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In conclusion we have shown that mGlu receptors negatively
2023-09-12
In conclusion, we have shown that mGlu7 receptors negatively regulate α1-adrenergic receptor signalling in heterologous expression systems, UK-5099 tissue and living animals. This interaction might represent a protective mechanism aimed at restraining an excessive activation of noradrenergic transm
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br Actin cytoskeleton in protrusion Pushing
2023-09-12
Actin cytoskeleton in protrusion Pushing force driving membrane protrusion is generated by polymerizing 46619 filaments organized either into branched networks or parallel bundles. Branched networks are assembled through Arp2/3 complex-dependent actin nucleation and drive protrusion of lamellipo
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br Funding This work was supported by Arena Pharmaceuticals
2023-09-12
Funding This work was supported by Arena Pharmaceuticals, Inc, San Diego, CA, USA. Introduction 5-hydroxytryptamine 1B (5-HT1B) receptors are widely distributed in the central nervous system (CNS); they have various modulatory functions in drug reinforcement, appetitive behaviors, stress, moo
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Having taken a step back
2023-09-12
Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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TG101209 It was previously demonstrated that dissociation of
2023-09-12
It was previously demonstrated that dissociation of the V-ATPase in response to glucose depletion in yeast requires an intact microtubular network [28] and a catalytically active enzyme [29]. Interestingly, mutations in the non-homologous region of the catalytic subunit A are able to block dissociat
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In our H K ATPase assay Fig
2023-09-12
In our H+, K+-ATPase assay (Fig. 1 and Supplementary Fig. 1), myricetin (IC50 = 0.58μM) was more potent than acid-activated omeprazole (IC50 = 1.50μM). In contrast, in oral administration in mice (Fig. 3), omeprazole (20mg/kg) more effectively inhibited gastric KU-0059436 secretion compared to myri
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To better illustrate the involved neuronal postganglionic pa
2023-09-12
To better illustrate the involved neuronal postganglionic pathways, central apelin-13 injection was performed in rats received peripheral preadministration of NOS inhibitor L-NAME, sympatholytic agent guanethidine and/or muscarinic receptor agonist bethanechol. Compared with the rats received vehicl
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br Acknowledgements This study was
2023-09-11
Acknowledgements This study was funded the Irish Department of Agriculture, Food and the Marine through the research program FIRM/RSF/CoFoRD (Reference: 13 F 462). The authors declare no conflict of interest. Introduction Radiotherapy (RT) is one of the major treatment methods among patients
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br Model Fig demonstrates the block
2023-09-11
Model Fig. 1 demonstrates the block-scheme of main interactions between variables of the model under investigation. These interactions are described below in details and are expressed in mathematical form as well, where all variables are the functions of space and time coordinates, r and t, which
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Incubation of the aortic segments of rats with indomethacin
2023-09-11
Incubation of the aortic segments of rats with indomethacin significantly decreased the vasoconstrictor response to Phe but only in HgCl2-treated group (Fig. 9A,B), as indicated by dAUC values (Fig. 9E). Co-treatment with losartan once again proved to be effective and prevented the increased partici
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br Valsartan It is another ARB with several reports for
2023-09-11
Valsartan It is another ARB, with several reports for its beneficial effects on CV system both in preclinical and clinical studies. Valsartan treatment has reduced the levels of pentraxin 3, a marker for inflammation and is well tolerated in terms of side effects [17]. In BSCORE study, 90-day se
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Several mechanisms of Cd induced
2023-09-11
Several mechanisms of Cd-induced carcinogenicity have been reported and are comprehensively summarized by Hartwig [32]. As early as 1980, basic science studies supported a role for endocrine disruption of AR by Cd. Donovan et al. [33], using extracts of mouse prostate cytosol, showed Cd to be the mo
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br AR signals and chemosensitivity in urothelial cancer
2023-09-11
AR signals and chemosensitivity in urothelial cancer A significant amount of patients with urothelial cancer fail to respond to cisplatin-based systemic chemotherapy, although it remains the mainstay of successful management of advanced disease. However, underlying mechanisms for chemoresistance
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KN-93 The most common adverse effects were ARIA which occurr
2023-09-11
The most common adverse effects were ARIA, which occurred at higher levels than in any previous anti-Aβ mAb study. ARIA-E was observed at some point during the trial in no participants in the placebo group compared with 1 (3%), 2 (6%), 11 (37%), and 13 (41%) participants receiving 1, 3, 6, and 10 mg
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br Conflict of interest statement br Introduction The
2023-09-11
Conflict of interest statement Introduction The global prevalence of Alzheimer's disease (AD) is expected to increase to 106 million in 2050 from 30 million in 2010 (Brookmeyer et al., 2007), which will further impose a significant economic burden on health systems and society as a whole (Broo
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