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Stereospecific Binding of the Potent Narcotic Analgesic [ 3 H]Etorphine to Rat-Brain Homogenate
Open accessAbstract
Etorphine, the most potent narcotic analgesic known, was labeled with tritium by catalytic exchange. This drug exhibits stereospecific, saturable binding to rat-brain homogenate. At saturation, the stereospecific binding is 0.1-0.15 pmol/mg of protein. Specific binding is inhibited high salt concentrations, sulfhydryl reagents, and proteolytic enzymes, but is unaffected by phospholipases A and C, sodium azide, sodium fluoride, and prostaglandins E 1 and E 2 . Competition for binding of [ 3 H]etorphine correlates with agonist and antagonist potencies. The stable, stereospecific binding of an active narcotic analgesic supports the existence of opiate receptors.
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Cited by
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Lord, J. A. H., Waterfield, A. A., Hughes, J., & Kosterlitz, H. W. (1977) · Nature · doi:10.1038/267495a0 · Cited by 2,485
Prolactin: structure, function, and regulation of secretion
Freeman, M. E., Kanyicska, B., Lerant, A., & Nagy, G. (2000) · Physiological Reviews · doi:10.1152/physrev.2000.80.4.1523 · Cited by 2,457
Benzodiazepine receptors in rat brain
SQUIRES, R. F., & BRAESTRUP, C. (1977) · Nature · doi:10.1038/266732a0 · Cited by 1,449
A perceptual-defensive-recuperative model of fear and pain
Bolles, R. C., & Fanselow, M. S. (1980) · Behavioral and Brain Sciences · doi:10.1017/s0140525x0000491x · Cited by 832
Waldhoer, M., Bartlett, S. E., & Whistler, J. L. (2004) · Annual Review of Biochemistry · doi:10.1146/annurev.biochem.73.011303.073940 · Cited by 740
Metadata
- Authors
- Simon, E. J., Hiller, J. M., & Edelman, I.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 1973-07
- Volume
- 70
- Issue
- 7
- Pages
- 1947-1949
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W1984414350
- Cited by
- 1,067
- References
- 0
- FWCI
- 11.94
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: Stereospecific Binding of the Potent Narcotic Analgesic [ 3 H]Etorphine to Rat-Brain Homogenate. https://app.cochat.ai/papers/10.1073/pnas.70.7.1947
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- Simon, E. J., Hiller, J. M., & Edelman, I. (1973). Stereospecific Binding of the Potent Narcotic Analgesic [ 3 H]Etorphine to Rat-Brain Homogenate. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.70.7.1947
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