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It has been known for some time
2022-01-12
It has been known for some time that an oral salt load given to mammals induces a much greater natriuresis than the intravenous administration of an equivalent amount of saline (Carey et al., 1976, Singer et al., 1998). In addition, oral administration of salt to rats has been reported to augmented
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Studies utilising GPR mice however report different effects
2022-01-12
Studies utilising GPR55−/− mice, however, report different effects of GPR55 on body weight and insulin sensitivity. Genetic deletion of GPR55 appears to have no effect on overall body weight 5, 6, 7. However, one of these studies found increased fat deposition and insulin resistance in GPR55−/− mice
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To gain insights for further improvement of
2022-01-12
To gain insights for further improvement of the agonistic activity, we compared the structural features of the -carbamate piperidine moiety in with that of the spirocyclic moiety in –. Obviously, the substituent corresponding to an isopropyl group on the -carbamate in was lacking in the spirocyclic
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Variants of NEIL were also analysed in
2022-01-12
Variants of NEIL1 were also analysed in Primary sclerosing cholangitis (PSC) and cholangiocarcinoma (CCA) patients by Forsbring et al. to identify effect of variants on these diseases. Four variants were identified i.e., one earlier validated (G83D) and three novel (E181K, H275, R339W). E181K was fo
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Growing evidence suggests that the glycine site seems to
2022-01-11
Growing evidence suggests that the glycine site seems to play a pivotal role in NMDAR-related function. For example, it Decoquinate has been demonstrated in a hippocampal slice study that the glycine site sub-serves the spatiotemporal detection of synaptic activity (Li et al., 2009). Moreover, mice
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Our overall goal is to develop
2022-01-11
Our overall goal is to develop selective compounds for low-affinity/high-capacity transporters inhibitors (i.e. OCT1–3 and PMAT), and provide the field with much needed, specific pharmacological tools to study these transporters. In our initial efforts, we synthesized halogen substituted analogs and
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Epinephrine responses to hypoglycemia are probably triggered
2022-01-11
Epinephrine responses to hypoglycemia are probably triggered centrally, perhaps with input from peripheral hypoglycemia sensing [3], [4]. We observed increased epinephrine responses in GCK-MODY and I366F diabetic mice. Consistent with a role for Cathepsin Inhibitor 1 receptor GCK in detecting a low
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Here we examined whether complete ablation of GIP
2022-01-11
Here, we examined whether complete ablation of GIP production could reduce weight gain in the absence of the adipocyte hormone leptin, a condition that results in extreme hyperphagia, obesity, hyperinsulinemia, and insulin resistance, in both mice [24] and humans [25]. We found that Lepob/ob mice be
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Recently some researchers working in China Pharmaceutical
2022-01-11
Recently, some researchers working in China Pharmaceutical University developed novel FFA1 agonists some of which were found to be efficacious in the management of type 2 diabetes and with low toxicity. For instance, Zheng et al. [48] in their in vivo study using experimental animals, reported that
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Conclusions br Author information The
2022-01-11
Conclusions Author information The obtained models of complexes of FPR2 with most of the described compounds are freely available at the author’s web site: http://www.biomodellab.eu/models/. Acknowledgements This work was partly done at the Interdisciplinary Centre for Mathematical and Compu
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Several transgenic and knockout congenic mouse models have
2022-01-11
Several transgenic and knockout/congenic mouse models have been generated in order to assess the role of FFAR1 for proper insulin secretion and maintenance of glucose homeostasis. The results obtained with three different receptor knockout mouse models were not consistent. The protection against hig
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We found the FAAH CC genotype only confers
2022-01-11
We found the FAAH CC genotype only confers risk for anxiety if the CRFR1 minor allele combination is also present. Additionally, the FAAH AA/AC genotype was riskier than the CC if the three CRFR1 minor ARCA EGFP were not present. This result is somewhat contrary to our prediction as we hypothesized
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Migration chemotaxis and trafficking of
2022-01-11
Migration, chemotaxis and trafficking of leukocytes, including eosinophils from the peripheral blood into the site of inflammation requires their adhesion to endothelial EGFR Inhibitor (Ley et al., 2007). Despite ongoing research, the histamine effect on eosinophils adhesion to endothelium cells ha
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Tylophora atrofolliculata is a centuries used folk medicine
2022-01-11
Tylophora atrofolliculata is a centuries-used folk medicine for the treatment of rheumatism in China (Jiangsu New Medical College, 1977). One group of its bioactive components is phenanthroindolizidine alkaloids, which have been demonstrated as lead compounds of anti-tumor agents in our previous stu
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The overall response rate to
2022-01-11
The 13% overall response rate to afatinib is comparable to a 19% response rate reported by Peters et al. [20] in a separate retrospective series investigating the use of afatinib in more heavily pretreated patients with HER2-mutant lung adenocarcinomas. Our 13% response rate is also comparable to an
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