Topic summary
Gabapentinoid
Gabapentinoids, also known as α2δ ligands, are a class of drugs that are chemically derivatives of the inhibitory neurotransmittergamma-Aminobutyric acid (GABA) (i.e., GABA analogues) which bind selectively to the α2δ protein that was first described as an auxiliary subunit of voltage-gated calcium channels (VGCCs).
Clinically used gabapentinoids include gabapentin, pregabalin, baclofen and mirogabalin, as well as a gabapentin prodrug, gabapentin enacarbil. Further analogues like imagabalin and atagabalin have been tested in clinical trials but their development has been halted. Other gabapentinoids which are used in scientific research but have not been approved for medical use include 4-methylpregabalin and PD-217,014.
Additionally, phenibut and baclofen have been found to act as very low affinity gabapentinoid in addition to their action as GABAB receptoragonist.