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Cited by 1,181

The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.

The Novel Anticonvulsant Drug, Gabapentin (Neurontin), Binds to the α2δ Subunit of a Calcium Channel

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Gee, Nicolas S., Brown, Jason P., Dissanayake, Visaka U.K., Offord, James, Thurlow, Richard, Woodruff, Geoffrey N.·1996·Journal of Biological Chemistry
DOI 10.1074/jbc.271.10.5768
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Abstract

Gabapentin (1-(aminomethyl)cyclohexane acetic acid; Neurontin) is a novel anticonvulsant drug, with a mechanism of action apparently dissimilar to that of other antiepileptic agents. We report here the isolation and characterization of a [3H]gabapentin-binding protein from pig cerebral cortex membranes. The detergent-solubilized binding protein was purified 1022-fold, in a six-step column-chromatographic procedure, with a yield of 3.9%. The purified protein had an apparent subunit Mr of 130,000, and was heavily glycosylated. The partial N-terminal amino acid sequence of the Mr 130,000 polypeptide, EPFPSAVTIK, was identical to that reported for the alpha2delta subunit of the L-type Ca2+ channel from rabbit skeletal muscle (Hamilton, S. L., Hawkes, M. J., Brush, K., Cook, R., Chang, R. J., and Smilowitz, H. M. (1989) Biochemistry 28, 7820-7828). High levels of [3H]gabapentin binding sites were found in membranes prepared from rat brain, heart and skeletal muscle. Binding of [3H]gabapentin to COS-7 cells transfected with alpha2delta cDNA was elevated >10-fold over controls, consistent with the expression of alpha2 delta protein, as measured by Western blotting. Finally, purified L-type Ca2+ channel complexes were fractionated, under dissociating conditions, on an ion-exchange column; [3H]gabapentin binding activity closely followed the elution of the alpha2 delta subunit. [3H]Gabapentin is the first pharmacological agent described that interacts with an alpha2delta subunit of a voltage-dependent Ca2+ channel.

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Metadata

Authors
Gee, N. S., Brown, J. P., Dissanayake, V. U. K., Offord, J., Thurlow, R., & Woodruff, G. N.
Venue
Journal of Biological Chemistry
Publisher
Elsevier BV
Published
1996-03
Volume
271
Issue
10
Pages
5768-5776
ISSN
0021-9258 (ISSN-L)
DOI
10.1074/jbc.271.10.5768
OpenAlex
W2103289578
Cited by
1,181
References
2
FWCI
8.91
Type
journal article
Language
en
Open access
hybrid
Licence

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CoChat. (2026). Citation check: The Novel Anticonvulsant Drug, Gabapentin (Neurontin), Binds to the α2δ Subunit of a Calcium Channel. https://app.cochat.ai/papers/10.1074/jbc.271.10.5768
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Gee, N. S., Brown, J. P., Dissanayake, V. U. K., Offord, J., Thurlow, R., & Woodruff, G. N. (1996). The Novel Anticonvulsant Drug, Gabapentin (Neurontin), Binds to the α2δ Subunit of a Calcium Channel. Journal of Biological Chemistry. https://doi.org/10.1074/jbc.271.10.5768

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.