The quantification and differentiation of the drug receptor theory, c. 1910-1960

Annals of Science

Volumn 62, Issue 4, 2005, Pages 479-500

  Maehle, Andreas Holger ^a  

^a DURHAM UNIVERSITY   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

DRUG PRODUCTS PLANTS; MOLECULAR BIOLOGY; RESEARCH AND DEVELOPMENT MANAGEMENT;

MOLECULAR PHARMACOLOGY; PHARMACEUTICAL RESEARCH; RECEPTOR THEORY;

DRUG INFUSION;

DRUG RECEPTOR;

ANIMAL; DRUG INTERACTION; HISTORY; HUMAN; MEDICAL RESEARCH; PHARMACOLOGY; REVIEW;

ANIMALS; BIOMEDICAL RESEARCH; DRUG INTERACTIONS; HISTORY, 20TH CENTURY; HUMANS; PHARMACOLOGY; RECEPTORS, DRUG;

EID: 31444435283     PISSN: 00033790     EISSN: None     Source Type: Journal    
DOI: 10.1080/00033790412331312666     Document Type: Article

References (145)

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4. ; Cay-Rüdiger Prüll, Andreas-Holger Maehle and Robert F. Halliwell, 'Drugs and Cells - Pioneering the Concept of Receptors', Pharmacy in History, 45 (2003), 18-30;
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8. ; Gerald O. Carrier, 'Evolution of the Dual Adrenergic Receptor Concept: Key to Past Mysteries and Modern Therapy', in Discoveries in Pharmacology (note 1), III, 203-21;
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10. A brief, summarising account is given in Joseph D. Robinson, Mechanisms of Synaptic Transmission: Bridging the Gaps (1890-1990) (Oxford, Oxford University Press, 2001), 143-52;
11. Clark's contribution to receptor theory has been highlighted in Parascandola (note 1), 148 53;
12. J. Parascandola, 'A. J. Clark: Quantitative Pharmacology and the Receptor Theory', Trends in Pharmacological Sciences, 3 (1982), 421-23;
13. and Prüll, Maehle and Halliwell (note 1), 26-27.
14. Early receptor theories are considered in some pharmacological textbooks, e.g. Philip Michael Dean, Molecular Foundations of Drug-Receptor Interaction (Cambridge, Cambridge University Press, 1987), 1 -34;
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16. John Newport Langley, 'On the Reaction of Cells and of Nerve-Endings to Certain Poisons, Chiefly as Regards the Reaction of Striated Muscle to Nicotine and to Curari', Journal of Physiology, 33 (1905), 374-413.
17. See also J. N. Langley, 'Croonian Lecture, 1906. - On Nerve Endings and on Special Excitable Substances in Cells', Proceedings of the Royal Society of London, series B, 78 (1906), 170-94.
18. Paul Ehrlich, 'Experimental Researches on Specific Therapy' (Harben Lectures, 1907), in The Collected Papers of Paul Ehrlich, 3 vols, edited by Fred Himmelweit (London, Pergamon Press, 1956-60), III, 10634
19. ; John Parascandola, 'The Theoretical Basis of Paul Ehrlich's Chemotherapy', Journal of the History of Medicine and Allied Sciences, 36 (1981), 1943;
20. Silverstein (note 1), 129-32; Prüll (note 1).
21. Alfred Joseph Clark, The Mode of Action of Drugs on Cells (London, Edward Arnold & Co., 1933), 1.
22. See The Road to Medical Statistics, edited by Eileen Magnello and Anne Hardy (Amsterdam, Rodopi, 2002), especially the chapter by J. Rosser Matthews, 'Almroth Wright, Vaccine Therapy and British Biometrics: Disciplinary Expertise versus Statistical Objectivity', 125-47.
23. th centuries, J. R. Matthews, Quantification and the Quest for Medical Certainty (Princeton, N.J., Princeton University Press, 1995),
24. and Harry M. Marks, The Progress of Experiment: Science and Therapeutic Reform in the United States, 1900 -1990 (Cambridge, Cambridge University Press, 1997).
