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2,3-Benzodiazepine binding site on AMPA receptors
- Molecular classification
- Allosteric binding site, Ion channel subunit, AMPA receptor subunit
01
Overview
The 2,3-benzodiazepine binding site is an allosteric site on AMPA receptors that is targeted by 2,3-benzodiazepine compounds. These compounds act as noncompetitive antagonists, inhibiting AMPA receptor function and reducing excitatory neurotransmission. This mechanism has potential therapeutic applications in neurological disorders associated with excessive AMPA receptor activation, such as epilepsy and ischemic brain injury.
- Other names
- 2,3-BDZ receptorAMPA receptor 2,3-benzodiazepine binding siteGYKI 52466 binding site
02
Mechanism of action
Noncompetitive antagonism of AMPA receptors, stabilization of closed-channel conformation.
03
Biological functions
Regulation of excitatory neurotransmissionModulation of AMPA receptor activity
04
Disease associations
EpilepsyIschemic brain injuryAmyotrophic lateral sclerosis (ALS)
05
Safety considerations
Potential for off-target effectsLimited clinical dataEffects on neuronal excitability
06
Interacting drugs
GYKI 52466
1 more in the full profile.
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