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    Affinity Efficacy Potency: Compete With Agonists For The Receptor

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    william warton
    Antagonists bind to receptors but do not activate them, and therefore have no intrinsic efficacy. They can elicit a response by preventing receptor activation by endogenous chemicals, but only in the presence of an agonist. Antagonists compete with agonists for receptor binding sites. Competitive surmountable antagonism occurs when increasing antagonist concentration causes a parallel rightward shift in the dose-response curve without changing the maximum response. The antagonist dissociation constant and pattern of antagonism are determined by factors like the antagonist's binding affinity, concentration, and duration of exposure to the receptor.

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    Affinity Efficacy Potency: Compete With Agonists For The Receptor

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    william warton
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    Antagonists bind to receptors but do not activate them, and therefore have no intrinsic efficacy. They can elicit a response by preventing receptor activation by endogenous chemicals, but only in the presence of an agonist. Antagonists compete with agonists for receptor binding sites. Competitive surmountable antagonism occurs when increasing antagonist concentration causes a parallel rightward shift in the dose-response curve without changing the maximum response. The antagonist dissociation constant and pattern of antagonism are determined by factors like the antagonist's binding affinity, concentration, and duration of exposure to the receptor.

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    Competitive Antagonism

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    Antagonists bind to receptors but do not activate them, and therefore have no intrinsic efficacy. They can elicit a response by preventing receptor activation by endogenous chemicals, but only in the presence of an agonist. Antagonists compete with agonists for receptor binding sites. Competitive surmountable antagonism occurs when increasing antagonist concentration causes a parallel rightward shift in the dose-response curve without changing the maximum response. The antagonist dissociation constant and pattern of antagonism are determined by factors like the antagonist's binding affinity, concentration, and duration of exposure to the receptor.

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    20 views1 page

    Affinity Efficacy Potency: Compete With Agonists For The Receptor

    Uploaded by

    william warton
    Antagonists bind to receptors but do not activate them, and therefore have no intrinsic efficacy. They can elicit a response by preventing receptor activation by endogenous chemicals, but only in the presence of an agonist. Antagonists compete with agonists for receptor binding sites. Competitive surmountable antagonism occurs when increasing antagonist concentration causes a parallel rightward shift in the dose-response curve without changing the maximum response. The antagonist dissociation constant and pattern of antagonism are determined by factors like the antagonist's binding affinity, concentration, and duration of exposure to the receptor.

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    of 1

    Antagonists bind (have affinity) but do not activate he receptor so they do not have any

    intrinsic efficacy. All drugs have potency.

    Antagonists can elicit a response in the body by preventing receptor activation by


    endogenous chemicals. The effect is only observed when an agonist is present however.
    - No efficacy in vitro
    - Active in vivo (clinical efficacy) // therefore has a measurable potency
    Compete with agonists for the receptor.
    Competitive surmountable antagonism – as the concentration of the antagonist is increased
    there is a parallel rightward shift. The maximum is unchanged. Reduce potency = more
    agonist for the same effect.
    Antagonist dissociation constant (KB) can be derived from:
    - Direct binding assays
    - Schild plot
    - pA2 // How much antagonist do you need to shift the curve two-fold, to double to
    concentration of agonist? It is an indication of antagonist potency
    Not all antagonists are surmountable | If not surmountable, maximum depressed rightward
    shift, not parallel.
    Competitive insurmountable antagonism – The same antagonist gives different effects on
    full and partial agonists acting at the same receptor. Maximum response decreases
    immediately if there are no spare receptors.
    Pattern of antagonism is determined by:
    - KD (association/dissociation constants)
    - Concentration
    - Duration of exposure
    Binding of antagonist is slowly reversible/ irreversible:
    - Strong binding, very high affinity
    - Antagonist effectively candecreases the number of the receptors

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