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27. Theodore M. Porter, Trust in Numbers: The Pursuit of Objectivity in Science and Public Life (Princeton, N.J., Princeton University Press, 1995), 29-32
28. ; Silverstein (note 1), 41 54.
29. Archibald Vivian Hill, '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, 39 (1909), 36173 (361).
30. On the conflict between chemical and physical theories of drug action see John Parascandola, 'The Controversy over Structure-Activity Relationships in the Early Twentieth Century', Pharmacy in History, 16(1974), no. 2, 54-63.
31. Hill (note 9), 372f
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33. See also W. Straub, Die Bedeutung der Zellmembran für die Wirkung chemischer Stoffe auf den Organismus, Gesellschaft Deutscher Naturforscher und Ärzte, Verhandlungen 1912, Sonderabdruck (Leipzig, August Pries, 1912).
34. On Straub and the Schmiedeberg-School see Günther Stille, Der Weg der Arznei von der Materia Medica zur Pharmakologie: Der Weg yon Arzneimittelforschung und Arzneitherapie (Karlsruhe, G. Braun Fachverlage, 1994), 222-30, 247-49.
35. See also Marcel H. Bickel, Die Entwicklung zur experimentellen Pharmakologie 1790-1850. Wegbereiter von Rudolf Buchheim (Basel, Schwabe, 2000), 115-18.
36. Cf. Clark (note 6), 189-202; Prüll, Maehle and Halliwell (note 1), 24-26.
37. Bernard Katz, 'Archibald Vivian Hill', Biographical Memoirs of Fellows of the Royal Society, 24 (1978), 71-149(77).
38. A. V. Hill, 'Lecture I: The Physical Environment of the Living Cell', in Lectures on Certain Aspects of Biochemistry, by H. H. Dale, J. C. Drummond, L. J. Henderson, A. V. Hill (London, University of London Press, 1926), 253-80 (279).
39. Joseph Barcroft and A.V. Hill, 'The Nature of Oxyhaemoglobin, with a Note on its Molecular Weight', Journal of Physiology, 39 (1910), 411-28.
40. A. V. Hill, 'The Possible Effects of the Aggregation of the Molecules of Haemoglobin on its Dissociation Curves', Journal of Physiology, 40 (1910), iv-vii;
41. Katz (note 14), 78.
42. A. V. Hill, 'The Mechanism of Muscular Contraction', in Nobel Lectures including Presentation Speeches and Laureates' Biographies. Physiology or Medicine 1922-1941, edited by the Nobel Foundation (Amsterdam, Elsevier, 1965), 10-23.
43. Hill (note 15), 276-78.
44. Friedrich Cramer, 'Emil Fischers Schlüssel-Schloβ-Hypothese der Enzymwirkung - 100 Jahre danach', in Räume des Wissens: Repräsentation, Codierung, Spur, edited by Hans-Jörg Rheinberger, Bettina Wahrig-Schmidt and Michael Hagner (Berlin, Akademie Verlag, 1997), 191-212
45. ; Peter J. Ramberg, Chemical Structure, Spatial Arrangement: The Early History of Stereochemistry, 1874-1914 (Aldershot, Ashgate, 2003), 271f.
46. For Clark's biographical details see David Hazell Clark, Alfred Joseph Clark 1885-1941. A Memoir (Glastonbury, C. & J. Clark Ltd. Archives, 1985).
47. Useful is also E. B. Verney and J. Barcroft, 'Alfred Joseph Clark 1885-1941', Obituary Notices of Fellows of the Royal Society, 3 (1939-1941), 969-84.
48. A. J. Clark, 'Walter Ernest Dixon - 1871-1931', Proceedings of the Royal Society of London, series B, 110 (1932), xxix-xxxi.
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50. Arthur Robertson Cushny, 'The Action of Atropine, Pilocarpine and Physostigmine', Journal of Physiology. 41 (1910), 233-45;
51. John Parascandola, 'Arthur Cushny, Optical Isomerism, and the Mechanism of Drug Action', Journal of the History of Biology, 8 (1975), 145-65.
52. See W. Straub, 'Quantitative Untersuchungen über den Chemismus der Strophanthinwirkung', Biochemische Zeitschrift, 28 (1910), 392-407
