Affinity and intrinsic activity in the theory of competitive inhibition. I. Problems and theory¶
Ariëns, E. J. (1954). Affinity and intrinsic activity in the theory of competitive inhibition. I. Problems and theory. Archives Internationales de Pharmacodynamie et de Therapie.
Cited by¶
2 citations across 2 artifacts.
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Domain-specific¶
- Efficacy
- The mechanistic basis of efficacy is the agent's intrinsic activity (α in Stephenson's formulation; intrinsic efficacy in the operational model)
This sourceThe origin of 'intrinsic activity' and the symbol alpha - cited here because it REFUTES the attribution of alpha to Stephenson.
- The mechanistic basis of efficacy is the agent's intrinsic activity (α in Stephenson's formulation; intrinsic efficacy in the operational model)
- Potency
- Third, the in vitro correlate of potency is receptor-binding affinity: the drug's affinity for its receptor (expressed as the dissociation constant Kd or its inverse) is a primary determinant of how little drug is required to produce a given receptor-occupancy and, from that, a given functional effect, making receptor pharmacology the mechanistic basis from which potency is predicted and engineered
This sourceReceptor affinity, separate from intrinsic activity, sets where on the dose axis the response curve sits and so is the in vitro correlate of potency.
- Third, the in vitro correlate of potency is receptor-binding affinity: the drug's affinity for its receptor (expressed as the dissociation constant Kd or its inverse) is a primary determinant of how little drug is required to produce a given receptor-occupancy and, from that, a given functional effect, making receptor pharmacology the mechanistic basis from which potency is predicted and engineered
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