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GPR detection by reverse transcription
2022-04-18
GPR35 detection by reverse transcription-polymerase chain reaction (RT-PCR). Total RNA of cultured DRG neurons was extracted using the RNAqueous kit (Ambion). Complementary DNA (cDNA) was synthesized from 1μg of isolated total RNA with SuperScript III reverse transcriptase (Invitrogen). An aliquot o
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br Conclusions br Acknowledgements The authors thank
2022-04-18
Conclusions Acknowledgements The authors thank Matt JM Wood and colleagues (AstraZeneca, UK) for permission to use logD and protein binding data presented in Sup. Table S2. Introduction The number of people suffering from type 2 diabetes mellitus (T2DM) has escalated worldwide as a conseq
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Introduction Nicotinic acid niacin NA has been used in
2022-04-18
Introduction Nicotinic Colistin Methanesulfonate sodium salt (niacin, NA) has been used in the treatment of dislipidemia and cardiovascular disease for almost 60years (Offermanns, 2006). Large clinical studies showed that niacin alone or in combination with LDL-lowering drugs improved cardiovascul
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ICH induced striatal lesion produced a reduction of
2022-04-18
ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino caspofungin transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischemi
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Conoidin A br Materials and methods br
2022-04-18
Materials and methods Results Conclusions We developed a glutamate biosensor with chitosan as a matrix for the immobilization of the enzyme glutamate oxidase on the surface of a platinum electrode. Our miniaturized biosensor of 50 µm in diameter can be applied for monitoring glutamate in vi
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During the tests in vitro SHP
2022-04-18
During the tests in vitro, SHP289-04 showed the beneficial effect on both two important aspects. In human liver carcinoma cell line HepG2, it was found to improve glucose consumption significantly. Otherwise, in pancreas cell line NIT1, it could only promote insulin secretion significantly at high g
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The eradication of agonist activity in
2022-04-18
The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary Retigabine dihydrochloride as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could
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Fourthly the distribution sites after
2022-04-18
Fourthly, the distribution sites after i.c.v. injection of FAM-ghrelin(1–7)-NH2 were explored in mice using the technologies of fluorescence labeling. The green fluorescence of FAM-ghrelin(1–7)-NH2 was strongly distributed in these structures of lateral ventricle, lateral septal nucleus, dorsal part
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The intestinal epithelium is the first line of
2022-04-18
The intestinal epithelium is the first line of defense against pathogens and noxious agents and exerts a range of physiological activities, including digestion and CC-10004 of nutrients. The intestinal wall consists of a series of finger shaped protrusions called villi and invaginations known as cry
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The FAAH inhibitor activity of the ethoxycarbonyl phenyl
2022-04-18
The FAAH inhibitor activity of the 3-(5-(ethoxycarbonyl)-1-phenyl-1H-pyrazol-3-yl)phenyl cyclohexylcarbamates was investigated by preparation of compounds (43–52, Table 3). These new compounds displayed an important loss of activity in comparison with the corresponding regioisomers 5-phenyl compound
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br Introduction Lysine acetylation is an important post
2022-04-16
Introduction Lysine acetylation is an important post-translational modification that is found on numerous cellular proteins, including both histone and non-histone proteins [1], [2]. Dynamic acetylation and deacetylation is regulated by enzymes called histone acetyltransferases (HATs) as writers
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Dual H H receptor antagonists
2022-04-16
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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br Materials and methods br Results br Discussion
2022-04-16
Materials and methods Results Discussion Serum HBsAg is not only an important serological marker for the screening and diagnosis of HBV infection but also an important indicator for the treatment of hepatitis B [15]. Jaroszewicz et al. [4] and Nguyen et al. [8] reported that the HBsAg level
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Carbon monoxide another key product from
2022-04-16
Carbon monoxide, another key product from the breakdown of heme by HO-1, also plays an important role in the vasculature. Like NO, CO is endogenously derived from the endothelium [68] and can weakly activate sGC by binding to its heme moiety [69]. CO was found to have vasodepressor activity in rats
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br GSK The GSK family is highly conserved throughout
2022-04-16
GSK-3 The GSK-3 family is highly conserved throughout evolution and is encoded by two genes, GSK-3α and GSK-3β, which are located in chromosomes 19q13.2 and 3q13.3 in human, respectively. Both GSK-3α and GSK-3β proteins exist in a variety of tissues with the highest levels found in Darunavir Etha
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