Understanding Receptors in Pharmacology
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Questions and Answers

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?

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

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

    <p>The dissociation constant between drug and receptor</p> Signup and view all the answers

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

    <p>50%</p> Signup and view all the answers

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

    <p>Unoccupied receptors are half of the occupied receptors</p> Signup and view all the answers

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

    <p>Agonists</p> Signup and view all the answers

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

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

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

    <p>Ligand-independent activity</p> 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?

    <p>Antagonists</p> 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?

    <p>Constitutive receptors</p> Signup and view all the answers

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

    <p>Equally bind to both conformations</p> Signup and view all the answers

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

    <p>Receptor</p> Signup and view all the answers

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