Pseudo-equilibrium in the brain was reached similar to 45 min post-injection. Metabolite analysis of [F-18]TZ3108 in NHP blood and rodent blood and brain revealed that
similar to 70% parent remained in the plasma of NHPs 60 min post-injection and the major radiometabolite did not cross the blood-brain barrier in rats. In summary, the potent, selective and metabolically stable sigma(1) specific radioligand [F-18]TZ3108 represents a potentially useful PET radioligand for quantifying the sigma(1) AC220 cost receptor in the brain.”
“Background: Many persistent organic pollutants (POPs) accumulate readily in polar bears because of their position as apex predators in Arctic food webs. The pregnane X receptor (PXR, formally NR1I2, here proposed to be named promiscuous
xenobiotic receptor) is a xenobiotic sensor that is directly find more involved in metabolizing pathways of a wide range of environmental contaminants. Objectives: In the present study, we comparably assess the ability of 51 selected pharmaceuticals, pesticides and emerging contaminants to activate PXRs from polar bears and humans using an in vitro luciferase reporter gene assay. Results: We found that polar bear PXR is activated by a wide range of our test compounds (68%) but has a slightly more narrow ligand specificity than human PXR that was activated by 86% of the 51 test compounds. The majority Fosbretabulin price of the agonists identified (70%) produces a stronger induction of the reporter gene via human PXR than via polar bear PXR, however with some notable and environmentally relevant exceptions. Conclusions: Due to the observed differences in
activation of polar bear and human PXRs, exposure of each species to environmental agents is likely to induce biotransformation differently in the two species. Bioinformatics analyses and structural modeling studies suggest that amino acids that are not part of the ligand-binding domain and do not interact with the ligand can modulate receptor activation. (C) 2015 The Authors. Published by Elsevier Inc.”
“Navder KP, He Q, Zhang X, He S, Gong L, Sun Y, Deckelbaum RJ, Thornton J, Gallagher D. Relationship between body mass index and adiposity in prepubertal children: ethnic and geographic comparisons between New York City and Jinan City (China). J Appl Physiol 107: 488-493, 2009. First published June 18, 2009; doi: 10.1152/japplphysiol.00086.2009.-Body mass index (BMI) is often used as a surrogate estimate of percent body fat in epidemiological studies. This study tested the hypothesis that BMI is representative of body fatness independent of age, sex, ethnicity, and geographic location in prepubertal children.