Variability in D2‐dopamine receptor density and affinity: A PET study with [11C]raclopride in man
Abstract
The variability of D 2‐dopamine receptor binding parameters in man was determined using Positron Emission Tomography (PET) and [11 C]raclopride. A saturation analysis based on five PET‐experiments was performed in each of ten men and ten women. The mean density of D 2‐dopamine receptors (B max) was 28 ± 6.9 pmol/ml (mean ± S.D.) and the apparent affinity (K dapp)9.1 ± 1.9 pmol/ml. The Hill coefficient was in all subjects close to unity (n H: 0.999 ± 0.020), thereby indicating binding to a homogeneous class of receptors. No significant differences between males and females were found in B max or K dapp. The interindividual difference in B max was statistically significant (α = 0.01). The difference in K dapp was not significant. Upregulation of the receptor density (B max) has been widely discussed as a mechanism for increased dopaminergic neurotransmission in schizophrenia. This study indicates that receptor density varies considerably in a group of healthy subjects. © 1995 Wiley‐Liss, Inc.
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The relationship between wrist temperature and extrapyramidal disease is likely modulated by the high degree of inter-individual variability in dopamine D2 receptor density, which, with its role in central thermoregulation, may lead to the high association of wrist temperature for susceptibility to extrapyramidal disease.
“This relationship is likely modulated by the high degree of inter-individual variability in dopamine D2 receptor density37, which, with its role in central thermoregulation, may lead to the high association of wrist temperature for susceptibility to extrapyramidal disease.”
From Diurnal rhythms of wrist temperature are associated with future disease risk in the UK Biobank (2023) · cites this paper as [37]
Cites
THE ATTRACTIONS OF PROTEINS FOR SMALL MOLECULES AND IONS
Scatchard, G. (1949) · Annals of the New York Academy of Sciences · doi:10.1111/j.1749-6632.1949.tb27297.x · Cited by 19,724 · see citing works
LIGAND: A versatile computerized approach for characterization of ligand-binding systems
Munson, P. J., & Rodbard, D. (1980) · Analytical Biochemistry · doi:10.1016/0003-2697(80)90515-1 · Cited by 8,494 · see citing works
Sokoloff, P., Bruno Giros, A., Martres, M., Bouthenet, M.-L., & Schwartz, J. (1990) · Nature · doi:10.1038/347146a0 · Cited by 2,608 · see citing works
Quantitative Analysis of D2 Dopamine Receptor Binding in the Living Human Brain by PET
Farde, L., Hall, H., Ehrin, E., & Sedvall, G. (1986) · Science · doi:10.1126/science.2867601 · Cited by 831 · see citing works
Self-citationImaging Dopamine Receptors in the Human Brain by Positron Tomography
Wagner, H. N., Burns, H. D., Dannals, R. F., Wong, D. F., Långström, B., Duelfer, T., Frost, J. J., Ravert, H. T., Links, J. M., Rosenbloom, S. B., et al. (1983) · Science · doi:10.1126/science.6604315 · Cited by 741 · see citing works
Wong, D. F., Wagner, H. N., Dannals, R. F., Links, J. M., Frost, J. J., Ravert, H. T., Wilson, A. A., Rosenbaum, A. E., GJEDDE, A. H., Douglass, K. H., et al. (1984) · Science · doi:10.1126/science.6334363 · Cited by 700 · see citing works
Alternative splicing directs the expression of two D2 dopamine receptor isoforms
Bruno Giros, A., Sokoloff, P., Martres, M., Riou, J., Emorine, L. J., & Schwartz, J.-C. (1989) · Nature · doi:10.1038/342923a0 · Cited by 685 · see citing works
Lévesque, D., Díaz, J., Pilon, C., Martres, M., Bruno Giros, A., Souil, E., Schott, D., Morgat, J. L., Schwartz, J., & Sokoloff, P. (1992) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.89.17.8155 · Cited by 674 · see citing works
Wienhard, K., Dahlbom, M. L., Eriksson, L., Michel, C. J., Bruckbauer, T., Pietrzyk, U., & Heiss, W. (1994) · Journal of Computer Assisted Tomography · doi:10.1097/00004728-199401000-00023 · Cited by 561 · see citing works
D2 Dopamine Receptors in Neuroleptic-Naive Schizophrenic Patients
Farde, L. (1990) · Archives of General Psychiatry · doi:10.1001/archpsyc.1990.01810150013003 · Cited by 529 · see citing works
Self-citationThe significance of dopamine-receptor blockade for the mechanism of action of neuroleptic drugs.
