Understanding Receptors in Pharmacology

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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?

Hydrophobic interaction

Ionic interaction

Hydrogen bond

Covalent interaction (correct)

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?

By comparing drug affinity and potency at a target to the concentrations producing pharmacological benefit Signup and view all the answers

What does the equation KD = [D] [R] represent in pharmacology?

The dissociation constant between drug and receptor Signup and view all the answers

When the concentration of ligand equals the Kd, what percentage of receptors will be occupied at equilibrium?

50% Signup and view all the answers

Based on the text, what can be inferred about unoccupied receptors and occupied receptors?

Unoccupied receptors are half of the occupied receptors Signup and view all the answers

Which type of ligands preferentially bind and stabilize the active conformation of a receptor?

Agonists Signup and view all the answers

What is the significance of half the receptors being free and half being bound to ligand?

It reflects a specific type of ligand-receptor interaction Signup and view all the answers

What is constitutive (basal) activity of a receptor defined as?

Ligand-independent activity Signup and view all the answers

Which type of ligands block the ability of agonists to bind but do not change the equilibrium of a receptor?

Antagonists Signup and view all the answers

What is the term used to describe receptors that spend enough time in the active conformation in the absence of agonist to activate transducers?

Constitutive receptors Signup and view all the answers

What is the equilibrium effect of antagonists on the inactive and active conformations of a receptor?

Equally bind to both conformations Signup and view all the answers

In pharmacology, what term is used to refer to the macromolecule with which a drug interacts?

Receptor Signup and view all the answers

Understanding Receptors in Pharmacology

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