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Gabapentinoid
Gabapentinoids are 3-substituted derivatives of the neurotransmitter γ-aminobutyric acid (GABA) which block α2δ subunit-containing voltage-dependent calcium channels (VDCCs). Clinically-used gabapentinoids include gabapentin (Neurontin) and pregabalin (Lyrica),〔〔 as well as a gabapentin prodrug, gabapentin enacarbil (Horizant). Another analogue mirogabalin is in clinical trials but has not yet been approved.〔Vinik A, Rosenstock J, Sharma U, Feins K, Hsu C, Merante D, et al. 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''. 2014 Dec;37(12):3253-61. doi: 10.2337/dc14-1044. PMID 25231896〕 Other compounds from this family used in research but not developed for medical use include atagabalin, 4-methylpregabalin and PD-217,014. Gabapentinoids are used clinically in the treatment of conditions including epilepsy, neuropathic pain, fibromyalgia, anxiety, and restless legs syndrome, among others.〔〔
Recently, phenibut (β-phenyl-GABA), a close analogue of pregabalin (β-isobutyl-GABA), has been found to similarly bind to and block α2δ-containing VDCCs, notably with an affinity exceeding that of its other actions, effectively making it a gabapentinoid. Baclofen (β-(4-chlorophenyl)-GABA) has also been found to do this, but relatively weakly.〔
==See also==
* GABAergic
* GABA analogue
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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