Ca super(2+) channel alpha sub(2) delta ligands: novel modulators of neurotransmission

The term Ca2+ channel 2 ligands has recently been applied to an evolving drug class that includes gabapentin (Neurontin) and pregabalin (Lyrica), and reflects significant progress over the past decade in elucidating the mechanism of action of these drugs: a novel, specific action at one of the subun...

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Veröffentlicht in:Trends in pharmacological sciences (Regular ed.) 2007-02, Vol.28 (2), p.75-82
Hauptverfasser: Dooley, David J, Taylor, Charles P, Donevan, Sean, Feltner, Douglas
Format: Artikel
Sprache:eng
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Zusammenfassung:The term Ca2+ channel 2 ligands has recently been applied to an evolving drug class that includes gabapentin (Neurontin) and pregabalin (Lyrica), and reflects significant progress over the past decade in elucidating the mechanism of action of these drugs: a novel, specific action at one of the subunits constituting voltage-sensitive Ca2+ channels. Binding of these ligands to the 2 subunit is considered to explain their usefulness in treating several clinical disorders, including epilepsy, pain from diabetic neuropathy, postherpetic neuralgia and fibromyalgia, and generalized anxiety disorder. The evidence indicates a relationship between 2 subunit binding and the modulation of processes that subserve neurotransmission. This modulation is characterized by a reduction of the excessive neurotransmitter release that is observed in certain neurological and psychiatric disorders.
ISSN:0165-6147
DOI:10.1016/j.tips.2006.12.006