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Methods br Results br Discussion SV exocytosis from
2021-12-10

Methods Results Discussion SV exocytosis from excitatory boutons is more sensitive to inhibition by isoflurane than exocytosis from inhibitory boutons,4, 31 but the mechanism(s) of this synaptic selectivity is unknown. Although P/Q-type VGCCs contributed quantitatively more to SV exocytosis t
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br Dual acting HR antagonists While the present medicinal
2021-12-10

Dual-acting HR antagonists While the present medicinal chemistry efforts are mainly focused on selective ligands targeting GPCRs, and particularly on H1R, H3R and H4R selective antagonists/agonists, there were and, also, still are several efforts to develop dual acting H1R/H2R, H1R/H3R and H3R/H4
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br Histamine and glycaemia Histamine is involved in a
2021-12-10

Histamine and glycaemia Histamine is involved in a wide variety of pathophysiological events mostly related to the inflammatory response through four receptors, namely H1-4Rs. The first studies of BIBR-1048 and diabetes date back to the 1950s. Since that time the involvement of histamine in diab
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br STAR Methods br Author
2021-12-10

STAR★Methods Author Contributions Introduction Hyaluronan, a major constituent of the extracellular matrix (ECM), is produced by hyaluronan synthases (HASs) and degraded by hyaluronidases (HYALs) (Vigetti et al., 2014). Physiologically, hyaluronan exists in a form with a molecular weight of
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Several bacterial functional pathways were observed after DO
2021-12-10

Several bacterial functional pathways were observed after DON administration, of which signal transduction, metabolism and genetic information processing displayed the highest levels of enrichment. Importantly, these three pathways were reported to be closely associated with DON's toxicity. Many evi
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br Heme oxygenase inhibitors Historically the first class
2021-12-10

Heme oxygenase-1 inhibitors Historically, the first class of competitive HO-1 inhibitors was represented by MPs, heme analogs in which the central iron Serdemetan of heme is exchanged by another element, such as zinc, cobalt, tin, or chromium. These molecules compete with heme for binding to the
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hydroxychloroquine sulfate mg In summary we have designed an
2021-12-09

In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstra
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In vertebrates three cognate receptors or receptor like sequ
2021-12-09

In vertebrates, three cognate receptors or receptor-like sequences have been identified with distinct distributions and functions (Millar, 2005, Neill et al., 2001). Only two types of GnRHR occur in mammals, though (Morgan and Millar, 2004). The mammalian type I GnRHR shares over 80% amino CCK Octap
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Additionally increased GLO gene expression protein
2021-12-09

Additionally, increased GLO1 gene expression, protein expression, and activity have been reported in a variety of cancers, including breast,22, 23, 24 pancreatic, melanoma, and prostate.27, 28, 29 Vince and Daluge proposed that inhibitors of GLO1 could serve as anti-tumor agents, by increasing conce
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Xie et al b reported that the combination of
2021-12-09

Xie et al. (2009b) reported that the combination of diagnostic ultrasound impulses and cyclic RGD-bearing MBs targeted for GP IIb/IIIa resulted in the successful recovery of epicardial and microvascular blood flow in swine models with acute thrombotic occlusion. It is well known that the stability o
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In a previous study M ykkynen et
2021-12-09

In a previous study (Möykkynen et al., 2003), we reported that ethanol lengthens the time needed for the AMPA receptors to recovery from desensitization in isolated hippocampal neurons. Here, we did not observe any effect of ethanol on recovery from desensitization in recombinant homomeric GluR-D re
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br Experimental section br Acknowledgments MIN cells were ki
2021-12-09

Experimental section Acknowledgments MIN6 RHPS4 synthesis were kindly provided by Dr. Junichi Miyazaki, Osaka University. This research was supported in part by the Ministry of Education, Culture, Sports, Science and Technology of Japan (JP16H05099 and JP18H04609 to K.H., and JP16H06574 to T.
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br Conclusions We have shown that despite the
2021-12-09

Conclusions We have shown that despite the development of severe insulin intolerance and marked alterations in whole body substrate oxidation that Gcgr−/− mice are protected against olanzapine-induced hyperglycemia. Our data provides evidence that this protective effect is likely due in large par
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When PKC was applied alone it attenuated the activity
2021-12-09

When PKC19–31 was applied alone, it attenuated the activity run-down following excision. Furthermore, the activity induced by addition of PKC19–31 during PMA treatment in many cases was higher than in controls. Accordingly, in our experimental conditions, the mechanism which underlays channel inhibi
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Glucocorticoid is a major regulator of body
2021-12-09

Glucocorticoid is a major regulator of body's response to stress (Armario, 2006). Repeated injections of the glucocorticoid corticosterone (CORT) in mice have been shown to produce an animal model of depression (Zhao et al., 2008). Further study of this phenomenon suggested that prolonged CORT expos
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