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排序方式: 共有393条查询结果,搜索用时 15 毫秒
1.
Viktoria M. S. Kjær Loukas Ieremias Dr. Viktorija Daugvilaite Dr. Michael Lückmann Prof. Thomas M. Frimurer Prof. Trond Ulven Prof. Mette M. Rosenkilde Dr. Jon Våbenø 《ChemMedChem》2021,16(17):2623-2627
The G protein-coupled receptor GPR183/EBI2, which is activated by oxysterols, is a therapeutic target for inflammatory and metabolic diseases where both antagonists and agonists are of potential interest. Using the piperazine diamide core of the known GPR183 antagonist (E)-3-(4-bromophenyl)-1-(4-(4-methoxybenzoyl)piperazin-1-yl)prop-2-en-1-one (NIBR189) as starting point, we identified and sourced 79 structurally related compounds that were commercially available. In vitro screening of this compound collection using a Ca2+ mobilization assay resulted in the identification of 10 compounds with agonist properties. To enable establishment of initial structure-activity relationship trends, these were supplemented with five in-house compounds, two of which were also shown to be GPR183 agonists. Taken together, our findings suggest that the agonist activity of this compound series is dictated by the substitution pattern of one of the two distal phenyl rings, which functions as a molecular efficacy-switch. 相似文献
2.
Douglas E. Olesen 《The Electricity Journal》1995,8(10)
Technology developments on the horizon promise to transform the electricity industry far from its present shape and structure. But, just as technology has played a critical role in pushing the industry to its present thrust toward competition and vertical de-integration, a sensible technology policy can make a utility or power supplier a winmer tomorrow. 相似文献
3.
The authors present a new traveling wave method for calculating the linewidth, the frequency tuning efficiency, and a mode stability parameter for a general class of laser-diode structures. The method leads to simple semianalytic expressions which allow an easy numerical determination of the three parameters 相似文献
4.
Mette B. Let Charlotte Jacobsen Edwin N. Frankel Anne S. Meyer 《European Journal of Lipid Science and Technology》2003,105(9):518-528
The oxidative deterioration of milk emulsions supplemented with 1.5 wt‐% fish oil was investigated by sensory evaluation and by determining the peroxide value and volatile oxidation products after cold storage. Two types of milk emulsions were produced, one with a highly unsaturated tuna oil (38 wt‐% of n‐3 fatty acids) and one with cod liver oil (26 wt‐% of n‐3 fatty acids). The effect of added calcium disodium ethylenediaminetetraacetate (EDTA) on oxidation was also investigated. Emulsions based on cod liver oil with a slightly elevated peroxide value (1.5 meq/kg) oxidised significantly faster than the tuna oil emulsions, having a lower initial peroxide value (0.1 meq/kg). In the tuna oil emulsions the fishy off‐flavour could not be detected throughout the storage period. Addition of 5—50 ppm EDTA significantly reduced the development of volatile oxidation products in the cod liver oil emulsions, indicating that metal chelation with EDTA could inhibit the decomposition of lipid hydroperoxides in these emulsions. This study showed that an oxidatively stable milk emulsion containing highly polyunsaturated tuna fish oil could be prepared without significant fishy off‐flavour development upon storage, provided that the initial peroxide value was sufficiently low. 相似文献
5.
To make health care more responsive to patient needs, insight into patient priorities is needed. A systematic literature review, using electronic and manual searches, was made of studies on patient priorities with regard to primary health care. Data-extraction was performed by two researchers, followed by systematic analyses of study features. 57 studies were included. The aspects of care and methods used showed a wide variation. Aspects most often included were "informativeness", "humaneness" and "competence/accuracy". Based on an analysis of 19 studies, the following aspects were seen by patients as most important in more than 50% of the studies that included them: "humaneness", "competence/accuracy", "patients' involvement in decisions", "time for care", "other aspects of availability/accessibility", "informativeness", "exploring patients' needs", "other aspects of relation and communication" and "availability of special services". 相似文献
6.
Rasmussen CD Jørgensen MB Carneiro IG Flyvholm MA Olesen K Søgaard K Holtermann A 《Ergonomics》2012,55(2):256-264
Worksite health promotion is seldom offered to workers who are low-educated and multi-ethnic, possibly due to an assumption that they are more reluctant to participate. Furthermore, little has been done to promote health at female-dominated workplaces. The main aim of this study was to investigate differences in participation among immigrant and Danish cleaners throughout a 1-year randomised controlled study tailored to cleaners and carried out in predominantly female workplaces. No significant differences in ethnicity were found in consent and participation throughout the 1-year intervention. Dropout was equally distributed among Danish and immigrant cleaners. This study indicates that a worksite health promotion intervention among a female-dominated, high-risk occupation such as cleaning can be equally appealing for Danes and immigrants. PRACTITIONER SUMMARY: This study provides insight about participation of Danish and immigrant cleaners in a worksite health promotion intervention in a predominantly female occupation. For attaining high participation and low dropout in future worksite health promotion interventions among cleaners, the intervention ought to not only target the ethnic background of the workers, but also to be specifically tailored to the job group. 相似文献
7.
8.
