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Compounds and were tested for pharmacodynamic effects
2022-01-29

Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion a
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br Discovery of GPR A The murine niacin receptor protein
2022-01-29

Discovery of GPR109A The murine niacin receptor, protein upregulated in macrophages by interferon-γ (PUMA-G), was identified as a G-protein-coupled receptor (GPCR) expressed in adipocytes and spleen [22], [23]. This finding suggested a role of this receptor in macrophage function [24]. In 2003, t
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Injury to oligodendrocyte progenitors caused
2022-01-29

Injury to oligodendrocyte progenitors caused in part by glutamate contributes to the pathogenesis of myelination disturbances in PVL [5]. In the immature human brain, the susceptibility of developing oligodendrocytes to hypoxia-ischemia correlates with their expression of glutamate receptors of the
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br Acknowledgments br Introduction Postmenopausal osteoporos
2022-01-29

Acknowledgments Introduction Postmenopausal osteoporosis, which is primarily caused by Biotin-HPDP deficiency, has been a worldwide health problem and threatens postmenopausal women of all races. An estimated 80% of osteoporosis patients in the United States are women, and approximately 30% of
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br Introduction The growth hormone secretagogue receptor
2022-01-29

Introduction The growth hormone secretagogue receptor (GHSR) gene, which was first isolated from rats and humans (Kojima et al., 1999), comprises two exons and one intron in mammals and chicken. The pig GHSR is located on chromosome 13 (range 110,981,465–111,006,149 on Reference Sscrofa11.1). Alt
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Given the estimated number of NSVDC channels in a red
2022-01-29

Given the estimated number of 150–300 NSVDC channels in a red cell [7] and a single channel conductance of 30 pS at physiological salt concentrations [6], the maximum conductance observed in intact red cgk indicate either a very low open state probability, in the order of 10−3 or a far lower unit co
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PK profiles of were evaluated and found to be improved
2022-01-28

PK profiles of were evaluated and found to be improved compared to compound presumably due to interruption of β-oxidation. Low clearance and high plasma exposure were considered to be suitable profiles as an oral agent (). We first examined in vitro insulinotropic effects of compound from MIN6 c
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Reducing the molecular weight According to a thorough analys
2022-01-28

Reducing the molecular weight: According to a thorough analysis of a large, structurally diverse Caco-2 permeability dataset using a variety of statistical techniques by AstraZeneca researchers, logD and molecular weight are suggested the most important factors in determining the permeability of dru
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Through the analysis of various synthetic GPR agonists
2022-01-28

Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic e mycin synthesis motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discove
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In conclusion our results showed that FFAR can mediate the
2022-01-28

In conclusion, our results showed that FFAR1 can mediate the effect of PIO in attenuating β-cell lipoapoptosis through anti-oxidative stress, which may be related to the activation of the PLCγ-ERK1/2-PPARγ pathway. Our study helps not only to distinguish the role played by FFAR1 in lipotoxicity, but
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Liver and muscle isozymes have been found
2022-01-28

Liver and muscle isozymes have been found in vertebrate tissues [2], [5], [6]. The liver FBPase is recognized as a regulatory enzyme of gluconeogenesis. The muscle isozyme participates in the glycogen synthesis from lactate and in the regulation of glycolysis [7], [8], [9]. The basic difference betw
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br Conclusion br Acknowledgements This
2022-01-28

Conclusion Acknowledgements This work was supported by R01 HL127386 (Niklason) and 1R01 HL128406-01A1 (Dardik), and by an unrestricted research gift from Humacyte Inc. KLL was supported by F30HL143880. KLL and EQ were supported by T32 GM007205. LEN is a founder and shareholder in Humacyte, Inc
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H R antagonism can prevent seizure development and
2022-01-28

H3R antagonism can prevent seizure development and improve working memory through the activation of histaminergic neurons (Huang et al., 2004, Zhang et al., 2003). In addition, we have recently found that H3R antagonism protects against ischemia-reperfusion injury via histamine-independent mechanism
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Dual H H receptor antagonists developed by GlaxoSmithKline h
2022-01-28

Dual H1/H3 receptor antagonists developed by GlaxoSmithKline have also reached clinical trials at various stages. These candidates are useful for alleviating the symptoms associated with allergic rhinitis(Daley-Yates et al., 2012). GSK-1004723, 4-[(4-chlorophenyl)methyl]-2-( (2R)-1-[4-(4- [3-(hexahy
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Over recent decades there were three breakthroughs of
2022-01-28

Over recent decades, there were three breakthroughs of high intensity heavy-ion acceleration [6]. The first is the invention of radio frequency quadrupole (RFQ) type accelerator, which could accelerate more than dozens of milli-ampere ion beams and is a good solution to space-charge-effect of heavy-
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