Cystic Fibrosis: A New Target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines

The pharmacology of the cystic fibrosis transmembrane conductance regulator (CFTR) Cl(-) channel has attracted significant interest in recent years with the aim to search for rational new therapies for diseases caused by CFTR malfunction. Mutations that abolish the function of CFTR cause the life-threatening genetic disease cystic fibrosis (CF). The most common cause of CF is the deletion of phenylalanine 508 (ΔF508) in the CFTR chloride channel. Felodipine, nifedipine, and other antihypertensive 1,4-dihydropyridines (1,4-DHPs) that block L-type Ca(2+) channels are also effective potentiators of CFTR gating, able to correct the defective activity of ΔF508 and other CFTR mutants ( Mol. Pharmacol. 2005 , 68 , 1736 ). For this purpose, we evaluated the ability of the previously and newly synthesized 4-imidazo[2,1-b]thiazoles-1,4-dihydropyridines without vascular activity and inotropic and/or chronotropic cardiac effects ( J. Med. Chem. 2008 , 51 , 1592 ) to enhance the activity of ΔF508-CFTR. Our studies indicate compounds 17, 18, 20, 21, 38, and 39 as 1,4-DHPs with an interesting profile of activity

A global database of lake surface temperatures collected by in situ and satellite methods from 1985–2009

Peer reviewe

Global data set of long-term summertime vertical temperature profiles in 153 lakes

peer reviewedClimate change and other anthropogenic stressors have led to long-term changes in the thermal structure, including surface temperatures, deepwater temperatures, and vertical thermal gradients, in many lakes around the world. Though many studies highlight warming of surface water temperatures in lakes worldwide, less is known about long-term trends in full vertical thermal structure and deepwater temperatures, which have been changing less consistently in both direction and magnitude. Here, we present a globally-expansive data set of summertime in-situ vertical temperature profiles from 153 lakes, with one time series beginning as early as 1894. We also compiled lake geographic, morphometric, and water quality variables that can influence vertical thermal structure through a variety of potential mechanisms in these lakes. These long-term time series of vertical temperature profiles and corresponding lake characteristics serve as valuable data to help understand changes and drivers of lake thermal structure in a time of rapid global and ecological change. © 2021, The Author(s)

A global database of lake surface temperatures collected by in situ and satellite methods from 1985–2009

Global environmental change has influenced lake surface temperatures, a key driver of ecosystem structure and function. Recent studies have suggested significant warming of water temperatures in individual lakes across many different regions around the world. However, the spatial and temporal coherence associated with the magnitude of these trends remains unclear. Thus, a global data set of water temperature is required to understand and synthesize global, long-term trends in surface water temperatures of inland bodies of water. We assembled a database of summer lake surface temperatures for 291 lakes collected in situ and/or by satellites for the period 1985–2009. In addition, corresponding climatic drivers (air temperatures, solar radiation, and cloud cover) and geomorphometric characteristics (latitude, longitude, elevation, lake surface area, maximum depth, mean depth, and volume) that influence lake surface temperatures were compiled for each lake. This unique dataset offers an invaluable baseline perspective on global-scale lake thermal conditions as environmental change continues

Global data set of long-term summertime vertical temperature profiles in 153 lakes

Climate change and other anthropogenic stressors have led to long-term changes in the thermal structure, including surface temperatures, deepwater temperatures, and vertical thermal gradients, in many lakes around the world. Though many studies highlight warming of surface water temperatures in lakes worldwide, less is known about long-term trends in full vertical thermal structure and deepwater temperatures, which have been changing less consistently in both direction and magnitude. Here, we present a globally-expansive data set of summertime in-situ vertical temperature profiles from 153 lakes, with one time series beginning as early as 1894. We also compiled lake geographic, morphometric, and water quality variables that can influence vertical thermal structure through a variety of potential mechanisms in these lakes. These long-term time series of vertical temperature profiles and corresponding lake characteristics serve as valuable data to help understand changes and drivers of lake thermal structure in a time of rapid global and ecological change

Global data set of long-term summertime vertical temperature profiles in 153 lakes

