Pharmacology: Anxiolytic and Hypnotic Drugs
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Questions and Answers

Where do benzodiazepines bind on the GABA extsubscript{A} receptor?

  • At a high-affinity site at the interface of the $eta$ and $eta$ subunits
  • At the GABA-binding site between the $eta$ and $ heta$ subunits
  • At a specific, high-affinity site at the interface of the $ extalpha$ subunit and the $ extgamma$ subunit (correct)
  • At a specific, high-affinity site at the interface of the $eta$ subunit and the $ heta$ subunit
  • What is one mechanism through which benzodiazepines produce anxiolytic effects at low doses?

  • By stimulating the release of GABA from presynaptic neurons in the cortex
  • By enhancing GABAergic transmission in neurons having the $ extalpha_2$ subunit in their GABA extsubscript{A} receptors (correct)
  • By reducing the synthesis of GABA in the limbic system
  • By inhibiting $ extalpha_1$ subunits in the GABA extsubscript{A} receptors in the motor cortex
  • What is the main action of benzodiazepines on chloride ion channels?

  • Increasing the frequency of channel openings produced by GABA (correct)
  • Increasing the amount of chloride that binds to the ion channel
  • Blocking the ion channel to prevent chloride from passing through
  • Decreasing the passage of chloride ions through the channel
  • What designations are given to common BZ receptor subtypes in the CNS?

    <p>BZ extsubscript{1} and BZ extsubscript{2}</p> Signup and view all the answers

    How do benzodiazepines affect the affinity of GABA for its binding site?

    <p>They increase the affinity of GABA for the binding site</p> Signup and view all the answers

    Which part of the brain is most involved in the anxiolytic effects of benzodiazepines?

    <p>Limbic system</p> Signup and view all the answers

    Study Notes

    Anxiolytic and Hypnotic Drugs

    • Benzodiazepines modulate GABA effects by binding to a specific, high-affinity site on the GABA(_A) receptor, located at the interface of the α subunit and the γ subunit.

    Mechanism of Action

    • Benzodiazepines increase the frequency of channel openings produced by GABA.
    • Binding of a benzodiazepine to its receptor site increases the affinity of GABA for the GABA-binding site (and vice versa).

    BZD Receptor Subtypes

    • BZ(_1) subtype: includes an α(_1) subunit.
    • BZ(_2) subtype: includes an α(_2) subunit.

    Clinical Effects

    • The clinical effects of benzodiazepines correlate well with the binding affinity of each drug for the GABA receptor–chloride ion channel complex.

    Actions of Benzodiazepines

    • Reduction of anxiety: anxiolytic effects at low doses.
    • Mechanism of anxiolytic action: selectively enhancing GABAergic transmission in neurons having the α(_2) subunit in their GABA(_A) receptors, thereby inhibiting neuronal circuits in the limbic system of the brain.

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    Description

    This quiz covers the effects and mechanisms of benzodiazepines on GABA receptors in the CNS, including receptor subtypes and binding sites.

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