A PET-study of [11C]FLB 457 binding to extrastriatal D2-dopamine receptors in healthy subjects and antipsychotic drug-treated patients |
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Authors: | L Farde Tetsuya Suhara Svante Nyberg P Karlsson Yoshifumi Nakashima Jarmo Hietala Christer Halldin |
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Institution: | (1) Psychiatry Section, The Department of Clinical Neuroscience, Karolinska Institutet, S-17176 Stockholm, Sweden Fax (+46)8/34 65 63, e-mail: larsf@psyk.ks.se, SE;(2) The Department of Pharmacology, Turku University, Turku, Finland, FI |
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Abstract: | We recently developed 11C]FLB 457 a substituted benzamide with the very high affinity of 20 pM for D2-dopamine receptors in vitro. The aim of the present exploratory study was to examine the anatomical distribution of 11C]FLB 457 binding in the human brain and to determine extrastriatal D2-receptor occupancy in antipsychotic drug-treated patients. 11C]raclopride was used to obtain reference values for D2-dopamine receptor occupancy in the putamen. After IV injection of 11C]FLB 457 there was a high concentration of radioactivity, not only in the caudate putamen but also in the thalamus and the
temporal cortex. The concentration of radioactivity in the frontal cortex, the substantia nigra and the colliculi was slightly
higher than in the cerebellum. Pretreatment with haloperidol and fluphenazine indicated that 11C]FLB 457 binding in extrastriatal regions to a high degree represents specific binding to D2-dopamine receptors. The D2-occupancy in antipsychotic drug-treated patients was on the same level in the thalamus and the temporal cortex as that determined
with 11C]raclopride in the putamen. The study shows that 11C]FLB 457 has potential for quantitative PET-examination of D2-dopamine receptors in man.
Received: 24 March 1997 /Final version: 5 May 1997 |
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Keywords: | [11C]FLB 457 D2-dopamine receptors Human Positron emission tomography Neuroleptic drug |
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