Gabapentinoid
Gabapentinoids, also known as α2δ ligands, are a class of drugs that are derivatives of the inhibitory neurotransmitter gamma-Aminobutyric acid (GABA) (i.e., GABA analogues) which block α2δ subunit-containing voltage-dependent calcium channels (VDCCs). This site has been referred to as the gabapentin receptor (α2δ subunit), as it is the target of the drugs gabapentin and pregabalin.
| Gabapentinoid | |
|---|---|
| Drug class | |
Gabapentin, the prototypical gabapentinoid | |
| Class identifiers | |
| Synonyms | α2δ ligands; Ca2+ α2δ ligands |
| Use | Epilepsy; Neuropathic pain; Postherpetic neuralgia; Diabetic neuropathy; Fibromyalgia, Generalized anxiety disorder; Restless legs syndrome |
| ATC code | N03AX |
| Biological target | α2δ subunit-containing VDCCs |
| Legal status | |
| In Wikidata | |
Clinically used gabapentinoids include gabapentin, pregabalin, and mirogabalin, as well as a gabapentin prodrug, gabapentin enacarbil. Additionally, phenibut has been found to act as a gabapentinoid in addition to its action of functioning as a GABAB receptor agonist. Further analogues like imagabalin are in clinical trials but have not yet been approved. Other gabapentinoids which are used in scientific research but have not been approved for medical use include atagabalin, 4-methylpregabalin and PD-217,014.