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The serotonin subtype‐4 (5‐HT4) receptor, which is known to be involved physiologically in learning and memory, and pathologically in Alzheimer's disease, anxiety, and other neuropsychiatric disorders—has few radioligands readily available for imaging in vivo. We have previously reported two novel 5‐HT4 receptor radioligands, namely [methoxy‐11C](1‐butylpiperidin‐4‐yl)methyl 4‐amino‐3‐methoxybenzoate;...
In vitro, D2 dopamine receptors (DAR) can exist in low‐ and high‐affinity states for agonists and increases of D2 receptors in high‐affinity state have been proposed to underlie DA receptor supersensitivity in vivo. Deletion of the gene for dopamine β‐hydroxylase (DBH) causes mice to become hypersensitive to the effects of psychostimulants, and in vitro radioligand binding results suggest an increased...
In vitro experiments have shown that protoporphyrin IX (PPIX) binds to the translocator protein 18 kDa (TSPO), which transports cholesterol across the outer mitochondrial membrane. The purpose of this study was to examine whether binding of PPIX to TSPO can also be detected in vivo using positron emission tomography and [11C]PBR28, a radioligand that binds with high affinity and selectivity to TSPO...
Rolipram is a selective inhibitor of phosphodiesterase‐4 (PDE4), and positron emission tomography (PET) using [11C]rolipram can monitor the in vivo activity of this enzyme that is part of the cAMP second messenger cascade. cAMP‐dependent protein kinase (PKA) phosphorylates PDE4 and increases both enzyme activity and affinity for rolipram. In the present PET study, we examined effects of PKA modulators...
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