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We found that several anticancer drugs inhibit
2023-10-30
We found that several anticancer drugs inhibit 5-HT3 57 9 current in vitro. Several studies have suggested that 5-HT3 receptor antagonists have anti-mitogenic and apoptotic effects on colorectal and breast cancer cell lines (Ataee et al., 2010, Hejazi et al., 2015). Irinotecan is used frequently to
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A previous study reported that the serotonergic mechanism wa
2023-10-30
A previous study reported that the serotonergic mechanism was involved in the psychological stress-induced alteration in synaptic plasticity in the rat hippocampal CA1 field (Matsumoto et al., 2004). Sumitaka Inoue et al. (Inoue et al., 2014) reported that pretreatment with a 5-HT1A receptor partial
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br Conclusion br Conflicts of Interest Disclosures br Acknow
2023-10-30
Conclusion Conflicts of Interest/Disclosures Acknowledgement This study was funded by the Ministry of Science of the Republic of Serbia (grant #175083). Introduction Myasthenia gravis (MG) is an antibody-mediated, neuromuscular transmission disorder, where the targets are postsynaptic p
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br Discussion Here we focused on seven plant alkaloids extra
2023-10-30
Discussion Here, we focused on seven plant alkaloids extracted from yokukansan. These alkaloids individually inhibited 5-HT-mediated 5-HT3A and 5-HT3AB receptor currents weakly. Simultaneous administration of these alkaloids, however, inhibited the 5-HT3A and 5-HT3AB receptor currents strongly. T
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Having established the structural requirements for potency i
2023-10-30
Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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Why do glutamate and glycine bind to the receptor
2023-10-30
Why do glutamate and glycine bind to the AZ20 in such different ways? Given the overall structural similarity between the GluN2A and GluN1 LBDs, one might conclude that the LBDs also bind ligands via similar processes. NMDA receptors with engineered disulfide linkages that lock the GluN1 lobes shut
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Thus phosphorylation of p was used to
2023-10-30
Thus, phosphorylation of p38 was used to measure the intracellular potency of ASK1 inhibitors. In this assay, HEK293/AP-1luc TAI-1 expressing human full-length ASK1 were incubated with compound for 18 h and then lysed and the level of phospho-p38 was quantified using the HTRF assay [33]. Results
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It is well known that neurosteroids
2023-10-30
It is well-known that neurosteroids such as testosterone and their metabolites endogenously modulate neural excitability in animals and humans. Testosterone has protective effects against seizures induced by KA and PTZ (Frye et al., 2001b; Reddy, 2004b). Estrogens, on the other hand, have proconvuls
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This study evaluated the anti tumor
2023-10-30
This study evaluated the anti-tumor influences of LA against HepG2 Chelerythrine Chloride synthesis in vivro, and investigated the molecular mechanisms of inducing apoptosis. Overall, our studies suggested that LA is a promising anti-cancer drug and a possible novel therapeutic agent directed towar
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Decoquinate australia br Roles of apelin and APJ in cardiova
2023-10-30
Roles of apelin and APJ in cardiovascular diseases Therapeutic potential of apelin/APJ in cardiovascular diseases Since the apelin/APJ system plays a key role in the occurrence and development of cardiovascular diseases, it seems logical to presume that targeting this axis should be feasible a
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Overall the expression of both components ligand and recepto
2023-10-30
Overall, the expression of both components (ligand and receptor) of the apelin signaling system allows for analysis of the direct role of apelin in CL function, and specifically P4 production. Although the CL secretes many different hormones, P4 is of predominant importance because it is necessary f
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Acknowledgments br Introduction Pulmonary fibrosis
2023-10-30
Acknowledgments Introduction Pulmonary fibrosis (PF) is a chronic, fibrosing interstitial pneumonia and a crushing disease that occurs as a result of a variety of lung injuries, including auto-immune, tuberculosis and traumatic insult [1], [2]. PF is characterized by the accumulation of extracel
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Therefore we have further investigated the anti
2023-10-30
Therefore, we have further investigated the anti-oxidant activity of isogarcinol in vitro by measuring the scavenging of 2,2′-diphenyl-1-1picrylhydrazyl (DPPH) and 2,2′-azino-bia (3-ethylben-zothiazoline-6-sulphonicacid) (ABTS), and determining its reducing power and ability to prevent lipid peroxid
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Recently AFF was used to convert
2023-10-30
Recently, AFF was used to convert an FN3-based binder specific to the Src homology 2 (SH2) domain of cAbl kinase into an allosterically regulated, intermolecular fluorescent switch (Figure 2D). Binding to cAbl kinase co-operatively stabilized the assembly of the FN3-based binder from two partial fra
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br Materials and methods br Results br Discussion Diabetic k
2023-10-27
Materials and methods Results Discussion Diabetic kidney disease (DKD) is the most common cause of end-stage renal disease [15], [16]. The pathogenesis of DKD is not fully understood, and there is no effective treatment. Although previous studies suggested that early lesions of DKD are foun
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