Construct · 1 fields · 3 citations

antagonist: a standalone construct

One name. One construct. A landmark on the map.

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antagonist1 CONSTRUCTReceptor antagonistGADDUM · RECEPTOR BLOCK

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Pharmacology

A molecule that blocks a receptor

In pharmacology, an antagonist is a molecule that binds a receptor and blocks it, occupying the site without switching it on and so preventing an agonist from producing the cell's response. Gaddum's 1937 report on the quantitative effects of antagonistic drugs gave an early measured account of how a blocking drug shifts the response to an activator, building on Clark's 1926 study of how drugs occupy receptors, and Schild's 1949 work on competitive drug antagonism fixed the modern way of grading a competitive antagonist by the concentration needed to counter the agonist. The referent is a chemical that silences a biological receptor, scaled by how strongly it blocks, and it has nothing to do with an opposing muscle or a figure in a drama.[1][2][3]

Unit
A single compound acting at a receptor, scaled by the strength of its block
Recovery means
Not applicable
Measured by
Quantified by the rightward shift it produces in an agonist dose-response curve, summarised by the Schild plot

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Nearby constructs

agonist1 fields · 3 citationsanchor · a standalone constructmuscle1 fields · 1 citationsanchor · a standalone constructconflict4 fields · 5 citationsjingle · one word, four constructs

References

  1. Gaddum, J. H. (1937). The quantitative effects of antagonistic drugs. Journal of Physiology, 89, 7P–9P.
  2. Clark, A. J. (1926). The reaction between acetyl choline and muscle cells. The Journal of Physiology, 61(4), 530–546. https://doi.org/10.1113/jphysiol.1926.sp002314
  3. Schild, H. O. (1949). pAx and competitive drug antagonism. British Journal of Pharmacology and Chemotherapy, 4(3), 277–280. https://doi.org/10.1111/j.1476-5381.1949.tb00548.x

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