PHAR 315 Lecture Notes - Lecture 2: Irreversible Antagonist, Agonist, Transmembrane Protein
23 Feb 2016
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Document Summary
3 key principles of pharmacodynamics: receptors largely impact the relationship between the dose and pharmacological effect of a drug, receptors are responsible for selectivity of drug action, receptors mediate the action of pharmacological agonists and antagonists. Components of cells that react with drugs, chemicals, and endogenous molecules: drug + receptor = altered receptor = altered biochemistry of the cell. Most are transmembrane proteins binding site outside, function inside. A drug, chemical or endogenous molecule that binds to the receptor and causes an action in the cell. Even when receptors are fully occupied, partial agonists produce a lesser response than full agonists. Their coupling is less efficient than full agonists. Their curves resemble that of the irreversible antagonist emax, same ec50. Thing that binds could be an agonist or antagonists. A drug, chemical, or endogenous molecule that binds to the receptor and prevents the agonist from binding. Prevents action of the agonist, but causes no action of its own.
