A database of [(18)F]-altanserin binding to 5-HT(2A) receptors in normal volunteers: normative data and relationship to physiological and demographic variables.
This study presents the results of an analysis of 5-hydroxytryptamine (5-HT)(2A) receptors in 52 healthy subjects. Thirty men and twenty-two women aged between 21 and 79 years were investigated with magnetic resonance imaging (MRI) and [(18)F]-altanserin positron emission tomography (PET). The distribution volumes of specific tracer binding (DV(3)') was calculated for 15 brain regions using either cerebellum or pons as reference regions and correlations between DV(3)' and physiological and demographic variables were made. The regional distribution of [(18)F]-altanserin binding in the healthy human brain was in agreement with existing in vitro post-mortem human 5-HT(2A) data. Apart from nonspecific cerebellar binding (DV(2)), there was no gender difference in 5-HT(2A) binding. A positive correlation between cerebellar binding and age was observed and negative correlations between age and DV(3)' were found in all cortical regions, except occipital cortex, corresponding to a decrease in DV(3)' of 6% or 4% per decade with cerebellum or pons as reference regions, respectively. In several temporal and frontal cortical regions, positive correlations were found between body mass index (BMI) and DV(3)'. Our findings provide a resource to aid design of clinical studies of the 5-HT(2A) receptors. [(18)F]-altanserin binding appears to be unaffected by gender, but the effects of ageing must be considered for clinical studies. The correlations between different cortical regions' 5-HT(2A) binding and BMI should be explored in future studies.
Neurobiology Research Unit, University Hospital of Copenhagen, Rigshospitalet, Denmark.
Karen H
KH
Adams
Lars H
LH
Pinborg
Claus
C
Svarer
Steen G
SG
Hasselbalch
Søren
S
Holm
Steven
S
Haugbøl
Karine
K
Madsen
Vibe
V
Frøkjaer
Lars
L
Martiny
Olaf B
OB
Paulson
Gitte M
GM
Knudsen
D000328:Adult; D000368:Aged; D000375:Aging / Q000502:physiology; D001798:Blood Proteins / Q000378:metabolism; D015992:Body Mass Index; D001921:Brain / Q000000981:diagnostic imaging; D016208:Databases, Factual; D005260:Female; D005462:Fluorine Radioisotopes; D006801:Humans; D007650:Ketanserin / Q000031:analogs & derivatives* / Q000097:blood / Q000378:metabolism*; D008279:Magnetic Resonance Imaging; D008297:Male; D008875:Middle Aged; D008959:Models, Neurological; D011485:Protein Binding; D044402:Receptor, Serotonin, 5-HT2A / Q000187:drug effects*; D012016:Reference Values; D012702:Serotonin Antagonists / Q000097:blood / Q000378:metabolism*; D012727:Sex Characteristics; D014055:Tomography, Emission-Computed
D001798:Blood Proteins; D005462:Fluorine Radioisotopes; D044402:Receptor, Serotonin, 5-HT2A; D012702:Serotonin Antagonists; C071983:altanserin; D007650:Ketanserin