The emergence of the drug receptor theory

@article{Maehle2002TheEO,
  title={The emergence of the drug receptor theory},
  author={A H Maehle and C R Pr{\"u}ll and Robert F. Halliwell},
  journal={Nature Reviews Drug Discovery},
  year={2002},
  volume={1},
  pages={637-641}
}
Today, the concept of specific receptors for drugs and transmitters lies at the very heart of pharmacology. Less than one hundred years ago, this novel idea met with considerable resistance in the scientific community. To mark the 150th anniversary of the birth of John Newport Langley, one of the founders of the receptor concept, we highlight his most important observations, and those of Paul Ehrlich and Alfred Joseph Clark, who similarly helped to establish the receptor theory of drug action. 
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  • 2006
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References

SHOWING 1-10 OF 47 REFERENCES
A study of the adrenotropic receptors.
  • R. Ahlquist
  • Chemistry, Medicine
    The American journal of physiology
  • 1948
TLDR
Experiments described in this paper indicate that although there are two kinds of adrenotropic receptors they cannot be classified simply as excitatory or inhibitory since each kind of receptor may have either action depending upon where it is found.
Drugs on trial
TLDR
This book demonstrates that the basic methodology of the field, including chemical analysis, in vitro testing, animal experimentation and human research, was already developed in the course of the seventeenth and eighteenth centuries.
The Rate of Action of Drugs on Cells
TLDR
The rate of response of a tissue to the action of a drug can be studied in two way: measurement of some graded action and measurement of the rate of incidence of some all-or-none effect.
Chemical structure and sympathomimetic action of amines
TLDR
The elucidation of the structure of the active principle of the stupra-renal medulla by the work of Abell and its synthesis by Stolz 7 and by Dakin8 led to the physiological investigation of substances nearly related to it in chemical structure.
Pasteur, Pastorians, and the dawn of immunology: the importance of specificity.
  • A. Silverstein
  • Biology, Medicine
    History and philosophy of the life sciences
  • 2000
Throughout his career, the problems that attracted Louis Pasteur almost invariably involved considerations of specificity of structure and/or of action. Thus, his work on asymmetric crystals showed
Paul Ehrlich's Receptor Immunology: The Magnificent Obsession
List of Plates. Introduction by Sir Gustav Nossal. Preface. The Background to Ehrlich's Immunology: Origins of the Receptor Theory. On Ricin and Abrin: Quantitation Enters Immunity Research. The
The Collected Papers of Paul Ehrlich
  • J. Fruton
  • Computer Science
    The Yale Journal of Biology and Medicine
  • 1957
TLDR
Although his studies on immune reactions and on chemotherapy came after 1890, the earlier work was no less important, since it included his research on the use of aniline dyes for hematological and bacteriological staining, for the study of biochemical reactions, and for the examination of pathological tissues and fluids.
Immunology Dichotomized. (Book Reviews: Species and Specificity. An Interpretation of the History of Immunology.)
TLDR
This chapter discusses specificity and Unitarianism in XIX Century Botany and Bacteriology, and the decline and persistence of Erlich's chemical theory.
The mode of action of specific substances with special reference to secretin
TLDR
The injection of tissue extracts during pancreatic secreti and the mode of action of strychnine reveal the role of substances in the pancreas upon which secretin acts.
Croonian Lecture, 1906: On Nerve Endings and on Special Excitable Substances in Cells
Amongst the fundamental problems of physiology is the determination of the actual seat of the changes which accompany or are the cause of physiological activity. The earliest step was the attribution
...
1
2
3
4
5
...