Podcast
Questions and Answers
What type of ligands preferentially bind and stabilize the inactive conformation of a receptor?
What type of ligands preferentially bind and stabilize the inactive conformation of a receptor?
- Inverse agonists (correct)
- Partial agonists
- Agonists
- Antagonists
Which type of drug interaction with a receptor can be irreversible, like aspirin?
Which type of drug interaction with a receptor can be irreversible, like aspirin?
- Hydrophobic interaction
- Ionic interaction
- Hydrogen bond
- Covalent interaction (correct)
What does KD measure in pharmacology when referring to drug affinity for a target?
What does KD measure in pharmacology when referring to drug affinity for a target?
- Concentration of drug needed to cause toxicity
- Affinity of a drug for multiple targets
- Concentration of drug needed to occupy 50% of receptors (correct)
- Drug concentration needed to produce the pharmacological benefit
How can you determine which receptor is mediating the effects of a drug?
How can you determine which receptor is mediating the effects of a drug?
What does the equation KD = [D] [R] represent in pharmacology?
What does the equation KD = [D] [R] represent in pharmacology?
When the concentration of ligand equals the Kd, what percentage of receptors will be occupied at equilibrium?
When the concentration of ligand equals the Kd, what percentage of receptors will be occupied at equilibrium?
Based on the text, what can be inferred about unoccupied receptors and occupied receptors?
Based on the text, what can be inferred about unoccupied receptors and occupied receptors?
Which type of ligands preferentially bind and stabilize the active conformation of a receptor?
Which type of ligands preferentially bind and stabilize the active conformation of a receptor?
What is the significance of half the receptors being free and half being bound to ligand?
What is the significance of half the receptors being free and half being bound to ligand?
What is constitutive (basal) activity of a receptor defined as?
What is constitutive (basal) activity of a receptor defined as?
Which type of ligands block the ability of agonists to bind but do not change the equilibrium of a receptor?
Which type of ligands block the ability of agonists to bind but do not change the equilibrium of a receptor?
What is the term used to describe receptors that spend enough time in the active conformation in the absence of agonist to activate transducers?
What is the term used to describe receptors that spend enough time in the active conformation in the absence of agonist to activate transducers?
What is the equilibrium effect of antagonists on the inactive and active conformations of a receptor?
What is the equilibrium effect of antagonists on the inactive and active conformations of a receptor?
In pharmacology, what term is used to refer to the macromolecule with which a drug interacts?
In pharmacology, what term is used to refer to the macromolecule with which a drug interacts?
