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Mechanisms of the gabapentinoids and α2δ-1 calcium channel subunit in neuropathic pain

Patel, RA; Dickenson, AH; (2016) Mechanisms of the gabapentinoids and α2δ-1 calcium channel subunit in neuropathic pain. Pharmacology Research & Perspectives , 4 (2) , Article e00205. 10.1002/prp2.205. Green open access

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Abstract

The gabapentinoid drugs gabapentin and pregabalin are key front-line therapies for various neuropathies of peripheral and central origin. Originally designed as analogs of GABA, the gabapentinoids bind to the α2δ-1 and α2δ-2 auxiliary subunits of calcium channels, though only the former has been implicated in the development of neuropathy in animal models. Transgenic approaches also identify α2δ-1 as key in mediating the analgesic effects of gabapentinoids, how- ever the precise molecular mechanisms remain unclear. Here we review the cur- rent understanding of the pathophysiological role of the α2δ-1 subunit, the mechanisms of analgesic action of gabapentinoid drugs and implications for efficacy in the clinic. Despite widespread use, the number needed to treat for gabapentin and pregabalin averages from 3 to 8 across neuropathies. The failure to treat large numbers of patients adequately necessitates a novel approach to treatment selection. Stratifying patients by sensory profiles may imply common underlying mechanisms, and a greater understanding of these mechanisms could lead to more direct targeting of gabapentinoids.

Type: Article
Title: Mechanisms of the gabapentinoids and α2δ-1 calcium channel subunit in neuropathic pain
Open access status: An open access version is available from UCL Discovery
DOI: 10.1002/prp2.205
Publisher version: http://dx.doi.org/10.1002/prp2.205
Language: English
Additional information: Copyright © 2016 The Authors. Pharmacology Research & Perspectives published by John Wiley & Sons Ltd, British Pharmacological Society and American Society for Pharmacology and Experimental Therapeutics. This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited. http://creativecommons.org/licenses/by/4.0/
Keywords: Neuropathic pain, gabapentin, pregabalin, alpha 2 delta 1, calcium channel subunit
UCL classification: UCL > Provost and Vice Provost Offices
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences > Neuro, Physiology and Pharmacology
URI: http://discovery.ucl.ac.uk/id/eprint/1475883
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