2025A · Question 1
Receptor Dose–Response
(a) Define receptors and provide a brief outline of their classification. (20% of marks). (b) Define the following terms and outline the receptor-drug binding and activation characteristics of each: (i) Agonists (20% of marks). (ii) Partial agonists (20% of marks). (ii) Inverse agonists (20% of marks). (iv) Antagonists (20% of marks).
Other appearances: 2024A Q01 · 2022B Q19
Examiner report comments
The first part of the question required a definition of receptors and outline of their classification. Good answers described receptors as proteins or glycoproteins that are found on cell membranes, on membranes of intracellular organelles or in the cytosol / nucleus and contain a region to which a natural ligand or drug binds specifically (receptor site or recognition site) to bring about a conformational change and subsequent response. Receptors can be grouped into 3 classes depending on mechanism of action, altered ion permeability, production of intermediate messengers and regulation of gene transcription. Further descriptions of the different types of receptors/downstream messages were not required. The second part of the question is well covered in the outlined pharmacology textbooks namely Peck and Hill, Stoelting and Goodman and Gillman’s. This is best answered by applying receptor theory: namely that receptors can exist in two states, an active and inactive state. Agonists stabilise the receptor in the active state, partial agonists occupy (and block) the binding site but do not completely favour the active state, whilst inverse agonists stabilise the receptor in the inactive state. Antagonists simply block the binding site and prevent agonists from binding. A description then of affinity and intrinsic activity of each group would complete your answer.