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Quantitative Analysis of D2 Dopamine Receptor Binding in the Living Human Brain by PET
Abstract
D2 dopamine receptors in the putamen of living human subjects were characterized by using the selective, high-affinity D2 dopamine receptor antagonist carbon-11-labeled raclopride and positron emission tomography. Experiments in four healthy men demonstrated saturability of [ 11 C]raclopride binding to an apparently homogeneous population of sites with Hill coefficients close to unity. In the normal putamen, maximum binding ranged from 12 to 17 picomoles per cubic centimeter and dissociation constants from 3.4 to 4.7 nanomolar. Maximum binding for human putamen at autopsy was 15 picomoles per cubic centimeter. Studies of [ 11 C]raclopride binding indicate that clinically effective doses of chemically distinct neuroleptic drugs result in 85 to 90 percent occupancy of D2 dopamine receptors in the putamen of schizophrenic patients.
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Citations
Cited by
Wang, G.-J., Volkow, N. D., Logan, J., Pappas, N. R., Wong, C. T., Zhu, W., Netusll, N., & Fowler, J. S. (2001) · The Lancet · doi:10.1016/s0140-6736(00)03643-6 · Cited by 1,864
The neuropsychology of schizophrenia
Gray, J. A., Feldon, J., Rawlins, J. N. P., Hemsley, D. R., & Smith, A. D. (1991) · Behavioral and Brain Sciences · doi:10.1017/s0140525x00065055 · Cited by 1,350
Breier, A., Su, T.-P., Saunders, R., Carson, R. E., Kolachana, B. S., de Bartolomeis, A., Weinberger, D. R., Weisenfeld, N., Malhotra, A. K., Eckelman, W. C., et al. (1997) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.94.6.2569 · Cited by 1,154
Kapur, S., Zipursky, R., Jones, C., Remington, G., & Houle, S. (2000) · American Journal of Psychiatry · doi:10.1176/appi.ajp.157.4.514 · Cited by 1,090
Decreases in dopamine receptors but not in dopamine transporters in alcoholics
Volkow, N. D., Wang, G., Fowler, J. S., Logan, J., Hitzemann, R., Ding, Y., Pappas, N., Shea, C., & Piscani, K. (1996) · Alcoholism: Clinical and Experimental Research · doi:10.1111/j.1530-0277.1996.tb05936.x · Cited by 612
Metadata
- Authors
- Farde, L., Hall, H., Ehrin, E., & Sedvall, G.
- Venue
- Science
- Published
- 1986-01-17
- Volume
- 231
- Issue
- 4735
- Pages
- 258-261
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2066735646
- Cited by
- 831
- References
- 0
- FWCI
- 19.95
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: Quantitative Analysis of D2 Dopamine Receptor Binding in the Living Human Brain by PET. https://app.cochat.ai/papers/10.1126/science.2867601
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- Farde, L., Hall, H., Ehrin, E., & Sedvall, G. (1986). Quantitative Analysis of D2 Dopamine Receptor Binding in the Living Human Brain by PET. Science. https://doi.org/10.1126/science.2867601
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
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.
