Characterization and regional distribution of serotonin S2-receptors in human brain
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Serotonin 2A receptors and cannabinoids
2021, Progress in Brain ResearchCitation Excerpt :The study of the anatomical distribution of 5-HT2ARs in the CNS is essential to elucidate the brain regions implicated in the regulation of the different mental processes in which this receptor is involved. In this context, 5-HT2ARs are abundantly expressed in several brain cortical areas, as originally outlined by studies using receptor radioligand binding approaches with human brain tissue homogenates (Schotte et al., 1983). A posterior study in postmortem human brain sections demonstrated that 5-HT2ARs are especially present in cortical layers III and V, hypothalamus and, to a lesser extent, in the hippocampus and striatal structures (Pazos et al., 1987).
Assessment of serotonin release capacity in the human brain using dexfenfluramine challenge and [ <sup>18</sup>F]altanserin positron emission tomography
2012, NeuroImageCitation Excerpt :Post hoc test revealed that especially the 60 mg dose significantly reduced BPP measures (Fig. 6). It should be noted that BPP might underestimate the true treatment effect, given that the cerebellum still has ~ 15% of the 5-HT2AR receptor density of the PFC (Eastwood et al., 2001; Luabeya et al., 1984; Pazos et al., 1987; Schotte et al., 1983). Cerebellar 5-HT2ARs might be comparably susceptible to dexfenfluramine-induced 5-HT efflux (or internalization) as cortical 5-HT2ARs.
Antipsychotic drug interactions with specific [<sup>3</sup>H]ketanserin binding sites in membrane fragments derived from human prefrontal cortex and human amygdala
2003, Brain ResearchCitation Excerpt :The possibility of a third affinity state for [3H]ketanserin in prefrontal cortex is also suggested by the fact that adrenergic agonists compete for less than 70% of the binding present in this region, but all of the binding present in amygdala. Multiple affinity states for [3H]ketanserin have been previously reported in human brain, rodent brain, and human platelets [9,12,13,18,19,26], although single affinity states have also been reported in these same tissues [8,12,14,16,18,21,28]. The previous studies of human amygdala have shown a single affinity state for [3H]ketanserin [8,14].
Antagonist binding at 5-HT(2A) and 5-HT(2C) receptors in the rabbit: High correlation with the profile for the human receptors
2000, European Journal of Pharmacology