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Hydroxyfasudil H R antagonism can prevent
2021-12-06

H3R antagonism can prevent seizure development and improve working memory through the activation of histaminergic neurons (Huang et al., 2004, Zhang et al., 2003). In addition, we have recently found that H3R antagonism protects against ischemia-reperfusion injury via histamine-independent mechanism
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Receptor guanylyl cyclases play essential roles in cardiovas
2021-12-06

Receptor guanylyl cyclases play essential roles in cardiovascular and gastrointestinal (patho-)physiology, reproduction biology, cell proliferation, bone growth and sensory signal transduction and, therefore, are important pharmacological targets. Accordingly, the receptor guanylyl cyclase agonists
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The Fe deficiency treatment significantly increased
2021-12-06

The Fe-deficiency treatment significantly increased the shoot/root Fe ratios in both WT and transgenic lines (Fig. 5C), which implied that the Fe distribution from root to shoot may be an adaptive mechanism or stress response in tomato plants. Thus, the overexpression of GSNOR had a positive effect
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br Other Functions of HCA Receptors HCA receptors in particu
2021-12-06

Other Functions of HCA Receptors HCA receptors, in particular HCA1, are expressed in various primary tumor Arecaidine but-2-ynyl ester tosylate 77, 78, 79. This is of interest, as most solid tumors show increased glucose uptake and lactate formation even under normoxic conditions, with lactate co
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Modulation of the cannabinoid system has been reported to ex
2021-12-06

Modulation of the cannabinoid system has been reported to exert anti-parkinsonian properties through different mechanisms. On one hand, cannabinoids have neuroprotective properties in different rodent models of PD, both through a CB1/CB2 receptor-independent mechanism (Lastres-Becker et al., 2005) a
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Functional studies based on patch clamp electrophysiology pr
2021-12-06

Functional studies based on patch-clamp electrophysiology provide additional information on the active state of GlyR α1. Current-voltage measurements from single QS 11 in outside-out patches at symmetric 145-mM chloride concentration yielded a unitary conductance of 86 pS for the main open state an
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muscarinic receptor antagonists Free fatty acid receptor FFA
2021-12-06

Free fatty muscarinic receptor antagonists receptor 1 (FFAR1, also known as GPR40) belongs to the family of G protein-coupled receptors (GPCRs) and was de-orphanized in 2003 as a receptor for medium-to long-chain free fatty acids (FFAs) [9,10]. Mainly expressed in beta cells of pancreatic islets, G
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Up to now the research about
2021-12-06

Up to now, the research about the effect of PAs on inhibiting carbohydrase activity in vitro or reducing blood sugar level in vivo was mainly reported in PAs from grape seeds, Lepisanthes alata (Malay cherry) leaves, sorghum, pomegranate, cranberry and persimmon (Banerji and Banerjee, 2016, Barrett
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In order to test whether the
2021-12-06

In order to test whether the enhanced hyperpolarization in the presence of increasing amounts of extracellular Ca2+ could be due to an ionophore effect of NS309, red cell uptake of 45Ca and partition of 45Ca into a water/n-octanol phase +/−100 μM NS309 were determined. However, no indication of iono
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GSK 650394 Hypocotyl development is a crucial phase of early
2021-12-04

Hypocotyl development is a crucial phase of early vegetative growth that influences seedling vigor contributing to fitness and productivity of a plant system (Stinchcombe and Schmitt, 2006; Luo et al., 2017). The development of a hypocotyl is characterized by an initial slow growth phase followed by
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The Ala to Leu substitution would reduce the
2021-12-04

The Ala116 to Leu110 substitution would reduce the size of the active-site cavity disfavoring the production of longer allylic compounds as a result of steric hindrance, according to the observations of Poulter and co-workers [29], [30]. However, this explanation appears to be unlikely since several
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br Acknowledgement This research was supported by Basic Scie
2021-12-04

Acknowledgement This research was supported by Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Education, Science and Technology (NRF-2016R1A2B4012818). Oral ionophore is the most popular administration route due to good patients’ com
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A biochemical characterisation of this functionally crucial
2021-12-04

A biochemical characterisation of this functionally crucial LSD1-p53 interaction is the focus of this study. Using several complementary assays [29], [30], [31], [32], we find that a well-defined segment of p53-CTD is capable of binding to LSD1 active site, thereby inhibiting the enzymatic activity
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The mast cell has long been recognized as central to
2021-12-04

The mast cell has long been recognized as central to the mediation of allergic responses not least because it is the principal repository of histamine in the body. Following activation by allergens, the mast cell can release histamine as well as generate a host of additional mediators such as cystei
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In summary P P macrocyclization proved
2021-12-04

In summary, P2-P4 macrocyclization proved to be an effective strategy to drive activity in this series of HCV NS3 protease inhibitors while microsomal stability was enhanced by the introduction of steric bulk along the tether. This modification augmented the previously-described tactic of improving
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