The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
Psychotomimetic opiate receptors labeled and visualized with (+)-[3H]3-(3-hydroxyphenyl)-N-(1-propyl)piperidine.
Open accessAbstract
3-(3-Hydroxyphenyl)-N-(1-propyl)piperidine (3-PPP) has been proposed as a selective dopamine autoreceptor agonist in the central nervous system. This report describes the pharmacology and localization of specific high-affinity binding sites for (+)-[3H]3-PPP in brain. The drug specificity of (+)-[3H]3-PPP binding is identical to that of sigma receptors, which may mediate psychotomimetic effects of some opiates. Haloperidol and the opioid derivatives, pentazocine, cyclazocine, and SKF 10,047 are potent inhibitors of (+)-[3H]3-PPP binding. Stereoselectivity is exhibited for the (+) isomers of cyclazocine and SKF 10,047 at the sigma site, opposite to the stereoselectivity seen at mu, delta, and kappa opiate receptors. (+)-[3H]3-PPP does not label dopamine receptors, as potent dopamine agonists and antagonists are weak inhibitors of binding and the localization of specific (+)-[3H]3-PPP binding sites does not parallel that of dopamine neurons. Discrete localizations of (+)-[3H]3-PPP binding sites in many brain areas including limbic, midbrain, brainstem, and cerebellar regions may explain psychotomimetic actions of opiates and behavioral effects of 3-PPP.
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Cites
Yung-Chi, C., & Prusoff, W. H. (1973) · Biochemical Pharmacology · doi:10.1016/0006-2952(73)90196-2 · Cited by 12,922
Martin, W. R., Eades, C. G., Thompson, J. A., Huppler, R. E., & Gilbert, P. E. (1976) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)30536-7 · Cited by 2,992
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Wong, E. H. F., Knight, A. R., & Woodruff, G. N. (1988) · Journal of Neurochemistry · doi:10.1111/j.1471-4159.1988.tb13260.x · Cited by 454
Gundlach, A., Largent, B., & Snyder, S. (1986) · The Journal of Neuroscience · doi:10.1523/jneurosci.06-06-01757.1986 · Cited by 393
Self-citationHellewell, S. B., Bruce, A., Feinstein, G., Orringer, J., Williams, W., & Bowen, W. D. (1994) · European Journal of Pharmacology: Molecular Pharmacology · doi:10.1016/0922-4106(94)90115-5 · Cited by 390
Hellewell, S. B., & Bowen, W. D. (1990) · Brain Research · doi:10.1016/0006-8993(90)91143-5 · Cited by 341
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Hayashi, T., & Su, T.-P. (2001) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.98.2.491 · Cited by 329
Metadata
- Authors
- Largent, B. L., Gundlach, A. L., & Snyder, S. H.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 1984-08
- Volume
- 81
- Issue
- 15
- Pages
- 4983-4987
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2008670721
- Cited by
- 196
- References
- 2
- FWCI
- 5.45
- Type
- journal article
- Language
- en
- Open access
- green
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- Largent, B. L., Gundlach, A. L., & Snyder, S. H. (1984). Psychotomimetic opiate receptors labeled and visualized with (+)-[3H]3-(3-hydroxyphenyl)-N-(1-propyl)piperidine. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.81.15.4983
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