GYKI-52,466
GYKI-52,466
GYKI-52,466 is a chemical compound that acts as a non-competitive antagonist of the AMPA receptor, a subtype of the ionotropic glutamate receptors. It is primarily used in scientific research to study the role of AMPA receptors in the central nervous system.
Chemical Structure and Properties[edit | edit source]
GYKI-52,466 is a derivative of the 2,3-benzodiazepine class of compounds. Its chemical structure is characterized by a benzodiazepine core, which is modified to enhance its selectivity and potency as an AMPA receptor antagonist. The molecular formula of GYKI-52,466 is C₁₆H₁₄N₂O₂, and it has a molecular weight of 266.29 g/mol.
Mechanism of Action[edit | edit source]
GYKI-52,466 functions as a non-competitive antagonist of the AMPA receptor. Unlike competitive antagonists, which bind to the same site as the endogenous ligand, non-competitive antagonists bind to a different site on the receptor. This binding alters the receptor's conformation, reducing its activity regardless of the concentration of the endogenous ligand, glutamate.
Pharmacological Effects[edit | edit source]
By inhibiting AMPA receptors, GYKI-52,466 reduces excitatory neurotransmission in the brain. This can lead to a variety of effects, including neuroprotection in models of ischemia and epilepsy. The compound has been used in research to explore the potential therapeutic benefits of AMPA receptor antagonists in neurological disorders.
Research Applications[edit | edit source]
GYKI-52,466 is widely used in neuroscience research to investigate the physiological and pathological roles of AMPA receptors. Studies have utilized this compound to:
- Examine the contribution of AMPA receptors to synaptic plasticity and long-term potentiation (LTP).
- Investigate the role of AMPA receptors in neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease.
- Explore the potential of AMPA receptor antagonists as treatments for epilepsy and stroke.
Safety and Toxicology[edit | edit source]
As with many research chemicals, the safety profile of GYKI-52,466 is not fully established. It is primarily used in controlled laboratory settings, and researchers must adhere to safety guidelines when handling the compound.
Also see[edit | edit source]
Template:Receptor pharmacology
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