Ca2+ channel alpha2delta ligands: novel modulators of neurotransmission.
The term 'Ca2+ channel alpha2delta 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 alpha2delta 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 alpha2delta 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.
Dooley
David J
DJ
Department of CNS Pharmacology, Pfizer Global Research and Development, Ann Arbor, MI 48105, USA. david.dooley@pfizer.com
Taylor
Charles P
CP
Donevan
Sean
S
Feltner
Douglas
D
D000818:Animals; D001665:Binding Sites; D015220:Calcium Channels / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D008024:Ligands; D009435:Synaptic Transmission / Q000187:drug effects*
D015220:Calcium Channels; D008024:Ligands; C494035:voltage gated calcium channel subunit Ca alpha2delta-1, human