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Agonists—Antagonists
An agonist (A) has affinity (tendency to adhere) for a receptor and affects the receptor
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The agonist binds to the inactive receptor and thereby causes the resting conformation
to change into the active state. The antagonist attaches to the inactive receptor without
altering its conformation.
Allosteric antagonism. The antagonist is bound outside the agonist’s site of attachment at
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the receptor and induces a decrease in agonist affinity. The latter is increased in the case
of allosteric synergism.
Functional antagonism. Two agonists acting via different receptors affect the same
variable (e. g., luminal diameter of bronchi) in opposite directions (epinephrine† dilation;
histamine † constriction). 60 Drug–Receptor Interactions.
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