Effects of estradiol and progesterone administration on human serotonin 2A receptor binding: a PET study.
BACKGROUND
Preclinical studies demonstrate that 17beta-estradiol (E(2)) increases serotonin-2A receptor (5-HT(2A)R) density in rat frontal cortex.


METHODS
We investigated the impact of hormone replacement therapy on 5-HT(2A)R binding potential (BP) using positron emission tomography and [(18)F]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(2A)R 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(2A)R BP increased in widespread areas of the cerebral cortex following combined E(2) + P administration.
Moses
E L
EL
Department of Psychiatry, University of Pittsburgh, Magee-Women's Research Institute, Pittsburgh, Pennsylvania, USA.
Drevets
W C
WC
Smith
G
G
Mathis
C A
CA
Kalro
B N
BN
Butters
M A
MA
Leondires
M P
MP
Greer
P J
PJ
Lopresti
B
B
Loucks
T L
TL
Berga
S L
SL
D001667:Binding, Competitive; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D004958:Estradiol / Q000008:administration & dosage / Q000378:metabolism*; D005260:Female; D005640:Follicle Stimulating Hormone / Q000378:metabolism; D006801:Humans; D008875:Middle Aged; D011374:Progesterone / Q000008:administration & dosage / Q000378:metabolism*; D011985:Receptors, Serotonin / Q000378:metabolism*; D014055:Tomography, Emission-Computed
D011985:Receptors, Serotonin; D011374:Progesterone; D004958:Estradiol; D005640:Follicle Stimulating Hormone