A modification of receptor theory¶
STEPHENSON, R. P. (1956). A modification of receptor theory. British Journal of Pharmacology and Chemotherapy, 11(4), 379-393.
Cited by¶
4 citations across 4 artifacts.
Each citation links to the sentence it supports in the citing article.
Primes¶
- Dose-Response Relationship
- Dose-response is clarifying because it enforces explicit specification of the input and output metrics and their functional relationship—rescuing qualitative claims ("more exposure is worse") into quantitative, estimable, predictively-useful curves, in the spirit of Stephenson's (1956) modification of receptor theory, which separated affinity (binding to receptor) from Efficacy (capacity to elicit response) and so disambiguated the parameters latent in any sigmoidal curve.
This sourceDistinguishes affinity (binding) from efficacy (capacity to elicit response); supports D47-026 (dose-response curves encode two physically distinct parameters — potency vs maximal effect — refining Clark's occupancy-only theory).
- Dose-response is clarifying because it enforces explicit specification of the input and output metrics and their functional relationship—rescuing qualitative claims ("more exposure is worse") into quantitative, estimable, predictively-useful curves, in the spirit of Stephenson's (1956) modification of receptor theory, which separated affinity (binding to receptor) from Efficacy (capacity to elicit response) and so disambiguated the parameters latent in any sigmoidal curve.
- Receptor Saturation
- As Stephenson (1956) first formalized in his modification of receptor theory,
This sourceDistinguishes affinity (binding) from efficacy (capacity to elicit response) in receptor pharmacology; clarifies that dose-response curves encode two physically distinct parameters (potency vs maximal effect), refining Clark's earlier occupancy-only theory.
- As Stephenson (1956) first formalized in his modification of receptor theory,
Domain-specific¶
- Efficacy
- Efficacy is the receptor-pharmacology parameter for the maximum effect a drug or ligand can produce at a given target under full receptor engagement, formalized by R. P. Stephenson (1956) and given mechanistic grounding in the del Castillo–Katz two-state receptor model and later in the Black–Leff operational model of agonism
This sourceStephenson's formalization of efficacy as a parameter distinct from affinity, and the accompanying point that a maximal response can occur at fractional occupancy.
- Efficacy is the receptor-pharmacology parameter for the maximum effect a drug or ligand can produce at a given target under full receptor engagement, formalized by R. P. Stephenson (1956) and given mechanistic grounding in the del Castillo–Katz two-state receptor model and later in the Black–Leff operational model of agonism
- Partial Agonist
- A drug can sit on every receptor and still deliver only a fraction of the system maximum, a result that confounded early dose-response analysis until the two-state and operational models made it explicit
This sourceThe efficacy concept that made submaximal response at full occupancy explicit, separating occupancy from activation.
- A drug can sit on every receptor and still deliver only a fraction of the system maximum, a result that confounded early dose-response analysis until the two-state and operational models made it explicit
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