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Pregabalin is a structural analogue of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). However, it does not bind directly to GABA receptors. Instead, it binds with high affinity to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system. This action reduces the influx of calcium ions, thereby decreasing the release of excitatory neurotransmitters (such as glutamate, norepinephrine, and substance P), which stabilizes neuronal activity.

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