The affinity–efficacy problem: an essential part of pharmacology education Article Swipe
James P. Higham
,
David Colquhoun
·
YOU?
·
· 2024
· Open Access
·
· DOI: https://doi.org/10.1098/rsos.240487
YOU?
·
· 2024
· Open Access
·
· DOI: https://doi.org/10.1098/rsos.240487
A fundamental mistake in receptor theory has led to an enduring misunderstanding of how to estimate the affinity and efficacy of an agonist. These properties are inextricably linked and cannot be easily separated in any case where the binding of a ligand induces a conformation change in its receptor. Consequently, binding curves and concentration–response relationships for receptor agonists have no straightforward interpretation. This problem—the affinity–efficacy problem—remains overlooked and misunderstood despite it being recognized in 1987. To avoid the further propagation of this misunderstanding, we propose in this review that the affinity–efficacy problem should be included in the core curricula for pharmacology undergraduates proposed by the British Pharmacological Society and the International Union of Basic and Clinical Pharmacology (IUPHAR).
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Metadata
- Type
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- Language
- en
- Landing Page
- https://doi.org/10.1098/rsos.240487
- OA Status
- gold
- Cited By
- 3
- References
- 32
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The affinity–efficacy problem: an essential part of pharmacology educationWork title
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reviewOpenAlex work type
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2024Year of publication
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2024-07-01Full publication date if available
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James P. Higham, David ColquhounList of authors in order
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https://doi.org/10.1098/rsos.240487Publisher landing page
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YesWhether a free full text is available
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goldOpen access status per OpenAlex
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Pharmacology, Computational biology, Medicine, Chemistry, Computer science, BiologyTop concepts (fields/topics) attached by OpenAlex
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3Total citation count in OpenAlex
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2025: 2, 2024: 1Per-year citation counts (last 5 years)
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10Other works algorithmically related by OpenAlex
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