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leuprolide acetate receptor Mapping and separation of the an
2021-10-25

Mapping and separation of the anti-GlyT1C epitopes allowed us to verify the existence of calpain cleavage sites in isolated mouse synaptosomes. In order to allow calcium to enter the intrasynaptosomal compartment and activate endogenous calpain, we incubated synaptosomes in hypoosmotic high (200μM)
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Given that inactivation of GLO by BAB is an
2021-10-25

Given that inactivation of GLO1 by 4BAB is an active site directed mechanism, as the transition state analogue CHG protects GLO1 against inactivation by 4BAB (Figs. 2D and S6b), we next set out to determine the amino orphan receptor that is covalently modified by 4BAB. From the X-ray crystallograph
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In the latent inhibition model a conditioned stimulus CS
2021-10-25

In the latent inhibition model, a conditioned stimulus (CS) is pre-exposed alone without any consequences (i.e., unconditioned stimulus [US]) in the pre-exposure phase. The CS is then associated with a US to form a CS-US association. The strength of the CS-induced response in the pre-exposure group
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In the latent inhibition model a conditioned stimulus CS
2021-10-25

In the latent inhibition model, a conditioned stimulus (CS) is pre-exposed alone without any consequences (i.e., unconditioned stimulus [US]) in the pre-exposure phase. The CS is then associated with a US to form a CS-US association. The strength of the CS-induced response in the pre-exposure group
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br Acknowledgements Supported by the
2021-10-25

Acknowledgements Supported by the grant from National Natural Science Funds of China (81371262). I would like to express my heartfelt gratitude to Professor Yonghua Zhu, who help language editing. Introduction Glucocorticoids are steroid hormones secreted from the adrenal glands in response t
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The effects of GHS R a blockade
2021-10-25

The effects of GHS-R1a blockade on alcohol-related outcomes have been examined in numerous preclinical experiments, utilizing various GHS-R1a antagonists (JMV 2959, [D-Lys3]-GHRP-6, BIM 28163) and rodent species (prairie vole, mouse, rat). In spite of methodological differences, the results consiste
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In order to address the
2021-10-25

In order to address the Cyp inhibition issue, we tested the possibility of further changes in the heterocycle combined with reducing the electron density in the ring system by swapping the central aniline nitrogen atom for a ketone. details the synthesis of these analogs, which started with 7-bromo
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Our own search towards aryl imidazole
2021-10-25

Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,
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br Acknowledgments The research leading to these results was
2021-10-25

Acknowledgments The research leading to these results was funded by European Community’s Seventh Framework Programme (FP7/2007-2013) under grant agreement No. 222719 – LIFECYCLE and by the Foundation for Science and Technology of Portugal (FCT), through projects PTDC/MAR-BIO/3890/2012 and PEst-C/
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Among sensitizers tested in the previous study six test chem
2021-10-25

Among 22 sensitizers tested in the previous study, six test chemicals were pre- or pro-haptens (Nepal et al., 2018a). Among 6 chemicals, hydroquinone and 2-aminophenol, strong sensitizers, were falsely classified as non-sensitizers due to the lack of metabolic activation (Nepal et al., 2018a). Liter
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Fas ligand FasL the natural ligand of
2021-10-23

Fas ligand (FasL), the natural ligand of Fas, can interact with Fas and thus induce cell apoptosis through the cascade of death signal in various cell types [8]. Additionally, Fas, which is a member of the tumor necrosis factor (TNF) receptor superfamily and death receptor family, is one kind of tra
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br Acknowledgments I thank Takeshi Sakaba for
2021-10-23

Acknowledgments I thank Takeshi Sakaba for critical reading of the manuscript and helpful comments. This work was supported by JSPS/MEXT KAKENHI Grant Numbers 17K19466, 17H03548. Introduction The oral route of drug application is the main route in pharmacology since it is easy to handle and o
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br Histamine and glycaemia Histamine is involved in a wide
2021-10-23

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 GSK 650394 and diabetes date back to the 1950s. Since that time the involvement of histamine in dia
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Decoquinate Another level of complexity within the TGF
2021-10-23

Another level of complexity within the TGF-ß/SMAD and Hippo/YAP/TAZ pathway crosstalks was recently uncovered. TGF-ß induces robust TAZ, but not YAP, protein expression in both mesenchymal and epithelial Decoquinate through a SMAD3-independent, p38/MAPK-dependent mechanism that triggers myocardin-r
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BAMB-4 The observed tendency for higher
2021-10-23

The observed tendency for higher plasma lactate levels in the aerated thermal exposure suggests increased reliance on BAMB-4 metabolism to maintain function. This finding is supported by a recent study that observed an increased ṀO2 in European perch (Perca fluviatilis) exposed to a hyperoxic rathe
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