Pharmacodynamics 3 Flashcards
Competitive antagonists
Bind in reversible manner to the receptor to block agonist action
Competitive antagonists shift curve
To the right without shifting the maximum response
Will not change the maximum
Can overcome with more agonist
Partial agonists as an antagonist
Can block action of a full agonist by taking up receptor binding sites
Irreversible antagonists
Bind to receptor and then covalently link
Irreversible antagonists shift curve
Lower max and shift to the right
Cannot be overcome with more agonist
Constitutively active receptors
Under certain conditions, receptor can assume active conformation in absence of activting ligand
Cause of constitutively active receptors
Genetic mutations that cause loss of control by regulators
Inverse agonism
Inverse agonist binds to constiutively actie receptor, decreasing the receptor activation