53. ; A. J. Clark, 'The Influence of Ions upon the Action of Digitalis', Proceedings of the Royal Society of Medicine, 5 (1912), 181-197;
54. Clark, 'The Mode of Action of Strophanthin upon Cardiac Tissue', Journal of Pharmacology and Experimental Therapeutics, 5 (1913), 215-34.
55. Otto Loewi, 'Über humorale Übertragbarkeit der Herznervenwirkung. I. Mitteilung', Pflügers Archiv für die gesamte Physiologie, 189 (1921), 239-42;
56. Loewi, 'Über humorale Übertragbarkeit der Herznervenwirkung. II. Mitteilung', Pflügers Archiv für die gesamte Physiologie, 193 (1922), 201-13;
57. O. Loewi and E. Navratil, 'Über humorale Übertragbarkeit der Herznervenwirkung. X. Mitteilung. Über das Schicksal des Vagusstoffs', Pflügers Archiv für die gesamte Physiologie, 214 (1926), 678-88 (esp. 687f.)
58. See also Tilli Tansey, 'Sir Henry Dale and Autopharmacology: The Role of Acetylcholine in Neurotransmission', in Essays in the History of the Physiological Sciences, edited by Claude Debru (Amsterdam, Rodopi, 1995), 179-93.
59. A. J. Clark, 'The Reaction between Acetyl Choline and Muscle Cells', Journal of Physiology, 61 (1926), 530-46.
60. Clark (note 27), 534f.
61. Clark (note 27), 539-42, 546.
62. Clark (note 27), 545f.
63. Clark (note 27), 545.
64. The study of 'elective affinities' became a major preoccupation for eighteenth-century chemists. Cf. William H. Brock, The Fontana History of Chemistry (London, Fontana Press, 1992), 76.
65. Balthasar Luchsinger, 'Die Wirkungen von Pilocarpin und Atropin auf die Schweissdrüsen der Katze. Ein Beitrag zur Lehre vom doppelseitigen Antagonismus zweier Gifte', ügers Archiv für Anatomie und Physiologie, 15 (1877), 482-92;
66. J. N. Langley, 'On the Physiology of the Salivary Secretion. Part II. On the Mutual Antagonism of Atropin and Pilocarpin, having especial Reference to their Relations in the Sub-Maxillary Gland of the Cat', Journal of Physiology, 1 (1878), 33969.
67. Michael Joseph Rossbach, 'Neue Studien über den physiologischen Antagonismus der Gifte', Pflügers Archiv für Anatomie und Physiologie, 21 (1879), 1-38.
68. Straub 1907 (note 11), 148.
69. J. N. Langley, 'On the Contraction of Muscle, Chiefly in Relation to the Presence of "Receptive" Substances'. Part IV The Effect of Curari and of Some Other Substances on the Nicotine Response of the Sartorius and Gastrocnemius Muscles of the Frog', Journal of Physiology, 39 (1909/10), 235-95 (292).
70. A. R. Cushny, 'Quantitative Observations on Antagonism', Journal of Pharmacology and Experimental Therapeutics, 6 (1915), 439-50 (447f.)
71. Cushny (note 37), 448f.
72. Cushny (note 37), 447.
73. For Gaddum's biography see Wilhelm Feldberg, 'John Henry Gaddum 1900 1965', Biographical Memoirs of Fellows of the Royal Society, 13 (1967), 57-77.
74. John Henry Gaddum, 'The Action of Adrenalin and Ergotamine on the Uterus of the Rabbit', Journal of Physiology, 61 (1926), 141-50(142).
75. Gaddum (note 41), 149f.
76. Cf. A. J. Clark, 'The Antagonism of Acetyl Choline by Atropine', Journal of Physiology, 61 (1926), 547-56.
77. Clark (note 43), 555.
78. See Clark 1912 (note 25);
79. A. J. Clark, 'The Action of Ions and Lipoids upon the Frog's Heart', Journal of Physiology, 47 (1913), 66-107;
80. I. de Burgh Daly and A. J. Clark, 'The Action of Ions upon the Frog's Heart', Journal of Physiology, 54 (1921), 367-83;
81. A. J. Clark, The Mode of Action of Potassium Ions upon Isolated Organs', Journal of Pharmacology and Experimental Therapeutics, 18 (1922), 423-47.
