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FPR family Human FPR was first defined
2021-12-20
FPR family Human FPR was first defined biochemically, in 1976, as a high affinity binding site on the surface of neutrophils for the prototypic N-formyl peptide formyl-methionine-leucyl-phenylalanine (fMLF). It was then cloned in 1990, by Boulay et al. from a differentiated HL-60 myeloid leukemia-c
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High lipophilicity of seems to cause
2021-12-20
High lipophilicity of seems to cause poor PK profiles. First we replaced the phenyl ring of compound with various hetero aromatic rings to reduce lipophilicity, (). The synthesis of pyridine derivative was shown in . (2′,6′-Dimethylbiphenyl-3-yl)methanol () was reacted with 2,5-dibromopyridine in th
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Glucose induced nuclear translocation of several enzymes inc
2021-12-20
Glucose-induced nuclear translocation of several enzymes, including GK, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), muscle GS, aldolase, lactate dehydrogenase (LDH) and phosphoglycerate kinase (PGK) is a well-known phenomenon. Additional functions have been proposed for these enzymes in the nu
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br Conclusion In conclusion rats
2021-12-20
Conclusion In conclusion, rats in this model of HELLP syndrome demonstrated increased placental and circulating FasL and increased placental Fas when compared to NP rats. Administration of an ETA receptor antagonist to HELLP rats tended to decrease circulating FasL and placental Fas, while not af
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Previous studies have attributed the changes that occurs dur
2021-12-20
Previous studies have attributed the changes that occurs during the behvioral sensitization to many psychostimulants with neuroadaptation in dopaminergic cell bodies of the VTA (induction phase) along with alteration in dopamine axon terminal field transmission of NAc during the expression to sensit
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EdU is a thymidine analog that is incorporated into replicat
2021-12-20
EdU is a thymidine analog that is incorporated into replicated chromosomal DNA during the S phase of the cell cycle. DAPI is a fluorescent dye that binds strongly to A-T-rich regions in DNA and is commonly used for cell nucleus staining. We used the EdU incorporation assay, which is a highly sensiti
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To prevent toxicity of free hemoglobin as well as
2021-12-20
To prevent toxicity of free hemoglobin as well as its degradation metabolites heme and free iron, several scavenger proteins and degradation enzymes protect the body. Haptoglobin (Hp) is the most well described hemoglobin scavenging protein that binds free hemoglobin and transports it to macrophages
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br Introduction Activation of the
2021-12-18
Introduction Activation of the lipid sensing receptor, GPR55, by lysophosphatidyl inositol (LPI) has been well documented, and implicated in endocannabinoid signaling [1]. Intracellular events resulting from GPR55 activation include; enhanced β-arrestin activity, calcium mobilization and ERK1/2 p
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br Next we explored the SAR around the aryl ring
2021-12-18
Next, we explored the SAR around the aryl ring attached to the pyrrole nitrogen in the presence of the 3-CF and the 2,6-difluorophenylpropionic adipor1 sidechain (). The EC value of the unsubstituted phenyl was about 100 nM. The 4-methyl was 2-fold more potent, however ethyl and bromo did not
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In summary through medicinal chemistry design and computer
2021-12-18
In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on
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In addition to their functional
2021-12-18
In addition to their functional activation of GPR109A, compounds of the pyrazolopyrimidine class also enhanced the binding of nicotinic hoechst stain to the receptor. For instance, increased the binding of H-nicotinic acid to the receptor (black curve) in a concentration-dependent manner, whereas
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On the basis of their relative Glu transport rates
2021-12-18
On the basis of their relative Glu transport rates and anion currents, EAATs group into two functionally distinct classes, EAAT1–3 being efficient Glu transporters with small associated macroscopic anion currents and EAAT4–5 low-capacity transporters with predominant anion conductance [18]. The diff
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Glial cells have emerged as important protagonists of the ce
2021-12-18
Glial cells have emerged as important protagonists of the central nervous system (CNS) physiology (Chen and Swanson, 2003; Kettenmann and Verkhratsky, 2008; Parpura and Verkhratsky, 2012). As widely described in the literature, astrocytes regulate glutamatergic synapses by clearance of glutamate in
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AMN-107 australia Considerable evidence links sustained GCG
2021-12-18
Considerable evidence links sustained GCG administration to the reduction of food intake, enhancement of energy expenditure and weight loss in rodent and human studies [16], [17], [18]. Moreover, patients presenting with GCG-producing tumors frequently manifest severe weight loss, through mechanisms
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The GAL also modified HT system Millon et al
2021-12-17
The GAL(1–15) also modified 5-HT system (Millon et al., 2015). Using a rat medullary raphe-derived cell line RN33B, we observed that GAL(1–15) significantly decreased the 5-HT immunoreactivity in the RN33B Metformin (p Conclusion All these data emphasized the role of GAL and its N-Terminal fragme
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