinsic asthma. Clin. Allergy, 5, 311–316.Google Scholar
  27. Popa, V. T. (1977). Bronchodilating activity of an H1-blocker, Chlorpheniramine. J. Allergy Clin. Immunol, 59, 54–63.CrossRefGoogle Scholar
  28. Popa, V. T. (1980). Effect of an H1-blocker, Chlorpheniramine, on inhalation tests with histamine and allergen in allergic asthma. Chest, 78, 442–451.CrossRefGoogle Scholar
  29. Richardson, J. and Beland, J. (1976). Noadrenergic inhibitory nervous human airways. J. Appl. Physiol., 41, 764–771.Google Scholar
  30. Richardson, J. (1979). Nerve supply to the lungs. Am. Rev. Resp. Dis., 119, 785–802.Google Scholar
  31. Shelhamer, J. H., Marom, Z. and Kaliner, M. (1980). Immunologic and neuropharmacologic stimulation of mucous glycoprotein release from human airways in vitro. J. Clin. Invest., 66, 1400–1408.CrossRefGoogle Scholar
  32. Snashall, P. D., Boother, F. A. and Sterling, G. M. (1978). The effect of adrenoreceptor stimulation on the airways of normal and asthmatic man. Clin. Sci., 54, 283–289.Google Scholar
  33. Thomson, N. C. and Kerr, J. W. (1980). Effect of inhaled H1and H2-receptor antagonists in normal and asthmatic subjects. Thorax, 35, 428–434.CrossRefGoogle Scholar
  34. Woenne, R., Kattan, M.and Levison, H. (1979). Sodium cromoglycate-induced changes in the dose-response curve of inhaled methacholine and histamine in asthmatic children. Am. Rev. Respir. Dis., 119, 927–932.Google Scholar
  35. Zielinski, J. and Chodosowski, E. (1977). Exercise-induced bronchoconstriction in patients with bronchial asthma, its prevention with an antihistaminic agent. Respiration, 34, 31–35.CrossRefGoogle Scholar

Copyright information

© Springer Science+Business Media New York 1984

Authors and Affiliations

  • Noemi Eiser
    • 1
  1. 1.Department of Thoracic MedicineNew Cross HospitalLondonUK

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