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The more important effect of
2022-06-27
The more important effect of pitolisant is related to its wake-promoting and arousal activities as a result of enhanced BMH-21 mg release in animal models (Ligneau, Perrin, et al., 2007). Moreover, its potential in the treatment of severe excessive daytime sleepiness (EDS) in narcoleptic teenagers
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br Discussion In this study we show that
2022-06-27
Discussion In this study, we show that conditional loss of Yap/Taz in the endocardium results in a thin compact myocardium and early postnatal lethality. We also report that loss of Yap/Taz in the endocardium leads to diminished expression of Nrg1, which is a crucial endocardial-derived factor th
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The replacement of the P butyl
2022-06-27
The replacement of the P-butyl urea cap with sulfonamide derived cap had a profound effect on binding. Compound obtained by the replacement of -butyl urea P cap of compound with sulfonamide demonstrated a =34nM, a fifteen folds improvement in potency. Similarly replacement of P-butyl cap in the P cy
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ag1478 australia In order to study the role of haspin s kina
2022-06-27
In order to study the role of haspin’s kinase activity in mitosis (and other cellular processes) and its potential role in cancer, we sought to identify and optimize inhibitors. Utilizing a recently developed time-resolved fluorescence resonance energy transfer (TR-FRET) high throughput screening (H
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br Acknowledgments br Introduction Guanosine cyclic monophos
2022-06-27
Acknowledgments Introduction Guanosine 3′,5′-cyclic monophosphate (cGMP) is a signaling molecule with key roles in diverse (patho) physiological responses and processes in numerous prokaryotes and all eukaryotes. The number of reports stating the role of cGMP in different processes in plants i
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The glycine receptor is an ionotropic neurotransmitter recep
2022-06-24
The glycine receptor is an ionotropic neurotransmitter receptor coupled to a chloride ion channel. Glycine receptors are typically described as inhibitory and distributed in the spinal cord and brainstem, though mRNA transcription labelling studies in rats show expression in the hippocampus, cingula
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br Regulation of Glu transporters The pivotal role
2022-06-24
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino N-3-oxo-dodecanoyl-L-Homoserine lactone synthesis calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have
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br Introduction Atherothrombosis is associated with the pres
2022-06-24
Introduction Atherothrombosis is associated with the presence of a low-grade, subclinical smoldering inflammatory response [1]. Several inflammatory markers, among them high-sensitive C-reactive protein (hs-CRP) [2], the erythrocyte sedimentation rate (ESR) [3], fibrinogen concentrations [4], int
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The dramatic increase in the development of EAAT inhibitors
2022-06-24
The dramatic increase in the development of EAAT inhibitors and substrates over the last several years can likely be attributed to a number of experimental advances. Firstly, the isolation of the individual EAAT clones allowed each subtype to be selectively examined in well-characterized expression
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Finally it is possible that the increase in the
2022-06-24
Finally, it is possible that the increase in the number of EAAT-3-labelled cells in the DG at PD 60, when compared with the control and experimental animals at PD 14, is associated with natural changes in the number of neurons present during the postnatal development of the hippocampus (41, 42) and,
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Ulimorelin also known as TPZ is a macrocyclic
2022-06-24
Ulimorelin, also known as TPZ101, is a macrocyclic molecule that is a potent agonist of the ghrelin receptor (Hoveyda et al., 2011). Due to its ability to stimulate gastrointestinal motility, ulimorelin has been evaluated as a possible treatment in gastroparesis (Ejskjaer et al., 2010), ileus (Frase
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br Presenilins and Wnt catenin signalling Several groups hav
2022-06-24
Presenilins and Wnt/β-catenin signalling Several groups have provided substantial data indicating that PS1 acts as a negative modulator of the transcriptional activity of the β-catenin/Tcf-4 complex (Fig. 4) [120], [121], [122]. β-Catenin is a multifunctional protein that was first described as a
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It should be noted that
2022-06-24
It should be noted that the applied steered unfolding of the i-motif and G-quadruplex satisfies the conditions of Jarzynski inequality for computations of the free energy change. [41] However, in order to reproduce the free energy with an adequate quality a number of nonequilibrium unfolding transi
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br Conclusions We concluded that the inhibitory effects
2022-06-24
Conclusions We concluded that the inhibitory effects of propofol on fMMYALF-induced neutrophil activation are mediated by competition with FPR1, which inhibits receptor-mediated downstream signaling and inflammatory responses such as oxidative burst, elastase release, and chemotactic migration (F
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Herein we describe the design and optimization of
2022-06-24
Herein, we describe the design and optimization of fused-ring phenyl propanoic acids as novel GPR40 agonists, leading to the discovery of compound 40a which exhibits excellent pharmacokinetic properties, improved hepatobiliary transporter inhibition, and significant glucose-lowering efficacy during
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