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
… of gabapentin and pregabalin. (B) Structure and function of voltage-gated calcium channel
subunits are illustrated by a schematic diagram of a single calcium channel, including the four …

Mechanisms of analgesia by gabapentin and pregabalincalcium channel α2-δ [Cavα2-δ] ligands

CP Taylor - Pain, 2009 - journals.lww.com
… by binding at calcium channel alpha 2 -delta (Ca V α 2 -δ) proteins. The Ca V nomenclature
is … 10–30min) action of gabapentin and pregabalin to decrease calcium influx and transmitter …

[HTML][HTML] Pregabalin as a pain therapeutic: beyond calcium channels

SRA Alles, SM Cain, TP Snutch - Frontiers in Cellular Neuroscience, 2020 - frontiersin.org
… of both gabapentinoid actions and the distinct roles of specific calcium channel subtypes
in … notion that the main therapeutic action of these drugs involves reducing calcium-mediated …

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… that the observed responses with pregabalin may result from activity at the …

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
… site of action for pregabalin, we also explored whether pregabalin had any effects on
excitation–contraction coupling. The dihydropyridine receptor or calcium channel CaV1.1 protein is …

The mechanisms of action of gabapentin and pregabalin

GJ Sills - Current opinion in pharmacology, 2006 - Elsevier
… GBP was shown to reduce potassium-evoked calcium influx via voltage-gated calcium
channels in a mouse pituitary cell line that constitutively expresses GABA B receptors comprising …

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

JA Micó, R Prieto - CNS drugs, 2012 - Springer
… of action of pregabalin, a highly selective, high-affinity ligand of the P/Q type of voltage-gated
calcium channel (… hyperexcitability suggests that pregabalin reduces synaptic release of …

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's specificity (or unique mechanism of action) was inferred by measuring the
affinity of several central nervous system (CNS)-targeted therapeutic agents to the α 2 δ-1 and α …

Drugging the undruggable: gabapentin, pregabalin and the calcium channel α2δ subunit

J Offord, LL Isom - Critical reviews in biochemistry and molecular …, 2016 - Taylor & Francis
… The path to understanding the mechanisms of gabapentin and pregabalin action in epilepsy,
anxiety and neuropathic pain therapeutics has been a long one. Over time there have been …

Pregabalin modulation of neurotransmitter release is mediated by change in intrinsic activation/inactivation properties of Cav2. 1 calcium channels

MN Di Guilmi, FJ Urbano, CG Inchauspe… - Journal of Pharmacology …, 2011 - ASPET
calcium currents while minimizing its rundown. At the age period used in this work (postnatal
days 11 to 15), only P/Q type calcium channels … by blocking calcium channels during action