| 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 | |
Gabapentinoids, also known as α2δ ligands, are a class of drugs that are chemically derivatives of the inhibitory neurotransmitter gamma-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).[1][2][3][4][5]
Clinically used gabapentinoids include gabapentin, pregabalin, and mirogabalin,[3][4] as well as a gabapentin prodrug, gabapentin enacarbil.[6] Further analogues like imagabalin and atagabalin have been tested in clinical trials but their development has been halted.[7] Other gabapentinoids which are used in scientific research but have not been approved for medical use include 4-methylpregabalin and PD-217,014.[8]
Additionally, phenibut has been found to act as a very low affinity gabapentinoid in addition to its action as a GABAB receptor agonist.[9][10]
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ Douglas Kirsch (October 10, 2013). Sleep Medicine in Neurology. John Wiley & Sons. p. 241. ISBN 978-1-118-76417-6.
- ^ 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.
- ^ Varadi G (2024). "Mechanism of Analgesia by Gabapentinoid Drugs: Involvement of Modulation of Synaptogenesis and Trafficking of Glutamate-Gated Ion Channels". Journal of Pharmacology and Experimental Therapeutics. 388 (1): 121–133. doi:10.1124/jpet.123.001669. ISSN 0022-3565. PMID 37918854.
- ^ Cite error: The named reference
pmid26234470was invoked but never defined (see the help page). - ^ 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.
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