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Hartig PR, Scheffel U, Frost JJ, Wagner HN Jr. 
“In Vivo Binding Of 125-i-LSD To Serotonin 5-ht2 Receptors In Mouse Brain”. 
Life Sciences. 1985;37(7):657-664.
The binding of 125-I-LSD (2-[125-I]-lysergic acid diethylamide) was studied in various mouse brain regions following intravenous injection of the radioligand. The high specific activity of 125-I-LSD enabled the injection of low mass doses (14 ng/kg), which are well below the threshold for induction of any known physiological effect of the probe. The highest levels of 125-I-LSD binding were round in the frontal cortex, olfactory tubercles, extrafrontal cortex and striatum while the lowest level was found in the cerebellum. Binding was saturable in the frontal cortex but increased linearly in the cerebellum with increasing doses of 125-I-LSD. Serotonergic compounds potently inhibited 125-I-LSD binding in cortical regions, olfactory tubercles, and hypothalamus but had no effect in the cerebellum. Dopaminergic compounds caused partial inhibition of binding in the striatum while adrenergic compounds were inactive. From these studies we conclude that 125-I-LSD labels serotonin 5-HT2 receptor sites in cortical regions with no indication that other receptor sates are labeled. In the olfactory tuberclas and hypothalamus, 125-I-LSD labeling occurs predominantly or entirely at serotonin 5-HT2 sites.n In the striatum, 125-I-LSD labels approximately equal proportions of serotonergic and dopaminergio sites. This data indicates tha 125-I-LSD labels serotonin receptors in vivo and suggests that appropriate derivatives or 125-I-LSD may prove useful for tomographic imaging of serotonin 5-HT2 receptors in the mammalian cortex.
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