Gabapentinoid

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Chemical structure of pregabalin (Lyrica), a potent gabapentinoid

Gabapentinoids are 3-substituted derivatives of the neurotransmitter γ-aminobutyric acid (GABA) which block α2δ subunit-containing voltage-dependent calcium channels (VDCCs).[1][2] Clinically-used gabapentinoids include gabapentin (Neurontin) and pregabalin (Lyrica),[1][2] as well as a gabapentin prodrug, gabapentin enacarbil (Horizant).[3] Another analogue mirogabalin is in clinical trials but has not yet been approved.[4] 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.[1][3][5]

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.[6] Baclofen (β-(4-chlorophenyl)-GABA) has also been found to do this, but extremely weakly and likely insignificantly relative to its primary action of activation of the GABAB receptor.[6]

See also

References

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