82. A. J. Clark, The Mode of Action of Potassium Chloride on Muscles', Journal of Pharmacology and Experimental Therapeutics, 29 (1926), 311-24 (esp. 314).
83. Loewi and Navratil (note 26), 688.
84. A. J. Clark, The Reaction between Acetyl Choline and Muscle Cells. Part II', Journal of Physiology, 64 (1927), 123-43 (134).
85. Clark (note 6), 133.
86. A. J. Clark, General Pharmacology ( = Handbuch der Experimentellen Pharmakologie, founded by A. Heffter, Ergänzungswerk, edited by W. Heubner and J. Schüller, vol. 4) (Berlin, Verlag von Julius Springer, 1937).
87. Clark (note 50), 25f.
88. J. H. Gaddum, 'The Quantitative Effects of Antagonistic Drugs', Journal of Physiology, 89 (1937), 7P-9P
89. . Cf. Clark (note 50), 184f.
90. Clark (note 50), 217.
91. Cf. also A. J. Clark and J. Raventos, 'The Antagonism of Acetylcholine and of Quaternary Ammonium Salts', Quarterly Journal of Experimental Physiology, 26 (1937), 375-92 (esp. 391).
92. Clark (note 50), 216.
93. A. J. Clark, 'Discussion on the Chemical and Physical Basis of Pharmacological Action, 12 November, 1936. Opening Address', Proceedings of the Royal Society of London, series B, 121 (1937), 580-84 (584);
94. W. Straub, 'Mode of Action of Stimulating Alkaloids', Proceedings of the Royal Society of London, series B, 121 (1937), 584-87.
95. Hazell Clark (note 21), 44f.
96. See H. O. Schild and F. L. Rose, 'Harry Raymond Ing', Biographical Memoirs of Fellows of the Royal Society, 22 (1976), 239-55.
97. George Barger and Henry Hallett Dale, 'Chemical Structure and Sympathomimetic Action of Amines', Journal of Physiology, 41 (1910), 19-59
98. For the history of chemical neurotransmission see Robinson (note 3)
99. and Jean-Claude Dupont, Histoire de la Neurotransmission (Paris, Presses Universitaires de France, 1999).
100. Sir Henry Dale, 'Modes of Drug Action. A General Discussion. General Introductory Address', Transactions of the Faraday Society, 39 (1943), 319-22 (320).
101. Harry Raymond Ing, 'Chemical Constitution and Pharmacological Action', Transactions of the Faraday Society, 39 (1943), 372-80.
102. On the history of the structure-action problem in pharmacology, which dates back to the 1840s, see William F. Bynum, 'Chemical Structure and Pharmacological Action: A Chapter in the History of 19 Century Molecular Pharmacology', Bulletin of the History of Medicine, 44 (1970), 518-38.
103. Dale (note 59), 321.
104. Ing (note 60), 373, 379.
105. Schild and Rose (note 57), 247.
106. J. H. Gaddum, 'Introductory Address. Part I. Biological Aspects: The Antagonism of Drugs', Transactions of the Faraday Society, 39 (1943), 32332 (323).
107. Clark (note 50), 217.
108. Clark (note 6), 61.
109. Ing (note 60), 372f.
110. Thomas Renton Elliott, 'On the Action of Adrenalin', Journal of Physiology, 31 (1904), xx-xxi;
111. Robinson (note 3), 123f.
112. Henry Hallett Dale, 'Nomenclature of Fibres in the Autonomie System and their Effects', Journal of Physiology, 80 (1933), 10P-11P;
113. Dale, 'Acetylcholine as a Chemical Transmitter of the Effects of Nerve Impulses', Journal of the Mount Sinai Hospital, 4 (1938), 401-29 (410).
114. J. N. Langley, The Autonomie Nervous System. Part I (Cambridge, W. Heifer & Sons, 1921), 44.
115. Robinson (note 3), 70.
116. For a full discussion of Cannon and Rosenblueth's theory of Sympathin E and Sympathin I and its context see Elin L. Wolfe, A. Clifford Barger and Saul Benison, Walter B. Cannon, Science and Society (Cambridge, Mass., Boston Medical Library and Harvard University Press, 2000), 308-32.
