Synthesis of psoralen derivatives and their blocking effect of hKv1.5 channel

2007 ◽  
Vol 30 (2) ◽  
pp. 155-160 ◽  
Author(s):  
Jae Soon Eun ◽  
Kwang Sik Kim ◽  
Han Na Kim ◽  
Seon Ah Park ◽  
Tian-Ze Ma ◽  
...  
1962 ◽  
Vol 39 (4) ◽  
pp. 527-538 ◽  
Author(s):  
Pavo Hedner ◽  
Claus Rerup

ABSTRACT Measurements of plasma corticosteroid levels and adrenal ascorbic acid concentration in steroid blocked and hypophysectomized rats were performed. It was found that prednisolone and dexamethasone were effective in blocking endogenous corticotrophin release within 3–4 hours after subcutaneous injection. These agents also prevented completely the normally occurring rise in plasma corticoid levels after exposure of the rats to ether. Abdominal surgery (unilateral adrenalectomy) resulted in a slight but significant rise in plasma corticoid levels in spite of dexamethasone blockade. The values of adrenal ascorbic acid were not affected significantly. The blocking effect of two daily subcutaneous injections of a high dose of dexamethasone persisted for about one week after the last injection. The sensitivity of the plasma corticoid response was essentially the same in hypophysectomized and dexamethasone blocked rats. The lower part of the log dose response curve was found to be clearly non-linear in the plasma corticoid method following intravenous corticotrophin injection. As a consequence the dose level in quantitative assays of intravenously injected corticotrophin are, in our hands, of the same order as in the adrenal ascorbic acid depletion method.


2016 ◽  
Vol 11 (1) ◽  
pp. 30-37 ◽  
Author(s):  
A.A. Rakhimov ◽  
A.T. Akhmetov

The paper presents results of hydrodynamic and rheological studies of the inverse water hydrocarbon emulsions. The success of the application of invert emulsions in the petroleum industry due, along with the high viscosity of the emulsion, greatly exceeding the viscosity of the carrier phase, the dynamic blocking effect, which consists in the fact that the rate of flow of emulsions in capillary structures and cracks falls with time to 3-4 orders, despite the permanent pressure drop. The reported study shows an increase in viscosity with increasing concentration or dispersion of emulsion. The increase in dispersion of w/o emulsion leads to an acceleration of the onset of dynamic blocking. The use of microfluidic devices, is made by soft photolithography, along with high-speed photography (10,000 frames/s), allowed us to see in the blocking condition the deformation of the microdroplets of water in inverse emulsion prepared from simple chemical compounds.


Author(s):  
Hsiang-Yun Chen

This chapter addresses the assumed connection between de se attitude ascription and logophoricity in the case of Chinese ziji. It is widely believed that logophors are among the paradigm cases of de se marking, and that long-distance ziji is logophoric. Drawing on a critical examination of a variety of analyses, this chapter argues that long-distance anaphora, de se interpretation, and logophoric marking are overlapping but distinct phenomena. Even if ziji is logophoric, it does not automatically trigger de se requirement. A de se-neutral analysis of ziji is consistent with pragmatic derivations of interpretations that emphasize the self. The findings point to a new approach to long-distance binding, and identify the blocking effect as the key issue for further research.


Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 57
Author(s):  
Zhi-Ling Zhu ◽  
Xiao-Dan Qiu ◽  
Shuo Wu ◽  
Yi-Tong Liu ◽  
Ting Zhao ◽  
...  

The novel coronavirus disease (2019-nCoV) has been affecting global health since the end of 2019, and there is no sign that the epidemic is abating. Targeting the interaction between the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) spike protein and the human angiotensin-converting enzyme 2 (ACE2) receptor is a promising therapeutic strategy. In this study, surface plasmon resonance (SPR) was used as the primary method to screen a library of 960 compounds. A compound 02B05 (demethylzeylasteral, CAS number: 107316-88-1) that had high affinities for S-RBD and ACE2 was discovered, and binding affinities (KD, μM) of 02B05-ACE2 and 02B05-S-RBD were 1.736 and 1.039 μM, respectively. The results of a competition experiment showed that 02B05 could effectively block the binding of S-RBD to ACE2 protein. Furthermore, pseudovirus infection assay revealed that 02B05 could inhibit entry of SARS-CoV-2 pseudovirus into 293T cells to a certain extent at nontoxic concentration. The compoundobtained in this study serve as references for the design of drugs which have potential in the treatment of COVID-19 and can thus accelerate the process of developing effective drugs to treat SARS-CoV-2 infections.


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