Measurement(s) : temperature of water, temperature profile Technology Type(s) : digital curation Factor Type(s) : lake location, temporal interval Sample Characteristic - Environment : lake, reservoir Sample Characteristic - Location : global Machine-accessible metadata file describing the reported data: https://doi.org/10.6084/m9.figshare.14619009Climate change and other anthropogenic stressors have led to long-term changes in the thermal structure, including surface temperatures, deepwater temperatures, and vertical thermal gradients, in many lakes around the world. Though many studies highlight warming of surface water temperatures in lakes worldwide, less is known about long-term trends in full vertical thermal structure and deepwater temperatures, which have been changing less consistently in both direction and magnitude. Here, we present a globally-expansive data set of summertime in-situ vertical temperature profiles from 153 lakes, with one time series beginning as early as 1894. We also compiled lake geographic, morphometric, and water quality variables that can influence vertical thermal structure through a variety of potential mechanisms in these lakes. These long-term time series of vertical temperature profiles and corresponding lake characteristics serve as valuable data to help understand changes and drivers of lake thermal structure in a time of rapid global and ecological change

Dielectric spectra of some common solvents in the microwave region. Water and lower alcohols

Precise complex permittivity spectra of the hydrogen-bonding liqs. water, methanol, ethanol, 1-propanol, and 2-propanol have been detd. in the frequency range 0.95-8. GHz. The dielec. relaxation behavior of water is governed by two exponentials, whereas three discrete dispersion steps are found for the alcs

Molecular processes in electrolyte solutions at microwave frequencies

The microwave dispersion and absorption spectra are discussed for various protic and aprotic electrolyte solns. and their solvents over large frequency ranges, in general 0.9-90 GHz. Wider frequency ranges are covered for water (0.9-409 GHz) and for methanol, N-methylformamide, and N,N-dimethylformamide (all 0.9-293 GHz). The role of insufficient frequency coverage is critically discussed. Permittivities and relaxation times of the underlying relaxation processes are compared for electrolyte solns. of the hydrogen-bonding solvents water, methanol and higher alcs., formamide, N-methylformamide, and the dipolar aprotic solvents acetonitrile, propylene carbonate, DMSO, and N,N-dimethylformamide. The hydrogen-bonding mode at τ ≃1 ps is not affected by the addn. of alkali metal and tetrabutylammonium salts, in contrast to the bulk and the internal relaxation of the H-bonded chains; NH4+ in methanol produces peculiar effects. For 1:1-electrolytes ion-pair formation is detectable in all solvents of static permittivity below 50; the concn. dependence of the corresponding relaxation time permits sepn. into rotational and kinetic modes of ion-pair formation and decompn

Freshwater ecosystems profit from activated carbon-based wastewater treatment across various levels of biological organisation in a short timeframe

Background Wastewater treatment plants are known as major sources for the release of micropollutants and bacteria into surface waters. To reduce this contaminant and microbial input, new technologies for effluent treatment have become available. The present paper reports the chemical, microbiological, biochemical, and biological effects of upgrading a wastewater treatment plant (WWTP) with a powdered activated carbon stage in the catchment area of the Schussen River, the largest German tributary of Lake Constance. Data were obtained prior to and after the upgrade between 2011 and 2017. Results After the upgrading, the release of antibiotic resistant and non-resistant bacteria, micropollutants, and their effect potentials was significantly lower in the effluent. In addition, in the Schussen River downstream of the wastewater treatment plant, reduced concentrations of micropollutants were accompanied by both a significantly improved health of fish and invertebrates, along with a better condition of the macrozoobenthic community. Conclusions The present study clearly provides evidence for the causality between a WWTP upgrade by powdered activated carbon and ecosystem improvement and demonstrates the promptness of positive ecological changes in response to such action. The outcome of this study urgently advocates an investment in further wastewater treatment as a basis for decreasing the release of micropollutants and both resistant and non-resistant bacteria into receiving water bodies and, as a consequence, to sustainably protect river ecosystem health and drinking water resources for mankind in the future