This article is a stub.
As such, it may contain incomplete or wrong information. You can help by expanding it.
Gabapentinoids are a relatively small chemical class of psychoactive substances derived from gamma-aminobutyric acid (GABA). Members of this class include gabapentin, F-phenibut, phenibut and pregabalin.
Gabapentinoids are close structural relatives, and are all 3-substituted derivatives of GABA, the differences being the addition of a cyclohexyl group on the GABA chain in the case of gabapentin, the substitution of that cyclohexyl group for an isobutyl group in the case of pregabalin, and the substitution of that isobutyl group with a cyclic phenyl ring in the case of phenibut. Hence, they are GABA analogues, as well as γ-amino acids.
Gabapentinoids act by inhibiting the α2δ subunit-containing voltage-dependent calcium channels (VGCCs). While all gabapentinoids block the α2δ channels, they also have unique pharmacological characteristics such as enzyme inhibition.
- Elaine Wyllie; Gregory D. Cascino; Barry E. Gidal; Howard P. Goodkin (17 February 2012). Wyllie's Treatment of Epilepsy: Principles and Practice. Lippincott Williams & Wilkins. p. 423. ISBN 978-1-4511-5348-4.
- Honorio Benzon; James P. Rathmell; Christopher L. Wu; Dennis C. Turk; Charles E. Argoff; Robert W Hurley (11 September 2013). Practical Management of Pain. Elsevier Health Sciences. p. 1006. ISBN 978-0-323-17080-2.
- Patel, R., & Dickenson, A. H. (2016). Mechanisms of the gabapentinoids and α2δ‐1 calcium channel subunit in neuropathic pain. Pharmacology research & perspectives, 4(2).https://doi.org/10.1002/prp2.205
- Goldlust, A., Su, T. Z., Welty, D. F., Taylor, C. P., & Oxender, D. L. (1995). Effects of anticonvulsant drug gabapentin on the enzymes in metabolic pathways of glutamate and GABA. Epilepsy research, 22(1), 1-11.https://doi.org/10.1016/0920-1211(95)00028-9