Imaging of aromatase distribution in rat and rhesus monkey brains with [C-11]vorozole
2006 (English)In: Nuclear Medicine and Biology, ISSN 0969-8051, E-ISSN 1872-9614, Vol. 33, no 5, 599-605 p.Article in journal (Refereed) Published
Aromatase is an enzyme that converts androgens to estrogens and may play a role in mood and mental status. The aim of this study was to demonstrate that brain aromatase distribution could be evaluated with a novel positron emission tomography (PET) tracer [C-11]vorozole. Vorozole is a nonsteroidal aromatase inhibitor that reversibly binds to the heme domain of aromatase. In vitro experiments in rat brain, using frozen section autoradiography, illustrated specific binding in the medial amygdala (MA), the bed nucleus of stria terminalis (BST) and the preoptic area (POA) of male rat brain. Specific binding in female rat brain was found in the MA and the BST; however, the signals were lower than those of males. The K-d of [C-11]vorozole binding to aromatase in MA was determined to be 0.60 +/- 0.06 nM by Scatchard plot analysis using homogenates. An in vivo PET study in female rhesus monkey brain demonstrated the uptake of [C-11]vorozole in the amygdala, where the uptake was blocked by the presence of excess amounts of unlabeled vorozole. Thus, this tracer has a high affinity for brain aromatase and could have a potential for in vivo aromatase imaging. This technique might enable the investigation of human brain aromatase in healthy and diseased persons.
Place, publisher, year, edition, pages
2006. Vol. 33, no 5, 599-605 p.
positron emission tomography, aromatase, vorozole, Amygdala, hypothalamus, sex steroids
Medical and Health Sciences
IdentifiersURN: urn:nbn:se:uu:diva-97475DOI: 10.1016/j.nucmedbio.2006.03.009ISI: 000239530200003PubMedID: 16843834OAI: oai:DiVA.org:uu-97475DiVA: diva2:172442