γ-Aminobutyric acid analogue (gabapentinoids)

Gabapentinoids are a chemical class of organic compounds that are structural analogues of the neurotransmitter GABA (gamma-aminobutyric acid), built around the same short amino-acid chain but with a lipophilic group added at the 3-position of that backbone. The addition may be a cyclohexane ring fused onto the chain or a branched alkyl group, making the members 3-substituted GABA derivatives. Pharmacologically they act at the alpha-2-delta subunit of voltage-gated calcium channels, producing anxiolytic, anticonvulsant and sedating effects. This shared GABA backbone with a bulky lipophilic substituent is the structural thread linking the class.