Bioavailability Studies and in vitro Profiling of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor UCPH‐102 下载免费PDF全文
Dr. Isabell Haym Dr. Tri H. V. Huynh Dr. Stinne W. Hansen Dr. Martin H. F. Pedersen Dr. Josep A. Ruiz Dr. Mette N. Erichsen Dr. Mikko Gynther Walden E. Bjørn‐Yoshimoto Dr. Bjarke Abrahamsen Dr. Jesper F. Bastlund Dr. Christoffer Bundgaard Anette L. Eriksen Prof. Anders A. Jensen Prof. Lennart Bunch 《ChemMedChem》2016,11(4):403-419
Although the selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor UCPH‐101 has become a standard pharmacological tool compound for in vitro and ex vivo studies in the EAAT research field, its inability to penetrate the blood–brain barrier makes it unsuitable for in vivo studies. In the present study, per os (p.o.) administration (40 mg kg?1) of the closely related analogue UCPH‐102 in rats yielded respective plasma and brain concentrations of 10.5 and 6.67 μm after 1 h. Three analogue series were designed and synthesized to improve the bioavailability profile of UCPH‐102, but none displayed substantially improved properties in this respect. In vitro profiling of UCPH‐102 (10 μm ) at 51 central nervous system targets in radioligand binding assays strongly suggests that the compound is completely selective for EAAT1. Finally, in a rodent locomotor model, p.o. administration of UCPH‐102 (20 mg kg?1) did not induce acute effects or any visible changes in behavior. 相似文献
9.
The natural antimicrobial compound allyl isothiocyanate (AITC), found in mustard oil, is effective against cheese-related fungi both on laboratory media and cheese. Penicillium commune, Penicillium roqueforti, and Aspergillus flavus were more sensitive to AITC when it was added just after the spores had completed 100% germination and branching had started on Czapek yeast extract agar than were spores in the dormant phase. The use of 1 AITC label (Wasaouro interior labels, LD30D, 20 by 20 mm) in combination with atmospheric air in the packaging extended the shelf life of Danish Danbo cheese from 4 1/2 to 13 weeks. Two AITC labels extended the shelf life from 4 1/2 to 28 weeks. Both 1 and 2 labels in combination with modified atmosphere packaging extended the shelf life of the cheese from 18 to 28 weeks. This study showed that AITC was absorbed in the cheese, but it was not possible to detect any volatile breakdown products from AITC in the cheese. Cheese stored for up to 12 weeks with an AITC label had an unacceptable mustard flavor. The mustard flavor decreased to an acceptable level between weeks 12 and 28. Cheese stored in atmospheric air had a fresher taste without a CO2 off-flavor than did cheese stored in modified atmosphere packaging. AITC may be a good alternative to modified atmosphere packaging for cheese. The extended shelf life of cheese in the package is very desirable: the cheese can be transported longer distances, and the packaging can be used for the final maturing of the cheese. Furthermore, AITC can address problems such as pinholes and leaking seals in cheese packaging. 相似文献
10.
Mette B. Petersen Jeanette Pedersen Dinah L. Holm Matthew Denwood Liza R. Nielsen 《Journal of dairy science》2018,101(8):7383-7396
Mycoplasma bovis is an important pathogen causing disease and substantial economic losses in cattle. However, knowledge of the dynamics of antibody responses in individual cows in the face of an outbreak is currently extremely limited. The use of commercial antibody tests to support clinical decision-making and for surveillance purposes is therefore challenging. Our objective was to describe the dynamics of M. bovis antibody responses in 4 Danish dairy herds experiencing an acute outbreak of M. bovis-associated disease, and to compare the antibody dynamics between dairy cows with different disease manifestations. A total of 120 cows were examined using a standardized clinical protocol and categorized into 4 disease groups: “mastitis,” “systemic,” “nonspecific,” and “none.” Paired blood and milk samples were collected and tested using a commercial M. bovis antibody–detecting ELISA. Plots of raw data and generalized additive mixed models with cow and herd as random effects were used to describe serum and milk antibody dynamics relative to the estimated time of onset of clinical disease. Cows with mastitis had high optical density measurement (ODC%) of antibodies in both milk and serum at disease onset. The estimated mean ODC% in milk was below the manufacturer's cut-off for the other groups for the entire study period. The estimated mean serum ODC% in the “systemic” group was high at onset of disease and stayed above the cut-off until 65 d after disease onset. However, the lower 95% confidence interval (CI) for the mean ODC% was only above the manufacturer's cut-off between 7 and 17 d after onset of disease. The CI of the “systemic” and “none” groups did not overlap at any time between the day of disease onset and 65 d after disease onset, and the estimated mean ODC% for both the “nonspecific” and “none” groups were generally below the cut-off for the majority of the study period. In conclusion, the serum antibody responses were highly dynamic and showed a high level of variation between individual cows. This strongly suggests that serology is unlikely to be useful for individual diagnosis of M. bovis-associated disease in dairy cows. However, it might still be useful for herd- or group-level diagnosis. Antibodies in milk were only increased in cows with M. bovis mastitis, indicating that milk antibody measurements only have diagnostic utility for cows with mastitis. 相似文献