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Opiate Agonists and Antagonists Discriminated by Receptor Binding in Brain
Abstract
Receptor binding of opiate agonists and antagonists can be differentiated in vivo and in vitro. Administration of either rapidly elevates stereospecific [ 3 H]dihydromorphine binding to mouse brain extracts by 40 to 100 percent, but antagonists are 10 to 1000 times more potent than agonists; as little as 0.02 milligram of naloxone per kilogram of body weight significantly enhances opiate receptor binding. Sodium enhances antagonist binding in vitro but decreases agonist binding, a qualitative difference that may be relevant to the divergent pharmacological properties of opiate agonists and antagonists.
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Citations
Cited by
Mu Opioids and Their Receptors: Evolution of a Concept
Pasternak, G. W., & Pan, Y.-X. (2013) · Pharmacological Reviews · doi:10.1124/pr.112.007138 · Cited by 578
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Wacker, D., Stevens, R. C., & Roth, B. L. (2017) · Cell · doi:10.1016/j.cell.2017.07.009 · Cited by 560
Allosteric sodium in class A GPCR signaling
Katritch, V., Fenalti, G., Abola, E. E., Roth, B. L., Cherezov, V., & Stevens, R. C. (2014) · Trends in Biochemical Sciences · doi:10.1016/j.tibs.2014.03.002 · Cited by 511
C fragment of lipotropin has a high affinity for brain opiate receptors
BRADBURY, A. F., SMYTH, D. G., SNELL, C. R., BIRDSALL, N. J. M., & HULME, E. C. (1976) · Nature · doi:10.1038/260793a0 · Cited by 489
Membrane Receptors and Hormone Action
Cuatrecasas, P., & Hollenberg, M. D. (1976) · Advances in Protein Chemistry · doi:10.1016/s0065-3233(08)60481-7 · Cited by 478
Metadata
- Authors
- Pert, C. B., Pasternak, G., & Snyder, S. H.
- Venue
- Science
- Published
- 1973-12-28
- Volume
- 182
- Issue
- 4119
- Pages
- 1359-1361
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W1979569718
- Cited by
- 546
- References
- 0
- FWCI
- 9.82
- Type
- journal article
- Language
- en
- Open access
- closed
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- Pert, C. B., Pasternak, G., & Snyder, S. H. (1973). Opiate Agonists and Antagonists Discriminated by Receptor Binding in Brain. Science. https://doi.org/10.1126/science.182.4119.1359
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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.
