Lower and upper flammability limits (LFL and UFL) and explosion pressures of binary alkane-N 2 O mixtures are investigated. Binary alkane-N 2 O mixtures exhibit smaller LFLs than corresponding binary alkane-O 2 mixtures. For binary alkane-N 2 O mixtures, LFL and UFL can be predicted using the Le Chatelier's formulae.
A general and facile synthesis of enantiopure 1-deoxyazasugars was achieved from stereoselective dihydroxylation of a common synthetic intermediate, piperidine ring fused oxazolidin-2-one, originating from a commercially available starting substrate, chiral aziridine-2-carboxylate, in high yields.
LB30870, a new direct thrombin inhibitor, showed 80% reduction in oral bioavailability in fed state. The present study aims to propose trypsin binding as a mechanism for such negative food effect and demonstrate a prodrug approach to mitigate food effect. Effect of food composition on fed state oral bioavailability of LB30870 was studied in dogs. Various prodrugs were synthesized, and their solubility, permeability, and trypsin binding affinity were measured. LB30870 and prodrugs were subject to cocrystallization with trypsin, and the X-ray structures of cocrystals were determined. Food effect was studied in dogs for selected prodrugs. Protein or lipid meal appeared to affect oral bioavailability of LB30870 in dogs more than carbohydrate meal. Blocking both carboxyl and amidine groups of LB30870 resulted in trypsin Ki values orders of magnitude higher than that of LB30870. Prodrugs belonged to either Biopharmaceutical Classification System I, II, or III. X-ray crystallography revealed that prodrugs did not bind to trypsin, but instead their hydrolysis product at the amidine blocking group formed cocrystal with trypsin. A prodrug with significantly less food effect than LB30870 was identified. Binding of prodrugs to food components such as dietary fiber appeared to counteract the positive effect brought with the prodrug approach. Further formulation research is warranted to enhance the oral bioavailability of prodrugs. In conclusion, this study is the first to demonstrate that the negative food effect of LB30870 can be attributed to trypsin binding. Trypsin binding study is proposed as a screening tool during lead optimization to minimize food effect.
The purposes of this study are to investigate the factors influencing evacuation behavior, means of transportation, effective information tools, and country and gender effects in cases of toxic gas release. In this study, questionnaire surveys were conducted among Korean (n=158) and Japanese (n=108) younger adults. Explanatory factor analyses revealed that the extracted factor structures for the Korean and Japanese samples were similar. Surveys indicated that approximately three-quarters of Koreans (74%) chose "vehicle and motorcycle" as means of transportation, and 36% chose "Social network service and Internet" as effective information tools. Korean younger adults significantly rated knowledge and fear regarding toxic gas and chemical plants and lower anxiety about evacuation higher than Japanese younger adults. Gender effects were also identified regarding knowledge and anxiety.
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