117. Raymond P. Ahlquist, 'A Study of the Adrenotropic Receptors', American Journal of Physiology, 153 (1948), 586-600.
118. Robinson (note 3), 70f.
119. See also Peter Gaudenz Waser, 'The Cholinergic Receptor', in Parnham and Bruinvels (note 1), III, 157201 (194f.)
120. Henry Hallett Dale, 'The Action of Certain Esters and Ethers of Choline, and their Relation to Muscarine', Journal of Pharmacology and Experimental Therapeutics, 6 (1914), 14790.
121. See Carrier (note 2), 219; Shanks (note 2); Weatherall (note 8), 240f.
122. Weatherall (note 8), 150-54;
123. Wolf-Dieter Müller-Jahncke and Christoph Fischer, Geschichte der Arzneimitteltherapie (Stuttgart, Deutscher Apotheker Verlag, 1996), 226-29.
124. Everhardus Jacobus Ariëns, 'Affinity and Intrinsic Activity in the Theory of Competitive Inhibition', Archives Internationales de Pharmacodynamie et de Thérapie, 99 (1954), 3249.
125. R. P. Stephenson, 'A Modification of Receptor Theory', British Journal of Pharmacology, 11 (1956), 379-93 (380).
126. Robert F. Furchgott at the Department of Pharmacology in St. Louis also proposed that drug action was not directly proportional to the fraction of the total number of receptors occupied. He regarded the drug-receptor reaction only as the starting point of a complex chain of reactions leading to an observable response such as contraction. Cf. Robert F. Furchgott, 'The Pharmacology of Vascular Smooth Muscle', Pharmacological Review, 1 (1955), 183-265 (200).
127. Cf. Clark (note 50), 193.
128. Stephenson (note 78), 380.
129. Furchgott (note 79), 223.
130. Stephenson (note 78), 391.
131. See also the very similar explanation given by Mark Nickerson, 'Receptor Occupancy and Tissue Response', Nature. 178 (1956), 697-98.
132. Stephenson (note 78), 392.
133. Bernard Katz and S. Thesleff, 'A Study of the "Desensitization" Produced by Acetylcholine at the Motor End-Plate', Journal of Physiology, 138 (1957), 63-80.
134. For biographical details see H. P. Rang and Lord Perry of Wallon, 'Sir William Drummond Macdonald Paton, C.B.E.', Biographical Memoirs of Fellows of the Royal Society, 42 (1996), 291-314.
135. William D. M. Paton, 'A Theory of Drug Action Based on the Rate of Drug-Receptor Combination', Proceedings of the Royal Society of London, series B, 154 (1961), 21-69.
136. Rang and Wallon (note 86), 304.
137. Robinson (note 3), 152; Rang and Walton (note 86), 304.
138. E. J. Ariëns (ed.), Molecular Pharmacology. The Mode of Action of Biologically Active Compounds, 2 vols (New York, Academic Press, 1964).
139. D. K. de Jongh, 'Some Introductory Remarks on the Conception of Receptors', in Ariëns (note 90), I, xiii-xvi (xvi).
140. J. W Black, A. F. Crowther, R. G. Shanks, L. H. Smith, A. C. Dornhorst, A New Adrenergic Beta-Receptor Antagonist', Lancet, 1964/1, 1080-81;
141. Brian Prichard and Peter M. S. Gillam, The Use of Propranolol in the Treatment of Hypertension', British Medical Journal, 1964/11, 725-27.
142. See Robinson (note 3), 157-63.
143. See Maehle (note 1) and Gerald L. Geison, Michael Foster and the Cambridge School of Physiology: The Scientific Enterprise in Late Victorian Society (Princeton, N.J., Princeton University Press, 1978).
144. See also Mark Weatherall, Gentlemen, Scientists and Doctors." Medicine at Cambridge, 1800-1940 (Woodbridge, Boydell Press, 2000).
145. See also, especially for earlier criticisms of Ehrlich's concept of chemoreceptors in the 1920s, John Parascandola, 'Carl Voegtlin and the "Arsenic Receptor" in Chemotherapy', Journal of the History of Medicine and Allied Sciences, 32 (1977), 151-71.