BIOM 3090 Lecture Notes - Lecture 15: Morphine, Heparin, Receptor Antagonist
31 May 2016
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Proportion between the effect and the number of receptors bound. Need to have a model that we can make inferences about. Add at bottom: the affinity of a drug is most influenced by changed in the off rate. Kon forward or association rate of equation. Koff reverse or dissociation rate of the equation will go backwards. Affinity of a drug at a receptor, tend to talk about koff. Koff/kon dissociation rate constant specific for drug-receptor combo. Ka opposite = 1/kd drug with a really high affinity is going to have to have a low kd (high ka) Equilibrium equation: (l)(r) kon = lr x koff. Equation in red fraction of bound receptors over total receptors is equal to the ligand concentration over the kd for that receptor plus the ligand concentration. Lr/ro = fraction of all receptors that are ligand bound. Semilog allows us to pull the middle apart get a s shaped or sigmoidal plot.
