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Properties of Opiate-Receptor Binding in Rat Brain
Open accessAbstract
[ 3 H]Naloxone, a potent opiate antagonist, binds stereospecifically to opiate-receptor sites in rat-brain tissue. The binding is time, temperature, and pH dependent and saturable with respect to [ 3 H]naloxone and tissue concentration. The [ 3 H]naloxone-receptor complex formation is bimolecular with a dissociation constant of 20 nM. 15 Opiate agonists and antagonists compete for the same receptors, whose density is 30 pmol/g. Potencies of opiates and their antagonists in displacing [ 3 H]naloxone binding parallel their pharmacological potencies.
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Cited by
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Cuatrecasas, P., & Hollenberg, M. D. (1976) · Advances in Protein Chemistry · doi:10.1016/s0065-3233(08)60481-7 · Cited by 478
Herkenham, M., & Pert, C. (1982) · The Journal of Neuroscience · doi:10.1523/jneurosci.02-08-01129.1982 · Cited by 465
Self-citationOpioid Therapy and Immunosuppression: A Review
Vallejo, R., de Leon-Casasola, O., & Benyamin, R. (2004) · American Journal of Therapeutics · doi:10.1097/01.mjt.0000132250.95650.85 · Cited by 386
Structural insights into G-protein-coupled receptor allostery
Thal, D. M., Glukhova, A., Sexton, P. M., & Christopoulos, A. (2018) · Nature · doi:10.1038/s41586-018-0259-z · Cited by 319
Bennett, J. P., & Snyder, S. H. (1975) · Brain Research · doi:10.1016/0006-8993(75)90234-6 · Cited by 165
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Metadata
- Authors
- Pert, C. B., & Snyder, S. H.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 1973-08
- Volume
- 70
- Issue
- 8
- Pages
- 2243-2247
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2000125000
- Cited by
- 438
- References
- 0
- FWCI
- 9.16
- Type
- journal article
- Language
- en
- Open access
- green
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