GYKI-52466

GYKI-52466 is a non-competitive antagonist at the AMPA receptor, a type of ionotropic glutamate receptor. It was first synthesized and studied by the Hungarian pharmaceutical company Gedeon Richter in the 1980s. GYKI-52466 is known for its selectivity and potency, and it has been widely used in scientific research to understand the function and pharmacology of AMPA receptors.

Chemistry

GYKI-52466 is a derivative of quinazolinone, a nitrogenous heterocyclic compound. It is a 2,3-benzodiazepine compound, which is a class of drugs that includes many well-known anxiolytic and hypnotic medications. However, unlike these drugs, GYKI-52466 does not act on the GABA receptor, but instead selectively blocks the AMPA receptor.

Pharmacology

The primary mechanism of action of GYKI-52466 is as a non-competitive antagonist at the AMPA receptor. This means that it does not compete with the natural ligand, glutamate, for the binding site, but instead binds to a separate site on the receptor and inhibits its function. This inhibition prevents the flow of ions through the receptor, thereby reducing neuronal excitability.

Research and Clinical Implications

Research on GYKI-52466 has contributed significantly to our understanding of the AMPA receptor and its role in various neurological and psychiatric disorders. For example, it has been used in studies investigating the role of AMPA receptors in epilepsy, schizophrenia, depression, and neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease.

While GYKI-52466 itself has not been developed for clinical use due to its poor oral bioavailability and short half-life, its discovery has led to the development of other AMPA receptor antagonists that are currently in clinical use or undergoing clinical trials. These include perampanel, which is approved for the treatment of epilepsy, and decaboxyl-biotin-ligand conjugated AMPA receptor antagonists, which are being investigated for their potential in treating neurodegenerative diseases.

See Also

• AMPA receptor
• Non-competitive antagonist
• Gedeon Richter Plc.
• Quinazolinone
• 2,3-benzodiazepine

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