The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Evidence for a Common Binding Cavity for Three General Anesthetics within the GABAAReceptor
Open accessAbstract
The GABA(A) receptor is an important target for a variety of general anesthetics (Franks and Lieb, 1994) and for benzodiazepines such as diazepam. Specific point mutations in the GABA(A) receptor selectively abolish regulation by benzodiazepines (Rudolph et al., 1999; McKernan et al., 2000) and by anesthetic ethers (Mihic et al., 1997; Krasowski et al., 1998; Koltchine et al., 1999), suggesting the existence of discrete binding sites on the GABA(A) receptor for these drugs. Using anesthetics of different molecular size (isoflurane > halothane > chloroform) together with complementary mutagenesis of specific amino acid side chains, we estimate the volume of a proposed anesthetic binding site as between 250 and 370 A(3). The results of the "cutoff" analysis suggest a common site of action for the anesthetics isoflurane, halothane, and chloroform on the GABA(A) receptor. Moreover, the data support a crucial role for Leu232, Ser270, and Ala291 in the alpha subunit in defining the boundaries of an amphipathic cavity, which can accommodate a variety of small general anesthetic molecules.
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Cites
Whittington, M. A., Traub, R. D., & Jefferys, J. G. R. (1995) · Nature · doi:10.1038/373612a0 · Cited by 1,613
Gamma (40-100 Hz) oscillation in the hippocampus of the behaving rat
Bragin, A., Jando, G., Nadasdy, Z., Hetke, J., Wise, K., & Buzsaki, G. (1995) · The Journal of Neuroscience · doi:10.1523/jneurosci.15-01-00047.1995 · Cited by 1,527
Sites of alcohol and volatile anaesthetic action on GABAA and glycine receptors
Mihic, S. J., Ye, Q., Wick, M. J., Koltchine, V. V., Krasowski, M. D., Finn, S. E., Mascia, M. P., Valenzuela, C. F., Hanson, K. K., Greenblatt, E. P., et al. (1997) · Nature · doi:10.1038/38738 · Cited by 1,219
Self-citation
Cited by
General anaesthesia: from molecular targets to neuronal pathways of sleep and arousal
Franks, N. P. (2008) · Nature Reviews Neuroscience · doi:10.1038/nrn2372 · Cited by 1,295
Jurd, R., Arrasa, M., Lambert, S., Drexler, B., Siegwart, R., Crestani, F., Zaugg, M., Vogt, K. E., Ledermann, B., Antkowiak, B., et al. (2003) · The FASEB Journal · doi:10.1096/fj.02-0611fje · Cited by 558
Emerging molecular mechanisms of general anesthetic action
Hemmings, H. C., Akabas, M. H., Goldstein, P. A., Trudell, J. R., Orser, B. A., & Harrison, N. L. (2005) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2005.08.006 · Cited by 552
Self-citationDrug interactions at GABAA receptors
Korpi, E. R., Gründer, G., & Lüddens, H. (2002) · Progress in Neurobiology · doi:10.1016/s0301-0082(02)00013-8 · Cited by 473
Towards a comprehensive understanding of anesthetic mechanisms of action: a decade of discovery
Hemmings, H. C., Riegelhaupt, P. M., Kelz, M. B., Solt, K., Eckenhoff, R. G., Orser, B. A., & Goldstein, P. A. (2019) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2019.05.001 · Cited by 244
Metadata
- Authors
- Jenkins, A., Greenblatt, E. P., Faulkner, H. J., Bertaccini, E., Light, A., Lin, A., Andreasen, A., Viner, A., Trudell, J. R., & Harrison, N. L.
- Venue
- The Journal of Neuroscience
- Publisher
- Society for Neuroscience
- Published
- 2001-03-15
- Volume
- 21
- Issue
- 6
- Pages
- RC136-RC136
- ISSN
- 0270-6474 (ISSN-L)
- 1529-2401
- OpenAlex
- W1840025613
- Cited by
- 244
- References
- 3
- FWCI
- 6.50
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Jenkins, A., Greenblatt, E. P., Faulkner, H. J., Bertaccini, E., Light, A., Lin, A., Andreasen, A., Viner, A., Trudell, J. R., & Harrison, N. L. (2001). Evidence for a Common Binding Cavity for Three General Anesthetics within the GABAAReceptor. The Journal of Neuroscience. https://doi.org/10.1523/jneurosci.21-06-j0002.2001
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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