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Science 17 January 1986:
Vol. 231. no. 4735, pp. 258 - 261
DOI: 10.1126/science.2867601
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Articles

Science, Vol 231, Issue 4735, 258-261
Copyright © 1986 by American Association for the Advancement of Science

articles

Quantitative analysis of D2 dopamine receptor binding in the living human brain by PET

L Farde, H Hall, E Ehrin, and G Sedvall

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 [11C]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 [11C]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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Science. ISSN 0036-8075 (print), 1095-9203 (online)