Abstract
In this review we describe the genes encoding α2δ subunits, their topology and predicted structure. We then review the electrophysiological effects of α2δ subunits. It is clear from most studies that α2δ subunits increase channel density at the plasma membrane, but there is less agreement between studies and between channel subtypes concerning the effects of α2δ subunits on voltage-dependence of activation and inactivation. Most studies agree that α2δ subunits increase the kinetics of inactivation, for a number of different calcium channel subtypes. We also discuss the link between α2δ subunits and disease, particularly in terms of Ducky, the spontaneously occurring mutant mouse strain that has mutations in α2δ-2, and exhibits cerebellar ataxia and absence epilepsy. Finally, we will examine the evidence that α2δ subunits are the site of action of the anti-epileptic, anti-nociceptive drug gabapentin.
Keywords: voltage-dependence, ducky, cerebellar ataxia, epilepsy, anti-epileptic
Current Neuropharmacology
Title: Calcium Channel α2δ Subunits: Structure, Functions and Target Site for Drugs
Volume: 1 Issue: 3
Author(s): Carles Canti, Anthony Davies and Annette C. Dolphin
Affiliation:
Keywords: voltage-dependence, ducky, cerebellar ataxia, epilepsy, anti-epileptic
Abstract: In this review we describe the genes encoding α2δ subunits, their topology and predicted structure. We then review the electrophysiological effects of α2δ subunits. It is clear from most studies that α2δ subunits increase channel density at the plasma membrane, but there is less agreement between studies and between channel subtypes concerning the effects of α2δ subunits on voltage-dependence of activation and inactivation. Most studies agree that α2δ subunits increase the kinetics of inactivation, for a number of different calcium channel subtypes. We also discuss the link between α2δ subunits and disease, particularly in terms of Ducky, the spontaneously occurring mutant mouse strain that has mutations in α2δ-2, and exhibits cerebellar ataxia and absence epilepsy. Finally, we will examine the evidence that α2δ subunits are the site of action of the anti-epileptic, anti-nociceptive drug gabapentin.
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Cite this article as:
Canti Carles, Davies Anthony and Dolphin C. Annette, Calcium Channel α2δ Subunits: Structure, Functions and Target Site for Drugs, Current Neuropharmacology 2003; 1 (3) . https://dx.doi.org/10.2174/1570159033477116
DOI https://dx.doi.org/10.2174/1570159033477116 |
Print ISSN 1570-159X |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6190 |
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