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 …
subunits are illustrated by a schematic diagram of a single calcium channel, including the four …
Mechanisms of analgesia by gabapentin and pregabalin–calcium 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 …
is … 10–30min) action of gabapentin and pregabalin to decrease calcium influx and transmitter …
[HTML][HTML] Pregabalin as a pain therapeutic: beyond calcium channels
… 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 …
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 …
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 …
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 …
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 …
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 …
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 …
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 …
days 11 to 15), only P/Q type calcium channels … by blocking calcium channels during action …
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