5-Fluorowillardiine

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A chemical compound used in neuroscience research



Overview

5-Fluorowillardiine is a chemical compound that acts as an agonist at certain subtypes of the glutamate receptor, specifically the AMPA receptor and the kainate receptor. It is a derivative of the naturally occurring compound willardiine, with a fluorine atom substituted at the 5-position of the uracil ring.

Chemical Structure

5-Fluorowillardiine is a fluorinated analog of willardiine, which is an amino acid derivative. The presence of the fluorine atom enhances its activity at the AMPA and kainate receptors, making it a useful tool in neuroscience research for studying the function of these receptors.

Mechanism of Action

As an agonist, 5-Fluorowillardiine binds to the AMPA and kainate receptors, which are types of ionotropic glutamate receptors. These receptors are ligand-gated ion channels that mediate fast synaptic transmission in the central nervous system. Upon binding, 5-Fluorowillardiine induces a conformational change in the receptor, leading to the opening of the ion channel and the influx of cations such as sodium (Na_) and calcium (Ca__) into the neuron. This results in depolarization of the neuronal membrane and the propagation of an action potential.

Applications in Research

5-Fluorowillardiine is primarily used in research settings to study the physiological and pathological roles of AMPA and kainate receptors. It is particularly valuable in experiments designed to elucidate the mechanisms of excitotoxicity, a process by which excessive activation of glutamate receptors leads to neuronal injury and death. This compound is also used to investigate the synaptic plasticity mechanisms underlying learning and memory.

Safety and Handling

As with many research chemicals, appropriate safety precautions should be taken when handling 5-Fluorowillardiine. It should be used in a controlled laboratory environment, and researchers should wear suitable protective equipment to prevent exposure.

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Contributors: Prab R. Tumpati, MD