The DOI matches its Crossref record; 18 of the 18 references it cites were found in a registry or an index.
CHARACTERIZATION OF THE k‐SUBTYPE OF THE OPIATE RECEPTOR IN THE GUINEA‐PIG BRAIN
Open accessAbstract
In homogenates of guinea‐pig brain, the characteristics of the binding of [3 H]‐ethylketazocine, an agonist for the putative k‐receptor, were determined by estimation of the affinity and capacity of binding, by competitive inhibition for the binding site by unlabelled ligands and by selective protection of the binding site from alkylation by phenoxybenzamine. At 25°C the maximum number of binding sites for [3 H]‐ethylketazocine was about 14pmol/g fresh brain, of which about 50% were high affinity sites. In competition experiments, the high affinity binding of [3 H]‐ethylketazocine to the k‐binding site was readily displaced by several k‐agonists but not by the selective μ‐ligand, D‐Ala 2, MePhe 4, Glyol 5‐enkephalin or the selective δ‐ligand, D‐Ala 2, D‐Leu 5‐enkephalin. In contrast, the k‐agonists tested so far exhibit a high degree of cross‐reactivity with the μ‐binding site but somewhat less with the δ‐binding site. Similar specificities were observed in protection experiments. The approximate proportions of the three subtypes of opiate receptor in the guinea‐pig brain are 25% μ‐binding sites, 45% δ‐binding sites and 30% k‐binding sites. The endogenous opioids, Met‐enkephalin, Leu‐enkephalin and porcine β‐endorphin have only a low affinity for the k‐binding site.
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Self-citationThe possible effects of the aggregation of the molecules of haemoglobin on its dissociation curves
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Self-citationBremazocine: A potent, long-acting opiate kappa-agonist
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Salvinorin A: A potent naturally occurring nonnitrogenous κ opioid selective agonist
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75 years of opioid research: the exciting but vain quest for the Holy Grail
Corbett, A. D., Henderson, G., McKnight, A. T., & Paterson, S. J. (2006) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0706435 · Cited by 358
Self-citation30 years of dynorphins — New insights on their functions in neuropsychiatric diseases
Schwarzer, C. (2009) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2009.05.006 · Cited by 289
Species differences in the concentrations and distributions of opioid binding sites
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Self-citationOpiate antagonists enhance the working memory of rats in the radial maze
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Metadata
- Authors
- KOSTERLITZ, H. W., PATERSON, S. J., & ROBSON, L. E.
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 1981-08
- Volume
- 73
- Issue
- 4
- Pages
- 939-949
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- OpenAlex
- W1996997570
- Cited by
- 422
- References
- 18
- FWCI
- 16.95
- Type
- journal article
- Language
- en
- Open access
- bronze
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- KOSTERLITZ, H. W., PATERSON, S. J., & ROBSON, L. E. (1981). CHARACTERIZATION OF THE k‐SUBTYPE OF THE OPIATE RECEPTOR IN THE GUINEA‐PIG BRAIN. British Journal of Pharmacology. https://doi.org/10.1111/j.1476-5381.1981.tb08749.x
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