PCL302H1 Lecture 2: Lecture 2 - Receptor Quantitation I.pdf
28 Sep 2014
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Document Summary
Protein on the surface of or inside the cell that receives chemical signals and mediates a response . A cell surface receptor binds with high affinity to an agonist: non-specific binding site: A biological component to which the drug binds but does not lead to any effect . A mathematical model: describe drug-receptor interactions, calculate parameters of the interaction from experimental data, assumptions, a drug binds reversibly to its receptor with high affinity, the effect of a drug is proportional to the number of receptors occupied. Drug binds to receptor depends on concentration of the drug and the receptor and onset constant. On the same time there are drugs fall off the receptor. Dr = drug receptor complex kon = onset rate constant koff = offset rate constant. Rate of binding and rate of dissociation are the same. At equilibrium (i. e. when the two rates are equal): [d] [r] kon = [dr] koff.