Jm, V. R. (1966) · PubMed · Cited by 508 · see citing works
Farde, L., Eriksson, L. I., Blomquist, G., & Halldin, C. (1989) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1038/jcbfm.1989.98 · Cited by 448 · see citing works
Self-citationHill, A. V. (1910) · The Journal of Physiology · doi:10.1113/jphysiol.1910.sp001366 · Cited by 358 · see citing works
m, M. B., thius, J. B., Eriksson, L., Greitz, T. V. B., Ribbe, T., & Wid�n, L. (1981) · Journal of Computer Assisted Tomography · doi:10.1097/00004728-198102000-00027 · Cited by 315 · see citing works
Seeman, P. M., Guan, H. C., & Niznik, H. B. (1989) · Synapse · doi:10.1002/syn.890030113 · Cited by 294 · see citing works
No D2 Receptor Increase in PET Study of Schizophrenia
Farde, L. (1987) · Archives of General Psychiatry · doi:10.1001/archpsyc.1987.01800190091013 · Cited by 293 · see citing works
Self-citationQuantification of Neuroreceptors in the Living Human Brain. I. Irreversible Binding of Ligands
Wong, D. F., GJEDDE, A. H., & Wagner, H. N. (1986) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1038/jcbfm.1986.27 · Cited by 277 · see citing works
Malmberg, Å., Jackson, D. M., Eriksson, A., & Mohell, N. (1993) · Molecular Pharmacology · doi:10.1016/s0026-895x(25)13652-3 · Cited by 210 · see citing works
Farde, L., Pauli, S., Hall, H., Eriksson, L. I., Halldin, C., H�gberg, T., Nilsson, L., Sj�gren, I., & Stone‐Elander, S. (1988) · Psychopharmacology · doi:10.1007/bf00212840 · Cited by 200 · see citing works
Self-citationAntonini, A., Leenders, K. L., Reist, H. W., Thomann, R., Beer, H. ‐., & Locher, J. (1993) · Archives of Neurology · doi:10.1001/archneur.1993.00540050026010 · Cited by 186 · see citing works
Rinne, J. O., Hietala, J. A., Ruotsalainen, U., Säkö, E., Laihinen, A., Någren, K., Lehikoinen, P., Oikonen, V., & Syvälahti, E. K. G. (1993) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1038/jcbfm.1993.39 · Cited by 184 · see citing works
Reproducibility of repeated measures of carbon-11-raclopride binding in the human brain.
Volkow, N. D., Fowler, J. S., Wang, G., Dewey, S. L., Schlyer, D. J., MacGregor, R. R., Logan, J., Alexoff, D. L., Shea, C. E., & HITZEMANN, R. J. (1993) · PubMed · Cited by 178 · see citing works
Häfner, H., Behrens, S., Vry, J. D., & Gattaz, W. F. (1991) · Psychiatry Research · doi:10.1016/0165-1781(91)90038-q · Cited by 161 · see citing works
Human dopamine receptor subtypes?in vitro binding analysis using3H-SCH 23390 and3H-raclopride
Hall, H., Farde, L., & Sedvall, G. (1988) · Journal of Neural Transmission · doi:10.1007/bf01244618 · Cited by 149 · see citing works
Self-citationPerformance Study of the PC-384 Positron Camera System for Emission Tomography of the Brain
Litton, J.-E., Bergström, M., Eriksson, L. I., Böhm, C., Blomqvist, G., & Kesselberg, M. (1984) · Journal of Computer Assisted Tomography · doi:10.1097/00004728-198402000-00016 · Cited by 132 · see citing works
Young, L. T., Wong, D. F., Goldman, S., Minkin, E., Chen, C., Matsumura, K., Scheffel, U., & Wagner, H. N. (1991) · Synapse · doi:10.1002/syn.890090305 · Cited by 119 · see citing works
Cortés, R., Camps, M., Gueye, B., Probst, A., & Palacios, J. M. (1989) · Brain Research · doi:10.1016/0006-8993(89)90031-0 · Cited by 109 · see citing works
Roy, E. J., Buyer, D. R., & Licari, V. A. (1990) · Brain Research Bulletin · doi:10.1016/0361-9230(90)90064-7 · Cited by 79 · see citing works
Radioligand—receptor binding studies: what's wrong with the scatchard analysis?
