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Questions and Answers
Where do benzodiazepines bind on the GABA extsubscript{A} receptor?
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?
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?
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?
What designations are given to common BZ receptor subtypes in the CNS?
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How do benzodiazepines affect the affinity of GABA for its binding site?
How do benzodiazepines affect the affinity of GABA for its binding site?
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Which part of the brain is most involved in the anxiolytic effects of benzodiazepines?
Which part of the brain is most involved in the anxiolytic effects of benzodiazepines?
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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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