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Transmembrane AMPA receptor regulatory protein gamma 8-dependent AMPA receptor (TARP γ-8-dependent AMPAR)
- Target
- TARP γ-8-dependent AMPAR
- Molecular classification
- Receptor, Ion channel, AMPA receptor complex, Transmembrane AMPA receptor regulatory protein (TARP)
01
Overview
AMPA-type glutamate receptors whose function, trafficking, and pharmacology are specifically regulated by the auxiliary subunit TARP γ-8 (transmembrane AMPA receptor regulatory protein gamma 8). This interaction is crucial for synaptic transmission and plasticity in the central nervous system, particularly in the hippocampus. TARP γ-8 regulates assembly, trafficking, localization, gating kinetics, and pharmacological properties of AMPARs. Selective antagonists that require the presence of TARP γ-8 can modulate specific populations or regions expressing this complex. Deficiency or knockout models lacking functional TARP γ-8 show reduced surface expression/localization of hippocampal AMPARs, impaired long-term potentiation, and behavioral phenotypes resembling attention-deficit hyperactivity disorder (ADHD).
- Other names
- TARP gamma-8-dependent AMPA receptorCACNG8-dependent AMPA receptor
02
Mechanism of action
Selective antagonism of TARP γ-8-dependent AMPA receptors; Modulation of AMPA receptor activity and trafficking by TARP γ-8.
03
Biological functions
Synaptic transmissionSynaptic plasticityRegulation of AMPA receptor traffickingRegulation of AMPA receptor gatingRegulation of AMPA receptor localizationExcitatory neurotransmission
04
Disease associations
EpilepsyAttention-deficit hyperactivity disorder (ADHD)Neurological disorders
05
Safety considerations
Potential for motor side effects with non-selective AMPA receptor antagonistsSeizures (if AMPA receptor activity is excessively reduced)
06
Interacting drugs
LY3130481
3 more in the full profile.
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