Abstract

Background: Preclinical studies demonstrate that 17β-estradiol (E 2) increases serotonin-2A receptor (5-HT 2AR) density in rat frontal cortex. Methods: We investigated the impact of hormone replacement therapy on 5-HT 2AR binding potential (BP) using positron emission tomography and [ 18F]altanserin in five postmenopausal women. Subjects were imaged at baseline, following 8 to 14 weeks of transdermal E 2, 0.1 mg/d, and following 2 to 6 weeks of E 2 plus micronized progesterone (P) 100 mg per os twice daily. Regional BPs in the anterior cingulate cortex, dorsolateral prefrontal cortex, and lateral orbitofrontal cortex were calculated by Logan analysis. Results: There was a main effect of time ( p = .017) for 5-HT 2AR BP, which increased 21.2% ± 2.6% following combined E 2 and P administration relative to baseline. This effect was evident in all cerebral cortex regions examined. Conclusions: 5-HT 2AR BP increased in widespread areas of the cerebral cortex following combined E 2 + P administration.

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