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Gabapentinoids are a chemical class of psychoactive substances derived from gamma-aminobutyric acid (GABA). Members of this class include gabapentin, F-phenibut, phenibut, baclofen and pregabalin.
Gabapentinoids act by blocking α2δ subunit-containing voltage-dependent calcium channels (VGCCs). While all gabapentinoids block the α2δ channels, they also have unique pharmacological characteristics such as enzyme inhibition.
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