Characteristics of [3H](+)-amphetamine binding sites in the rat central nervous system
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Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class
2011, Bioorganic and Medicinal ChemistryCitation Excerpt :On the other hand, (S)-amphetamine, associated with stimulant properties, is bound at NET (EC50 = 7.1 nM) and DAT (EC50 = 24.8 nM) in cloned human cells7 and with low affinity at SERT (EC50 = 1.77 μM)7 and at rat adrenergic alpha sites (Ki∼1 μM)8 but not at 5-HT receptors. Binding sites for (S)-[3H]amphetamine have been reported in rat brainstem, hypothalamus, and striatum.9 Further studies have characterized two sites for [3H]amphetamine: a low affinity sequestration-site lacking stereospecificity10 and a high affinity, stereoselective site of (S)-[3H]amphetamine incorporation in striatal synaptosomes.11
Withdrawal from methylphenidate increases neural reactivity of dorsal midbrain
2010, Neuroscience ResearchCitation Excerpt :However, the study of Unis et al. (1985) showed no specific binding for MP in the brainstem. On the other hand, this encephalic region has the highest specific binding for [3H] amphetamine (Hauger et al., 1984). This result indicates that, in our study, the increased levels of anxiety induced during MP withdrawal, and attributed to midbrain regions sensitization, could be mainly due to changes in dopaminergic and noradrenergic pathways within cortical and subcortical limbic structures that act as modulators of unconditioned anxiety and fear behaviors organized in the brainstem.
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