Bürgisser, E. (1984) · Trends in Pharmacological Sciences · doi:10.1016/0165-6147(84)90396-1 · Cited by 71 · see citing works
Fernández‐Ruíz, J., Amor, J. C., & Ramos, J. A. (1989) · Brain Research · doi:10.1016/0006-8993(89)91266-3 · Cited by 70 · see citing works
Janowsky, A. J., Neve, K. A., Kinzie, J. M., Taylor, B., de Paulis, T., & Belknap, J. K. (1992) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)11150-6 · Cited by 68 · see citing works
Nordström, A., Farde, L., Pauli, S., Litton, J., & Halldin, C. (1992) · Human Psychopharmacology Clinical and Experimental · doi:10.1002/hup.470070302 · Cited by 66 · see citing works
Self-citationHalldin, C., Farde, L., Högberg, T., Hall, H., Ström, P., Ohlberger, A., & Solin, O. H. (1991) · International Journal of Radiation Applications and Instrumentation Part B Nuclear Medicine and Biology · doi:10.1016/0883-2897(91)90096-4 · Cited by 62 · see citing works
Self-citationSnyder, L., Roberts, J. L., & Sealfon, S. C. (1991) · Neuroscience Letters · doi:10.1016/0304-3940(91)90187-x · Cited by 41 · see citing works
The absolute density of neurotransmitter receptors in the brain
Seeman, P. M. (1987) · Journal of Pharmacological Methods · doi:10.1016/0160-5402(87)90048-9 · Cited by 30 · see citing works
Hall, H. (1992) · Pharmacology & Toxicology · doi:10.1111/j.1600-0773.1992.tb00519.x · Cited by 8 · see citing works
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Seeman, P., & Tallerico, T. (1999) · American Journal of Psychiatry · doi:10.1176/ajp.156.6.876 · Cited by 237 · see citing works
Hirvonen, M. M., Laakso, A., Någren, K., Rinne, J. O., Pohjalainen, T., & Hietala, J. (2009) · Synapse · doi:10.1002/syn.20672 · Cited by 176 · see citing works
Cárdenas, L., Houle, S., Kapur, S., & Busto, U. E. (2004) · Synapse · doi:10.1002/syn.10282 · Cited by 63 · see citing works
Diurnal rhythms of wrist temperature are associated with future disease risk in the UK Biobank
Brooks, T. G., Lahens, N. F., Grant, G. R., Sheline, Y. I., FitzGerald, G. A., & Skarke, C. (2023) · Nature Communications · doi:10.1038/s41467-023-40977-5 · Cited by 57 · see citing works
Mapping the amphetamine-evoked dopamine release in the brain of the Gottingen minipig
Lind, N. M., Olsen, A. K., Moustgaard, A., Jensen, S. B., Jakobsen, S., Hansen, A. K., Arnfred, S. M., Hemmingsen, R. P., Gjedde, A., & Cumming, P. (2005) · Brain Research Bulletin · doi:10.1016/j.brainresbull.2004.08.007 · Cited by 28 · see citing works
- Authors
- Farde, L., Hall, H., Pauli, S., & Halldin, C.
- Affiliations
- Karolinska University Hospital (SE)
- Venue
- Synapse
- Publisher
- Wiley
- Published
- 1995-07
- Volume
- 20
- Issue
- 3
- Pages
- 200-208
- ISSN
- 0887-4476 (ISSN-L)
- 1098-2396
- OpenAlex
- W2090291844
- Cited by
- 175
- References
- 36
- Citations by year
- 2026: 1 · 2025: 1 · 2024: 2 · 2023: 2 · 2022: 4 · 2021: 2 · 2020: 4 · 2019: 2 · 2018: 9 · 2017: 3 · 2016: 4 · 2015: 6 · 2014: 4 · 2013: 2 · 2012: 11
- FWCI
- 2.13
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Synapse (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Vetenskapsrådet
- National Institutes of Health (2r01mh041205-09a1)
- National Medical Research Council
- National Institute of Mental Health (MH41205-08)
- Topics
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Health Sciences › Medicine › Psychiatry and Mental health › Schizophrenia research and treatment
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Keywords
- dopamine D2 receptor, receptor density, receptor binding affinity, [11C]raclopride, interindividual variability, saturation analysis, Hill coefficient, sex differences, healthy volunteers, schizophrenia, receptor up-regulation
- MeSH terms
- Adult, Aging, Brain, Brain Chemistry, Female, Humans, Image Processing, Computer-Assisted, Male, Methylation, Salicylamides, Sex Characteristics, Tomography, Emission-Computed, Receptors, Dopamine D2, Dopamine Antagonists, Raclopride
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