• The physiological and pharmacological roles of

  2021-12-27

  

  The physiological and pharmacological roles of GPR81 remain largely unclear because of several reasons. The low potency of lactate agonizing GPR81 in the millimolar range, together with its fast metabolic turnover, renders as a challenge in in vivo studies using lactate. Furthermore, there are no p

• Because of its excellent GPR potency good hERG selectivity

  2021-12-27

  

  Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, NS3694 receptor was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive

• Next to their indirect effect

  2021-12-27

  

  Next to their indirect effect on ASBT expression, microbiota are also directly involved in BA homeostasis and FXR-FGF15/19 signaling. Different species of intestinal microbiota have the ability to biotransform BAs mainly by deconjugation and subsequent de-hydroxylation, the latter resulting in more

• In this study we examined whether zebrafish ionocytes

  2021-12-27

  

  In this study, we examined whether zebrafish ionocytes might also share other types of similarity in transport function with kidney cells. In addition to ion transport, mammalian kidney UNC1215 also play key roles in xenobiotic elimination, through the action of ATP-Binding Cassette (ABC) transport

• The discovery that GLUT in the microvasculature represents

  2021-12-27

  

  The discovery that GLUT1 in the microvasculature represents an important target of VEGF thereby affecting ApoBrdU DNA Fragmentation Assay Kit sale function is highly relevant. The work of Jais et al. identified VEGF as a determining player in the regulation of cognitive performance and provides an i

• br Ghrelin Ghrelin was purified from rat stomach about

  2021-12-27

  

  Ghrelin Ghrelin was purified from rat stomach about twenty years ago as a 28-amino AI-10-49 octanoylated peptide and shown to be the endogenous ligand of the growth hormone (GH) secretagogue receptor (now termed GHSR1a, Howard et al., 1996, Kojima et al., 1999). GHSR1a is a 7-transmembrane recep

• Formoterol Hemifumarate There is a dual inducer of

  2021-12-24

  

  There is a dual inducer of both galanin and super-threshold pain. First, injury-induced pain may stimulate galanin secretion. After peripheral nerve injury, the galanin expression level was upregulated in dorsal root ganglion (DRG), dorsal horn and hypothalamic arcuate of rats [25], [28], [33]. The

• We conclude that a combination of GD specific

  2021-12-24

  

  We conclude that a combination of GD2-specific CAR T cell therapy with pharmacological EZH2 inhibition deserves investigation as a new therapeutic strategy in EwS and potentially other cancers with heterogeneous GD2 expression, including osteosarcoma, various soft tissue sarcomas, melanoma, lung can

• br Introduction Histamine was generally accepted as

  2021-12-24

  

  Introduction Histamine was generally accepted as a neurotransmitter in 1984, when histamine was first identified to be located in tuberomamillary nucleus (TM) of the brain (Watanabe et al., 1984). In mammals, histaminergic neurons play an important role in regulating multiple physiological activi

• In addition to acting as the gatekeeper for the

  2021-12-24

  

  In addition to acting as the gatekeeper for the metabolic and antioxidant roles of glucose, HKs have also been found to regulate mPTP opening directly. First described in the cancer field, the high-affinity HK isoforms HK1 and HK2 are strongly anti-apoptotic when bound to the outer mitochondrial mem

• Two distinct mechanisms have been described

  2021-12-24

  

  Two distinct mechanisms have been described for niacin’s macrophage-based actions [21,22]. First, niacin blocks recruitment of macrophages to atherosclerotic lesions. Second, niacin upregulates macrophage ABCA1 and ABCG1, transporters involved in reverse cholesterol transport. Upregulation of choles

• The physiological role of lactate

  2021-12-24

  

  The physiological role of lactate-induced antilipolytic effects is less clear. It has been speculated that GPR81 mediates the inhibition of lipolysis during intensive exercise, a condition which results in high systemic lactate plasma concentrations 9, 10. Owing to oxygen shortage resulting from int

• Human GPR hGPR was originally isolated in as

  2021-12-24

  

  Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,

• The first hypothesis better fertility in heifers that had CL

  2021-12-24

  

  The first hypothesis, better fertility in heifers that had CL at day 0, was clearly supported by our results. Heifers with a CL had over 60% P/AI compared to ∼50% in heifers without CL. These results are consistent with several other studies reporting that cycling heifers have greater fertility than

• To further investigate the molecular

  2021-12-24

  

  To further investigate the molecular mechanisms that underlie glycine's β-cell protective effects through its antioxidative activity in diabetes, we used a H2O2/high glucose-induced apoptosis cell model. Similar effects on ROS generation of high glucose and H2O2 support the in vivo results, suggesti

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