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Occupancy Theory
Occupancy Theory
of a receptor, namely, that drug–receptor interactions involve two stages: first, there is a complexation
of the
drug with the receptor, which they both termed the affinity;
drugs with the same efficacy (all full agonists), but having
may have less affinity for their receptors than partial agonists or antagonists. Therefore, these two
properties,
why two drugs that can occupy the same receptor can act
would be fast (the latter faster than the former). The rate of
theory, the rate theory does not rationalize why the different
with a receptor two general types of macromolecular perturbations could result: a specific
conformational perturbation
inverse agonism.
Receptor Activation
which cannot. In the absence of a natural ligand or agonist, the equilibrium between R* and R defines
the basal activity
resting state, but not to the extent that a full inverse agonist
states.