Gabapentinoid
Calcium channel blockers / From Wikipedia, the free encyclopedia
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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).[1][2][3][4] This site has been referred to as the gabapentin receptor (α2δ subunit), as it is the target of the drugs gabapentin and pregabalin.[5]
Gabapentinoid | |
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Drug class | |
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 VDCCsTooltip voltage-dependent calcium channels |
Legal status | |
In Wikidata |
Clinically used gabapentinoids include gabapentin, pregabalin, and mirogabalin,[3][4] as well as a gabapentin prodrug, gabapentin enacarbil.[6] Additionally, phenibut has been found to act as a gabapentinoid in addition to its action of functioning as a GABAB receptor agonist.[7][8] Further analogues like imagabalin are in clinical trials but have not yet been approved.[9] Other gabapentinoids which are used in scientific research but have not been approved for medical use include atagabalin, 4-methylpregabalin and PD-217,014.[citation needed]