Nature of Occupancy-Response RelationshipGeneric: HyperbolicLimiting Case: Linear
Theoretical relationship between half-maximal drug response and the operational efficacy and affinity of a drug (Black et al. 2010)Embedded Image (6)
or
Embedded Image (7)
Anticipated experimental Embedded Image of reference agonistSince Embedded Image, eq. 6 becomesSince Embedded Image, eq. 6 becomes
Embedded Image (8a)Embedded Image (8b)
Anticipated experimental Embedded Image of a test agonistSince Embedded Image, eq. 6 becomes
Embedded Image (9a)Embedded Image (9b)
Experimental implementation of operational model to determine affinity
Implementation of the operational model assumes eq. 7 to be valid for experimentally measured values; in other words,
Embedded Image (10)
Experimental determination of affinity, Embedded Image, of a test agonist
Substituting eqs. 5a and 9aSubstituting eqs. 5b and 9b
Embedded ImageEmbedded Image
Embedded Image (11a)Embedded Image (11b)