Introduction To Agonists: Theory
Occupancy, Agonist Concentration And Size Of Response
The mathematical relationship between occupancy, agonist concentration and response has not yet been fully worked out.
But one possibility which takes into account the characteristics of both the tissue and the agonist-receptor complex is shown below:
Where:
= intrinsic efficacy of drug-receptor complex (drug characteristic)
xA = concentration of agonist
KA = backward rate constant / forward rate constant (drug characteristic)
f = transducer function (tissue characteristic)
Ntot = total number of receptors present (tissue characteristic)KA = backward rate constant / forward rate constant (drug characteristic)