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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 and pregabalin.
Gabapentinoids are close structural relatives, and are all 3-substituted derivatives of GABA, the differences being the addition of a cyclohexyl group on the GABA chain in the case of gabapentin, the substitution of that cyclohexyl group for an isobutyl group in the case of pregabalin, and the substitution of that isobutyl group with a cyclic phenyl ring in the case of phenibut. Hence, they are GABA analogues, as well as γ-amino acids.
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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