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In various models histamine has been shown to induce
2022-07-22

In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit
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With LML methyl oxo dihydropyridazin yl piperidin
2022-07-22

With LML-134 (1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate) containing drug-likeness properties (MW 375.47, five HBA, and MLogP 1.88), Novartis presents an additional drug-candidate to treat excessive sleepiness. A phase I clinical study was perform
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Allergic rhinitis characterized by inflammation of
2022-07-22

Allergic rhinitis, characterized by inflammation of the nasal membrane, results from an over-activated immune system exposed to VER 155008 in sensitized individuals, and is associated with nasal congestion, rhinorrhea, sneezing, and pruritus. As histamine is a key mediator in triggering allergic rh
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br Acknowledgments br Introduction The incidence of cholangi
2022-07-22

Acknowledgments Introduction The incidence of cholangiocarcinoma (CCA), a malignant tumor found in both intra- and extra-hepatic biliary epithelia [1], has been increased worldwide over the past two decades [2]. The prognosis of CCA patients are generally poor, due to the lack of early detecti
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Furthermore a direct thiol protective role of
2022-07-22

Furthermore, a direct thiol protective role of S-nitrosylation has been reported in animals [66]. Here, formation of higher order irreversible oxidative modifications, such as sulfinic and sulfonic acids were prevented by S-nitrosylation. All these observations underline the important role of ROS in
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br Conclusions br Acknowledgements The authors thank Matt JM
2022-07-21

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 consequ
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liothyronine sodium Some studies show that testosterone may
2022-07-21

Some studies show that testosterone may be involved in regulating cell proliferation and its stimulating effect has been proved in castrated rats (Wainwright et al., 2011), but not in mice and meadow voles (Ormerod and Galea, 2003; Benice and Raber, 2010). However, the seasonal difference in cell pr
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Based on the role of NMDA receptors
2022-07-21

Based on the role of NMDA receptors in initiation and propagation of epileptic seizures and on potentiation of NMDA function by glycine, it has been hypothesized that glycine will have proconvulsant activity (Foster and Kemp, 1989). Indeed, there is some evidence that human epileptogenic foci, remov
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AFB Fapy dG has been long recognized as a substrate
2022-07-21

AFB1-Fapy-dG has been long recognized as a substrate for nucleotide excision repair [24,25]. However, we recently demonstrated that this lesion is removed by Amphotericin B excision repair. We showed that DNA glycosylase NEIL1, a member of the Fpg/Nei glycosylase family, could excise AFB1-Fapy-dG fr
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Entry into CNS is tightly regulated by highly
2022-07-21

Entry into CNS is tightly regulated by highly dynamic barriers, namely, the BBB, the blood-CSF barrier, and the arachnoid epithelium (Abbott et al., 2010; Yasuda et al., 2013). Similar barriers also exist within the CNS including the ependymal barrier as well as the cellular membrane barriers of the
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The bioconversion of inositol from glucose was anticipated n
2022-07-21

The bioconversion of inositol from glucose was anticipated nearly a century ago and later confirmed by isotope tracing methods [[22], [23]]. This biosynthesis of inositol involves three sequentially acting enzymes: Firstly, ATP-dependent glucokinase converts glucose to glucose-6-phosphate (G-6P) [[2
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Animal studies have shown that various antidepressant treatm
2022-07-21

Animal studies have shown that various antidepressant treatment are capable of upregulating GR protein and mRNA in key (R,S)-Anatabine regions including the hippocampus and decreasing basal and/or stress-induced glucocorticoid secretion [37]. Changes in the level or function of GR regulate the nega
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br Acknowledgements br Introduction Glucagon a amino acid pe
2022-07-21

Acknowledgements Introduction Glucagon, a 29-amino Scrambled 10Panx peptide, is released from the pancreatic islets, intestine and stomach. Glucagon is released under hypoglycemic conditions and then elevates blood glucose levels, serving as a major counter hormone [1]. The regulation of gluc
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In addition to our results Chen et al
2022-07-21

In addition to our results, Chen et al. showed that administration of the GalR1 antagonist M40 improves cardiac function and attenuates cardiac remodeling in rats with heart failure [26]. These effects might be attributed to M40 suppression of galanin inhibitory effect on the vagal nerve in heart fa
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br Conclusions GPCRs are versatile signaling
2022-07-21

Conclusions GPCRs are versatile signaling molecules regulating almost all physiological processes, including energy homeostasis and glucose homeostasis.105, 106 They also prove to be important therapeutic targets. Drugs targeting GPCRs account for 30% of current pharmaceutical sales. GPR40 is a m
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