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Dopaminergic receptor sites in human brain

Positron emission tomography

From Service Hospitalier Frédéric Joliot (Drs. Baron, Comar, Crouzel, and Kellershohn), CEA, Département de Biologie, Orsay; Hôpital Sainte Anne (Drs. Zarifian, Loo, and Deniker), Service Hospitalo-universitaire de Santé Mentale et de Thérapeutique, Paris: and Hôpital La Salpéttrière (Dr. Agid), Service de Neurologie et de Neuropsychologie, Paris, France.

Positron emission tomography (PET) and ¹¹C-labeled pimozide were used to study the dopaminergic (DA) receptor sites in the human striatum by comparing the latter with the cerebellum, which lacks DA receptors. Although ¹¹C-pimozide concentration was not different in these two brain structures up to 53 minutes after IV injection (thus implying large nonspecific binding), a significant retention of radioactivity in striatum relative to cerebellum was found in controls but not in subjects pretreated with the unlabeled competitor haloperidol. This suggests that the striatal retention seen in controls was due to specific binding of ¹¹C-pimozide to DA receptor sites, whereas prior occupation of the receptor sites by the unlabeled competitor was achieved in pretreated subjects.

Address correspondence and reprint requests to Dr. Baron, Service Hospitalier Frédèric Joliot, Hôpital d'Orsay, CEA Départemente de Biologie, 91406 Orsay, France.

Supported by INSERM ATP SANTE Mentale et Cerveau No. PRC 120 082–120 006.

Accepted for publication April 13, 1984.

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