The diverse therapeutic actions of pregabalin: is a single mechanism responsible for several pharmacological activities?

SM Stahl, F Porreca, CP Taylor, R Cheung… - Trends in …, 2013 - cell.com
Pregabalin is a specific ligand of the alpha 2-delta (α 2-δ) auxiliary subunit of voltage-gated
calcium channels. A growing body of evidence from studies of anxiety and pain indicate that …

Pharmacology and mechanism of action of pregabalin: the calcium channel α2–δ (alpha2–delta) subunit as a target for antiepileptic drug discovery

CP Taylor, T Angelotti, E Fauman - Epilepsy research, 2007 - Elsevier
Pregabalin (Lyrica™) is a new antiepileptic drug that is active in animal seizure models.
Pregabalin is approved in US and Europe for adjunctive therapy of partial seizures in adults …

Pregabalin as a pain therapeutic: beyond calcium channels

SRA Alles, SM Cain, TP Snutch - Frontiers in Cellular Neuroscience, 2020 - frontiersin.org
Initially developed to generate new treatments for epilepsy, gabapentin, and pregabalin
(“gabapentinoids”) were engineered to mimic the action of GABA and to modulate GABA …

Pregabalin is a potent and selective ligand for α2δ-1 and α2δ-2 calcium channel subunits

Z Li, CP Taylor, M Weber, J Piechan, F Prior… - European journal of …, 2011 - Elsevier
Pregabalin, a synthetic branched chain γ-amino acid with anticonvulsant, anxiolytic, and
analgesic activities, has been shown to bind with high affinity to the voltage-gated calcium …

Elucidating the Mechanism of Action of Pregabalin: α2δ as a Therapeutic Target in Anxiety

JA Micó, R Prieto - CNS drugs, 2012 - Springer
This review provides a brief summary of what is known about the anxiolytic mechanism of
action of pregabalin, a highly selective, high-affinity ligand of the P/Q type of voltage-gated …

Pregabalin pharmacology and its relevance to clinical practice

E Ben‐Menachem - Epilepsia, 2004 - Wiley Online Library
Pregabalin is a potent ligand for the alpha‐2‐delta subunit of voltage‐gated calcium
channels in the central nervous system that exhibits potent anticonvulsant, analgesic, and …

Pregabalin: from molecule to medicine

R Kavoussi - European Neuropsychopharmacology, 2006 - Elsevier
Pregabalin, a compound with a novel mechanism of action (MOA), has demonstrated
efficacy as an adjunctive treatment for epilepsy and in several neuropathic pain models …

Calcium channel alpha2-delta type 1 subunit is the major binding protein for pregabalin in neocortex, hippocampus, amygdala, and spinal cord: an ex vivo …

F Bian, Z Li, J Offord, MD Davis, J McCormick… - Brain research, 2006 - Elsevier
Pregabalin is a synthetic amino acid compound effective in clinical trials for the treatment of
post-herpetic neuralgia, diabetic peripheral neuropathy, generalized anxiety disorder and …

Pregabalin action at a model synapse: binding to presynaptic calcium channel α2-δ subunit reduces neurotransmission in mice

I Joshi, CP Taylor - European journal of pharmacology, 2006 - Elsevier
Pregabalin,((S)-3-(aminomethyl)-5-methylhexanoic acid, also known as (S)-3-isobutyl
GABA, Lyrica™) is approved for treatment of certain types of peripheral neuropathic pain …

The mechanisms of action of gabapentin and pregabalin

GJ Sills - Current opinion in pharmacology, 2006 - Elsevier
Gabapentin and pregabalin are structurally related compounds with recognized efficacy in
the treatment of both epilepsy and neuropathic pain. The pharmacological mechanisms by …