• br Acknowledgments br Introduction Guanosine cyclic monophos

  2021-09-18

  

  Acknowledgments Introduction Guanosine 3′,5′-cyclic monophosphate (cGMP) is a signaling molecule with key roles in diverse (patho) physiological responses and processes in numerous prokaryotes and all eukaryotes. The number of reports stating the role of cGMP in different processes in plants i

• br Results and discussion br Conclusion In summary starting

  2021-09-17

  

  Results and discussion Conclusion In summary, starting from our previous lead GZD824 1, we replaced the 5-nitropyrimidine core with pyrimidopyrimidine to obtain a series of novel compounds as drug candidates of GPR119 agonist for treatment of type 2 diabetes. Some derivatives showed good agon

• Adenine mg On the other hand it is quite possible that

  2021-09-17

  

  On the other hand, it is quite possible that strychnine-sensitive glycine sites are responsible for mediating the anticonvulsant effects of GlyT1 inhibitors. Strychnine, which acts as an antagonist at these sites, is a well-known as a convulsant drug, and elevation of endogenous glycine levels at th

• Histamine functions as a key neurotransmitter in multiple ci

  2021-09-17

  

  Histamine functions as a key neurotransmitter in multiple circuits to control various behaviors. In Drosophila photoreceptor, N-Methyl-D-aspartic acid is produced de novo by histidine decarboxylase (Burg et al., 1993); meanwhile, maintaining normal histamine content also depends on the histamine re

• Recent studies revealed that synthetic oligomeric A decrease

  2021-09-17

  

  Recent studies revealed that synthetic oligomeric Aβ1-42 decreased GLT-1 expression and promoted mislocalization of GLT-1 from the cell surface of primary astrocytes, leading to glutamate dyshomeostasis in synapses (Abdul et al., 2009, Scimemi et al., 2013). To address the cause for reduction of ast

• br Experimental br Acknowledgments This project was generous

  2021-09-17

  

  Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t

• As glucagon stimulated hepatic glucose production

  2021-09-17

  

  As glucagon-stimulated hepatic 43 7 production is a key component of the normal response to hypoglycemia, the potential of a GCGr antagonist to delay or prevent recovery from a hypoglycemic state is a critical safety issue that must be addressed. Studies of the effects on time to recovery from a hy

• Studies of human and mouse GPR as ascertained

  2021-09-17

  

  Studies of human and mouse GPR84, as ascertained by mRNA levels in various tissues, have determined that GPR84 is highly expressed on bone marrow cells, splenic T and B cells, and circulating granulocytes/monocytes/macrophages. In the latter cells, mRNA expression of is up-regulated only under infl

• br Materials and methods br Results The

  2021-09-17

  

  Materials and methods Results The immunoblot analysis demonstrated the presence of similar immunoreactivity by liver FBPase in hepatic and renal extracts. These results indicate that FBPase is present in a similar amount in both tissues. Moreover, the analysis revealed that the antibody detect

• Recent findings of us suggest that compounds

  2021-09-17

  

  Recent findings of us suggest that compounds that inhibit both FAAH and TRPV1 may be more efficacious in pain relief than those targeting only one such protein. As continuation of our efforts to identify new molecules able to target simultaneously both FAAH and TRPV1 receptors, we hypothesized that

• About of human primary melanomas and of melanoma metastases

  2021-09-17

  

  About 67% of human primary melanomas and 56% of melanoma metastases display cytoplasmic or nuclear β-catenin accumulation (Xue et al., 2016). Of note, active β-catenin stimulates emergence of metastasizing melanoma in mice harboring BrafV600E or NrasQ61K hyperplasia (Damsky et al., 2011, Delmas et a

• br Funding This study was supported by grants in

  2021-09-16

  

  Funding This study was supported by grants-in-aid for scientific research from the Japan Society for Promotion of Science (grant 16K186462 to Dr. Tomizawa, grant 16K19989 to Dr. Kobayashi, and grant 16H05433 to Dr. Mitsudomi) and a research grant from Boehringer-Ingelheim (to T. Mitsudomi). Co

• br Conclusions br Acknowledgement br Introduction

  2021-09-16

  

  Conclusions Acknowledgement Introduction The macrophage is an important cell species that plays key roles in innate immune responses and inflammatory reactions through phagocytosis of foreign bodies and secretion of inflammatory mediators such as interleukin (IL)-1, tumor necrosis factor (T

• br Activity dependent control of myelination and myelin

  2021-09-16

  

  Activity-dependent control of myelination and myelin maintenance Oligodendrocytes have intrinsic myelinating capacity and can myelinate fixed JSH-23 in addition to synthetic nanofibers and micropillars [21, 34, 35]. What prevents oligodendrocytes from myelinating dendrites or other cells in the C

• Firstly the impact on activity and selectivity was made

  2021-09-16

  

  Firstly, the impact on activity and selectivity was made by replacing the 2, 3-di-F substitution of ring A with 2,3-OCHO- () and 2-NO () substitutions, and replacing the 3, 5-di-F substitution of ring B with 3,5-di-OMe () and 3,5-di-Me () substitutions. Compound kept moderate activity (EC = 220 nM)

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