Agonist, definition

The pA2 calculation is derived by equating the response produced by the full agonist in the absence of the inverse agonist (Equation 6.64 with [B] = 0) to the response in the presence of a concentration of the inverse agonist that produces a dose ratio of 2 (by definition the pA2). For calculation of KB from 10-pAT... 

FIGURE 10.7 Figure illustrating the comparison of concentration-response curves to two full agonists. Equations describe response in terms of the operational model (variable slope version equation see Section 10.6.1). Schematic indicates the interacting species in this case, two full agonists A1 and A2 activating a common receptor R to produce response. Boxes show the relevant measurements (EPMRs) and definitions of the parameters of the model used in the equation. 

In conclusion, H3 ligands offer the attractive vista of multiple applications in various disorders, but the ultimate definition of their therapeutic utility will have to await clinical trial results. Future work will determine whether inverse agonists, neutral antagonists, or protean agonists will constitute the more useful pharmacological intervention. 

Classical approach, following Furchgott, and based on the early view that all the receptors occupied by an agonist are activated First, we recall one of our two earlier definitions of pAR, the proportion of binding sites occupied by A ... 

Both DCI and IEG are now classified as partial agonists. Partial agonist, by definition, is a comparative description. When substance B is unable to produce as large a maximum response as... 

---