Background: Anesthesia can significantly impact positron emission tomography (PET) neuroimaging in preclinical studies. Therefore, understanding these effects is crucial for accurate interpretation of the results. In this experiment, we investigate the effect of [F]-labeled glucose analog fluorodeoxyglucose ([F]FDG) uptake in the brains of rats anesthetized with two commonly used anesthetics for rodents: isoflurane, an inhalation anesthetic, and Hypnorm-Dormicum, a combination injection anesthetic.
View Article and Find Full Text PDFUnlabelled: β-arrestins (βarrs) are key regulators of G protein-coupled receptors (GPCRs), essential for modulating signaling pathways and physiological processes. While current pharmacological strategies target GPCR orthosteric and allosteric sites, as well as G protein transducers, comparable tools for studying βarrs are lacking. Here, we present the discovery and characterization of novel small-molecule allosteric inhibitors of βarrs through comprehensive biophysical, biochemical, pharmacological, and structural analyses.
View Article and Find Full Text PDFKetamine (KET) is recognized as rapid-acting antidepressant, but its mechanisms of action remain elusive. Considering the role of endocannabinoids (eCB) in stress and depression, we investigated if S-KET antidepressant effects involve the regulation of the eCB system using an established rat model of depression based on selective breeding: the Flinders Sensitive Line (FSL) and their controls, the Flinders Resistant Line (FRL). S-KET (15 mg/kg) effects were assessed in rats exposed to the open field and forced swimming test (FST), followed by analysis of the eCB signaling in the rat prefrontal cortex (PFC), a brain region involved in depression neurobiology.
View Article and Find Full Text PDFPharmaceuticals (Basel)
October 2024
Heterodimer peptides targeting more than one receptor can be advantageous, as tumors can simultaneously express more than one receptor type. For human breast cancer, a promising biological target is tumor angiogenesis through αβ integrin expression. Another promising target is Neuropeptide Y receptors, considering YR is overexpressed in 90% of human breast tumors.
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