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Gratifyingly compound also demonstrated improved
2024-03-12
Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and
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br Acknowledgments This work was supported by Grant in aid
2024-03-11
Acknowledgments This work was supported by Grant-in-aid for Scientific Research (S) (20229008) (to T.K.), Targeted Proteins Research Program (to T.K.), the Global COE Research Program (to T.K.) and Translational Systems Biology and Medicine Initiative (to T.K.) from the Ministry of Education, Cul
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Role of APPL in endosomal signaling pathways Endosomes
2024-03-11
Role of APPL in endosomal signaling pathways Endosomes consist of distinct membrane subdomains within individual organelles and assist in the translation of extracellular stimuli via cytoplasmic transduction cascades to the nucleus [3], [74]. Endosomal abnormalities are associated with the pathogen
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The cellular mechanism underlying the CGS mediated inhibitio
2024-03-11
The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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Pacritinib We observed PACAP immunoreactivity in the molecul
2024-03-11
We observed PACAP2 immunoreactivity in the molecular layer of the cerebellar cortex in zebrafish. This result is consistent with the reporting of PACAP immunoreactivity in the soma and fibers of Purkinje cells and the presence of PACAP mRNA in the Purkinje-cell and granular-cell layers in rats [43].
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br Acknowledgements This work was supported
2024-03-11
Acknowledgements This work was supported by Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES), Fundação de Amparo à Pesquisa do Estado do Rio Grande do Sul (FAPERGS) FINEP research grant “Rede Instituto Brasil
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The hippocampus is the primary brain structure
2024-03-11
The hippocampus is the primary brain structure involved in learning and memory. The role of hippocampal synaptic plasticity in neurological processes in cognition and depression has been extensively demonstrated. Synaptophysin is a critical substance in synaptogenesis, which is necessary for learnin
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NLX a k a F or befiradol exhibits nanomolar affinity
2024-03-11
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in perifosine to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it ha
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Crohn s disease an inflammatory bowel disease that affects t
2024-03-11
Crohn’s disease, an inflammatory bowel disease that affects the gastrointestinal (GI) tract, is characterized by a polymorphism in ULK1 autophagy gene due to the presence of single nucleotide polymorphisms (SNPs). Thus, the autophagic process is impaired during the disease. The mutations in the leuc
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Levodopa receptor Several in vivo and in vitro studies
2024-03-11
Several in vivo and in vitro studies have demonstrated changes in bioactive lipid profiles under hyperglycemic conditions and have linked these changes with increased leukocyte adhesion and vascular dysfunction during diabetes. This input has originated partly from lipidomic studies that showed elev
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br ASK in Huntington s disease and other polyglutamine disea
2024-03-11
ASK1 in Huntington's disease and other polyglutamine diseases The polyglutamine (polyQ) diseases are a group of inherited neurodegenerative disorders caused by the expansion of cytosine-adenine-guanine (CAG) trinucleotide repeats in the coding regions of specific genes, leading to the production
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calcitriol hormone br Introduction Arginase deficiency is a
2024-03-11
Introduction Arginase deficiency is a rare metabolic disorder resulting from a loss of arginase 1 (ARG1), the final enzyme in the urea cycle, which is the major pathway for the detoxification of ammonia in terrestrial mammals. ARG1 is expressed most prevalently in hepatocytes and red blood cells.
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873 synthesis CORT induced hippocampal damage has been impli
2024-03-11
CORT-induced hippocampal damage has been implicated in depression, aging and long-term glucocorticoid therapy. Therefore, finding a drug that can protect hippocampal neurons from the adverse effects of CORT could have significant clinical benefits. In this regard, we tested the potential protective
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Studies have demonstrated that AT
2024-03-11
Studies have demonstrated that AT2 plays a greater role in modulating arterial pressure in females than in males. Chronic low-dose infusion of Ang II decreased blood pressure in female rats at a dose that had negligible effects in males. Furthermore, AT2 blockade eliminates the depressor response to
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Circular dichroism CD provides useful information
2024-03-11
Circular dichroism (CD) provides useful information about protein structure, the extent and rate of structural changes and ligand binding. CD is a form of light ML 221 receptor spectroscopy that measures differences in the absorbance of right- and left-circularly polarized light (rather than the co
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