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Target intelligence / Profile preview
Benzodiazepine Site of the GABAA Receptor (BZD Site)
- Target
- BZD Site
- Molecular classification
- Receptor, Ligand-gated ion channel subunit interface, Allosteric binding site
01
Overview
The benzodiazepine site is an allosteric binding site on the GABAA receptor, located at the interface between alpha and gamma subunits. Binding of benzodiazepines to this site enhances GABA's effects, leading to increased chloride ion influx and neuronal inhibition. Different alpha subunit combinations confer distinct pharmacological properties, influencing sedation, anxiolysis, and other therapeutic effects.
- Other names
- Benzodiazepine ReceptorBZD binding siteGABAA Receptor Benzodiazepine Site
02
Mechanism of action
Positive allosteric modulation of GABAA receptor activity, increasing the frequency of chloride channel opening in response to GABA.
03
Biological functions
Modulation of GABAergic neurotransmissionRegulation of neuronal excitabilityChloride ion channel modulationSynaptic inhibition
04
Disease associations
Anxiety disordersInsomniaEpilepsyMuscle spasticityAlcohol withdrawal
05
Safety considerations
SedationRespiratory depressionToleranceDependenceWithdrawal syndromeCognitive impairment
06
Interacting drugs
Diazepam
4 more in the full profile.
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