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 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 …

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 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 …

Activity profile of pregabalin in rodent models of epilepsy and ataxia

MG Vartanian, LL Radulovic, JJ Kinsora, KA Serpa… - Epilepsy research, 2006 - Elsevier
Pregabalin (Lyrica™) is a novel amino acid compound that binds with high affinity to the
alpha2–delta (α2–δ) auxiliary protein of voltage-gated calcium channels. In vivo, it potently …

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 …

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 …

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 …

Anxiolytic-like activity of pregabalin in the Vogel conflict test in α2δ-1 (R217A) and α2δ-2 (R279A) mouse mutants

SM Lotarski, S Donevan, A El-Kattan, S Osgood… - … of Pharmacology and …, 2011 - ASPET
The α2δ auxiliary subunits (α2δ-1 and α2δ-2) of voltage-sensitive calcium channels are
thought to be the site of action of pregabalin (Lyrica), a drug that has been shown to be …

Structure−Activity Relationships of Pregabalin and Analogues That Target the α2-δ Protein

TR Belliotti, T Capiris, IV Ekhato… - Journal of medicinal …, 2005 - ACS Publications
Pregabalin exhibits robust activity in preclinical assays indicative of potential antiepileptic,
anxiolytic, and antihyperalgesic clinical efficacy. It binds with high affinity to the α2-δ subunit …