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Subsequently Palvimaki et al corroborated Ni and Miledi s st
2024-05-15
Subsequently, Palvimaki et al. (1999) corroborated Ni and Miledi's study by demonstrating that treatment with fluoxetine leads to 43% occupancy of the 5-HT2C receptors. Moreover, the affinity of fluoxetine for 5HT2C receptors (Ki 65 nM) is close to its affinity for 5-HT transporters (Ki 33 nM) (Ni a
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Furthermore new strategies to achieve
2024-05-15
Furthermore, new strategies to achieve a total androgen deprivation namely by blocking either androgen biosynthesis as well as AR are being considered and should be a relevant topic in the near future. A successful example of this approach is galeterone (159), which not only inhibits the CYP17 enzym
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pelitinib Axl which belongs to the
2024-05-15
Axl, which belongs to the Tyro-Axl-Mer (TAM) family of RTKs, has been reported to regulate a variety of physiological processes including cell survival, proliferation, migration and adhesion, through the activation of the phosphoinositide 3-kinase (PI3K)/V-akt murine thymoma viral oncogene homolog (
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Since the beginning of s more than papers
2024-05-15
Since the beginning of 1990s, more than 17,000 papers about physiological relevance of antioxidants have been published according to data from web of science. Based on the available literature, it seems that assessing the antioxidant potential of food by means of in vitro assays or solely epidemiolo
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Besides above mentioned UV visible and fluorescence spectros
2024-05-15
Besides above-mentioned UV–visible and fluorescence spectroscopy methods, electron paramagnetic resonance (EPR) spectroscopy, the only analytical method that detect compounds having unpaired electrons known as free radicals, was rarely used in antioxidant capacity measurement (Amarowicz et al., 2004
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At Johns Hopkins Aramco Health JHAH we started an
2024-05-15
At Johns Hopkins Aramco Health (JHAH), we started an ASP in 2011 with an educational program of physicians and pharmacist. The program was enhanced mid-2012 with the following interventions: a re-designed antibiotic sensitivity report [2], intravenous to oral conversion program, vancomycin pharmacok
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In addition unconventional mechanisms of internalization can
2024-05-15
In addition, unconventional mechanisms of internalization cannot be ignored. It is generally believed that the conventional homologous internalization of a GPCR depends on the activation of G proteins, since GRK activation requires the pre-activation of G proteins (Fig. 2). Feng et al. demonstrated
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minocycline hydrochloride receptor Second the phosphorylatio
2024-05-15
Second, the phosphorylation events (e.g., α-Thr172 and β-Ser108) needed for AMPK activation by small molecules binding at the ADaM or other sites remains unclear. Within the β-GBD, phosphorylation of β1-Ser108 was shown to be required for the activation by small molecules binding in the ADaM site, s
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GSK2126458 Dose Response Studies Against Puromycin Sensitive
2024-05-15
Dose–Response Studies Against Puromycin–Sensitive Aminopeptidase (PSA). PSA is a ubiquitous metallopeptidase encoded by the NPEPPS gene with subcellular distribution in the cytosol and nucleus [49]. Comprising of a 919 amino GSK2126458 sequence, it has a broad substrate specificity, and is responsi
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The binding of TQ to
2024-05-14
The binding of TQ to hsALDH changes the characteristic amyloid beta protein spectrum of the enzyme. Therefore, TQ forms a complex with hsALDH and changes its absorption properties [39]. Ksv and Kb values indicate that the binding of TQ to hsALDH is very strong and of the order of static binding (com
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AdipoR and AdipoR have been reported
2024-05-14
AdipoR1 and AdipoR2 have been reported to be present in almost all type of tissues and low Bafetinib levels have been observed in white adipose tissue (Inukai et al., 2005). These receptors have been observed to become deregulated with the onset of obesity, resulting in a reduced level of APN expres
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In young animals the HT A receptor
2024-05-14
In young animals, the 5-HT2A Ramelteon antagonist ketanserin, at relatively low concentrations, shifted 5-HT concentration-response curves rightward, suggesting a role for 5-HT2A receptors in mediating 5-HT-induced contractions of the ureter. The slopes of the ketanserin Schild plots for the antago
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gamma secretase inhibitor Control of retinal vascularization
2024-05-14
Control of retinal vascularization during development and OIR likely involves close interactions among endothelial cells, neurons and glial gamma secretase inhibitor (microglial and astrocytes) (see Fig. 2). In particular, the interaction between endothelial tip cells and astrocytes plays a critica
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tie2 In vitro studies with soman inhibited non aged AChE
2024-05-14
In vitro studies with soman-inhibited, non-aged AChE revealed a species dependent reactivating potency of HI-6 and MMB-4. With guinea pig AChE second order reactivation rate constants of 0.051 and 0.038mM−1min−1 were determined for HI-6 and MMB-4, respectively (Luo et al., 2007). Corresponding value
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The next level of possible correlation and
2024-05-14
The next level of possible correlation and comparison between the α7 and 5HT3 receptors is at the subunit arrangement and protein folding. Crystal structures of the nicotinic and serotoninergic Phentolamine Mesylate mg receptors [45], [46] reinforced the concept of similarities between these familie
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