Pharmacology 3620 Lecture Notes - Lecture 7: Partial Agonist, Intrinsic Activity, Bind

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Introduction: types of drug-receptor interactions, how drugs mediate their effects depends on how they interact with the receptors. Partial agonists: partial agonists are molecules that bind to the receptor but only produce a partial response, even when all of the receptors are saturated. In the illustration, the binding of the agonist causes the channel to open: however, when the antagonist binds to the same site as the agonist, nothing happens, But that site is now blocked agonist cannot bind, and the channel stays closed. Irreversible antagonists bind to the receptor with very high affinity (usually a covalent bond; irreversible) Non-receptor antagonists: some antagonists do not act on receptors, and some are just lumped in the category. Other : chemical antagonists are drugs that bind and sequester the agonist, so it is unavailable to act on the receptor, ex: your patient has overdosed on heparin, an acidic negatively charged drug (a blood thinner).

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