Onfasprodil

Onfasprodil

Onfasprodil is a pharmacological agent that acts as an antagonist at the NMDA receptor, a type of ionotropic glutamate receptor in the central nervous system. It is primarily used in the research of neurological disorders and has potential therapeutic applications in conditions such as stroke, Alzheimer's disease, and Parkinson's disease.

Pharmacology

Onfasprodil is a selective antagonist at the polyamine site of the NMDA receptor. This site is distinct from the glutamate and glycine binding sites of the receptor. Antagonism at the polyamine site inhibits the activity of the NMDA receptor, reducing the influx of calcium ions into the cell. This can protect neurons from excitotoxicity, a process where excessive activation of glutamate receptors leads to cell death.

Therapeutic Potential

Due to its ability to inhibit NMDA receptor activity, onfasprodil has potential therapeutic applications in a variety of neurological disorders. In stroke, excessive glutamate release can lead to excitotoxicity and neuronal death. By inhibiting the NMDA receptor, onfasprodil may protect neurons and reduce the extent of brain damage.

In Alzheimer's disease, abnormal NMDA receptor activity is thought to contribute to the loss of neurons. Onfasprodil may have potential as a treatment to slow the progression of this disease.

Similarly, in Parkinson's disease, onfasprodil may protect dopaminergic neurons in the substantia nigra, a region of the brain that is particularly affected in this condition.

Research

Research into the potential therapeutic applications of onfasprodil is ongoing. Preclinical studies in animal models of stroke, Alzheimer's disease, and Parkinson's disease have shown promising results, but further research is needed to determine the safety and efficacy of onfasprodil in humans.

See Also

• NMDA receptor antagonist
• Excitotoxicity
• Neuroprotection