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iox australia Compounds and were tested for
2022-09-22
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 Ghrelin interactions with the opioid
2022-09-21
Ghrelin interactions with the opioid system The endogenous opioid system is an important regulator of appetite and metabolism (Bodnar, 2017, Nogueiras et al., 2012). In fact, several pharmacological studies have demonstrated that agonists of the three opioid receptors (mu, kappa, and delta) incre
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Interestingly GAL has also been shown to be co
2022-09-21
Interestingly, GAL has also been shown to be co-expressed and/or secreted in luteinizing hormone releasing hormone (LHRH) (Merchenthaler et al., 1991, Marks et al., 1994) and kisspeptin (KISS) neurons (Porteous et al., 2011). Furthermore, GAL was shown to stimulate luteinizing hormone (LH) secretion
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Cy7 NHS ester (non-sulfonated) mg There are many kinds of ne
2022-09-21
There are many kinds of neurological disorders and neuropsychiatric diseases, like stroke, dementia, schizophrenia and so on. Among these disorders, the most important reason for choosing depression in our study is that FXR has already been demonstrated to regulate the function of CREB, which is clo
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In recent years it was discovered
2022-09-21
In recent years, it was discovered in animals that certain types of non-apoptotic cell death are strictly dependent on iron and ROS. The term ‘ferroptosis’, derived from the Greek word ‘ptosis’ (falling) and the Latin word ‘ferrum’ (iron), is coined to describe such cell death phenomena. Cytoplasmic
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Histamine H and H receptors
2022-09-20
Histamine H1 and H2 receptors are considered as low affinity receptors (pKi of 4.2 and 4.3 respectively), whereas histamine H3 and H4 receptors as a high affinity receptors (pKi of 8 and 8.2 respectively) (Schreeb et al., 2013). Therefore it might well be that other histamine receptors might be invo
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To combat the detrimental effects of neuropathological condi
2022-09-20
To combat the detrimental effects of neuropathological conditions, additional therapeutic interventions that either dampen chronic neuroinflammation or attenuate reductions in hippocampal neurogenesis are critically needed. The cannabinoid system has already been shown to rescue impaired neurogenesi
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Introduction Gestational diabetes mellitus GDM
2022-09-20
Introduction Gestational diabetes mellitus (GDM) is one of the most common complications associated with pregnancy [1]. Approximately 7.6% of pregnancies in the United States are complicated by GDM [2,3], which significantly increases the mother's risk of developing type 2 diabetes (T2D) later in l
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With this goal in mind we proceeded
2022-09-20
With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in activ
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To verify DNA glycosylase AP lyase
2022-09-19
To verify DNA glycosylase/AP lyase activity we have employed a simple and efficient method to investigate based on fluorescein-labeled duplex oligonucleotides read on an automated sequencer (Allgayer et al., 2013, Lopes et al., 2007, Lopes et al., 2008). This approach using purified CpMutY proteins
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br Materials and methods br Results In this
2022-09-19
Materials and methods Results In this study we re-examined the kinetics of ET transport and tested the ability of various suggested substrates of OCNT1 to inhibit ET uptake. Using a native ET transporter expressed in the human HeLa cell line ET was found to be taken up with a Km of 51 μM and V
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The translation of our rat findings to bovine and
2022-09-17
The translation of our rat findings to bovine and human lenses revealed that the expression of glucose transporters was more straightforward in bovine and human than in the rat lens, since only GLUT1 was detected in these lenses. Using the C-terminal GLUT1 antibody, we observed bands for GLUT1 in al
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Various strategies have been pursued in the search for
2022-09-17
Various strategies have been pursued in the search for GIPR antagonists. Antibodies raised against both GIP(1–42) [14], [15] or the GIPR [16], [17], a small molecule antagonist [18], amino TNF-alpha, recombinant rat protein substitutions of GIP(1–42) [19], and various GIP(1–42) truncations and modif
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br Chemistry Analog has been previously reported by our grou
2022-09-17
Chemistry Analog 12 has been previously reported by our group. Experimental procedures for the synthesis and characterization of 13–32 are available in Scheme 1, Schemes S1–S9 and Table S1 in Supplementary data. Preparation of 30 and 31 is depicted in Scheme 1 as the representative example. Commo
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The mechanisms underlying the inhibitory effects of n
2022-09-17
The mechanisms underlying the inhibitory effects of n-3 FAs on neoplasia have not been completely elucidated. Until recently, the emphasis has been on the ability of n-3 FAs to compete for the pathways that lead to the synthesis of pro-inflammatory eicosanoids from arachidonic acid, an n-6 FA, there
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