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Gabapentinoid

Not to be confused with Gabapentin.

Gabapentinoid
Drug class
Gabapentin, the prototypical gabapentinoid
Class identifiers
Synonymsα2δ ligands; Ca2+ α2δ ligands
UseEpilepsy; Neuropathic pain; Postherpetic neuralgia; Diabetic neuropathy; Fibromyalgia, Generalized anxiety disorder; Restless legs syndrome
ATC codeN03AX
Biological targetα2δ subunit-containing VDCCsTooltip voltage-dependent calcium channels
Legal status
In Wikidata

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]

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]

  1. ^ Calandre EP, Rico-Villademoros F, Slim M (2016). "Alpha2delta ligands, gabapentin, pregabalin and mirogabalin: a review of their clinical pharmacology and therapeutic use". Expert Rev Neurother. 16 (11): 1263–1277. doi:10.1080/14737175.2016.1202764. PMID 27345098. S2CID 33200190.
  2. ^ Dooley DJ, Taylor CP, Donevan S, Feltner D (2007). "Ca2+ channel alpha2delta ligands: novel modulators of neurotransmission". Trends Pharmacol. Sci. 28 (2): 75–82. doi:10.1016/j.tips.2006.12.006. PMID 17222465.
  3. ^ a b Elaine Wyllie, Gregory D. Cascino, Barry E. Gidal, Howard P. Goodkin (February 17, 2012). Wyllie's Treatment of Epilepsy: Principles and Practice. Lippincott Williams & Wilkins. p. 423. ISBN 978-1-4511-5348-4.
  4. ^ a b Honorio Benzon, James P. Rathmell, Christopher L. Wu, Dennis C. Turk, Charles E. Argoff, Robert W Hurley (September 11, 2013). Practical Management of Pain. Elsevier Health Sciences. p. 1006. ISBN 978-0-323-17080-2.
  5. ^ Eroglu Ç, Allen NJ, Susman MW, O'Rourke NA, Park CY, Özkan E, Chakraborty C, Mulinyawe SB, Annis DS, Huberman AD, Green EM, Lawler J, Dolmetsch R, Garcia KC, Smith SJ, Luo ZD, Rosenthal A, Mosher DF, Barres BA (2009). "Gabapentin Receptor α2δ-1 is a Neuronal Thrombospondin Receptor Responsible for Excitatory CNS Synaptogenesis". Cell. 139 (2): 380–92. doi:10.1016/j.cell.2009.09.025. PMC 2791798. PMID 19818485.
  6. ^ Douglas Kirsch (October 10, 2013). Sleep Medicine in Neurology. John Wiley & Sons. p. 241. ISBN 978-1-118-76417-6.
  7. ^ Cite error: The named reference pmid26234470 was invoked but never defined (see the help page).
  8. ^ Vavers E, Zvejniece L, Svalbe B, Volska K, Makarova E, Liepinsh E, Rizhanova K, Liepins V, Dambrova M (2015). "The neuroprotective effects of R-phenibut after focal cerebral ischemia". Pharmacological Research. 113 (Pt B): 796–801. doi:10.1016/j.phrs.2015.11.013. ISSN 1043-6618. PMID 26621244.
  9. ^ Vinik A, Rosenstock J, Sharma U, Feins K, Hsu C, Merante D (2014). "Efficacy and Safety of Mirogabalin (DS-5565) for the Treatment of Diabetic Peripheral Neuropathic Pain: A Randomized, Double-Blind, Placebo- and Active Comparator–Controlled, Adaptive Proof-of-Concept Phase 2 Study". Diabetes Care. 37 (12): 3253–61. doi:10.2337/dc14-1044. PMID 25231896.

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