Regional specific binding of (/sup 11/C)RO 15 1788 to central type benzodiazepine receptors in human brain: quantitative evaluation by PET

Journal Article · Wed Jun 01 04:00:00 EDT 1988 · J. Cereb. Blood Flow Metab.; (United States)

DOI:https://doi.org/10.1038/jcbfm.1988.65· OSTI ID:6938464

Pappata, S; Samson, Y; Chavoix, C; Prenant, C; Maziere, M; Baron, J C

The central type benzodiazepine receptors were studied in 17 healthy human subjects with /sup 11/C-RO 15 1788 and positron emission tomography (PET). The brain regional distribution of the tracer in eight control studies performed after injection of trace doses of /sup 11/C-RO 15 1788 was consistent with that of benzodiazepine receptors. Saturation studies with co-injected cold RO 15 1788 in the remaining subjects showed a dose-dependent decrease of brain radiotracer until full inhibition of specific binding was achieved with doses above 0.1 mg/kg (four studies). Based on the results, a simple method to estimate the specifically bound /sup 11/C-RO 15 1788 regionally in a single PET study is proposed, using the data from the full-saturation studies as a stable estimate of the nondisplaceable radioligand concentration. Using this method, it was found that quasiequilibrium between the estimated specifically bound and nondisplaceable components was achieved at times equal to or longer than 20 min after tracer administration. The validity of this method was partly supported by further results, showing a good agreement between the regional specific binding so calculated and postmortem data of receptor density.

• Research Organization: Commissariat a l'Energie Atomique, Orsay (France)
• OSTI ID: 6938464
• Journal Information: J. Cereb. Blood Flow Metab.; (United States), Journal Name: J. Cereb. Blood Flow Metab.; (United States) Vol. 8:3; ISSN JCBMD
• Country of Publication: United States
• Language: English

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