Literature DB >> 20571971

The alpha2-delta protein: an auxiliary subunit of voltage-dependent calcium channels as a recognized drug target.

Andrew J Thorpe1, James Offord.   

Abstract

Currently, there are two drugs on the market, gabapentin (Neurontin) and pregabalin (Lyrica), that are proposed to exert their therapeutic effect through binding to the alpha2-delta subunit of voltage-sensitive calcium channels. This activity was unexpected, as the alpha2-delta subunit had previously been considered not to be a pharmacological target. In this review, the role of the alpha2-delta subunits is discussed and the mechanism of action of the alpha2-delta ligands in vitro and in vivo is summarized. Finally, new insights into the mechanism of drugs that bind to this protein are discussed.

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Year:  2010        PMID： 20571971

Source DB:  PubMed          Journal:  Curr Opin Investig Drugs        ISSN： 1472-4472


  10 in total

1.  Pharmacological tests of hypotheses for acquired pendular nystagmus.

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Journal:  Ann N Y Acad Sci       Date:  2011-09       Impact factor: 5.691

2.  Methodology for rapid measures of glutamate release in rat brain slices using ceramic-based microelectrode arrays: basic characterization and drug pharmacology.

Authors:  Jorge E Quintero; François Pomerleau; Peter Huettl; Kirk W Johnson; James Offord; Greg A Gerhardt
Journal:  Brain Res       Date:  2011-05-18       Impact factor: 3.252

3.  Levetiracetam synergizes with gabapentin, pregabalin, duloxetine and selected antioxidants in a mouse diabetic painful neuropathy model.

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4.  Gabapentin and memantine increases randomness of oscillatory waveform in ocular palatal tremor.

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5.  Amperometric measurement of glutamate release modulation by gabapentin and pregabalin in rat neocortical slices: role of voltage-sensitive Ca2+ α2δ-1 subunit.

Authors:  Jorge E Quintero; David J Dooley; François Pomerleau; Peter Huettl; Greg A Gerhardt
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6.  The efficacy of pregabalin for prevention of catheter-related bladder discomfort: a prospective, randomized, placebo-controlled double-blind study.

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7.  Genomic aberrations of the CACNA2D1 gene in three patients with epilepsy and intellectual disability.

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8.  Synergistic interaction between trazodone and gabapentin in rodent models of neuropathic pain.

Authors:  Beatrice Garrone; Anna di Matteo; Alessandro Amato; Luana Pistillo; Lucia Durando; Claudio Milanese; Francesco Paolo Di Giorgio; Serena Tongiani
Journal:  PLoS One       Date:  2021-01-04       Impact factor: 3.240

9.  Catheter-Related Bladder Discomfort: How Can We Manage It?

Authors:  Eun Bi Jang; Seong Hwi Hong; Kyu Shik Kim; Sung Yul Park; Yong Tae Kim; Young Eun Yoon; Hong Sang Moon
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Authors:  Wanchat Theeranaew; Hyo-Jung Kim; Kenneth Loparo; Ji-Soo Kim; Aasef G Shaikh
Journal:  Cerebellum       Date:  2021-10       Impact factor: 3.847
  10 in total

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