RS-8359, (+/-)-4-(4-cyanoanilino)-5,6-dihydro-7-hydroxy-7H-cyclopenta[d]pyrimidine selectively and reversibly inhibits monoamine oxidase A (MAO-A). After oral administration of rac-RS-8359 to rats, mice, dogs, monkeys, and humans, plasma concentrations of the (R)-enantiomer were greatly higher than were those of the (S)-enantiomer in all species studied. The AUC((R)) to AUC((S)) ratios were 2.6 in rats, 3.8 in mice, 31 in dogs, and 238 in monkeys, and the (S)-enantiomer was almost negligible in human plasma. After intravenous administration of RS-8359 enantiomers to rats, the pharmacokinetic parameters showed that the (S)-enantiomer had a 2.7-fold greater total clearance (CL(t)) and a 70% shorter half-life (t(1/2)) than those for the (R)-enantiomer but had no difference in distribution volume (V(d)). No significant difference in the intestinal absorption rate was observed. The principal metabolites were the 2-keto form, possibly produced by aldehyde oxidase, the cis-diol form, and the 2-keto-cis-diol form produced by cytochrome P450 in rats, the cis-diol form in mice, RS-8359 glucuronide in dogs, and the 2-keto form in monkeys and humans. Thus, the rapid disappearance of the (S)-enantiomer from the plasma was thought to be due to the rapid metabolism of the (S)-enantiomer by different drug-metabolizing enzymes, depending on species.

The binding of (؊)-epigallocatechin gallate (EGCG), a representative natural polyphenol, to human serum albumin (HSA) and bovine serum albumin (BSA) was investigated using induced circular dichroism (

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second indoor sample (collected at a spectator's area) was 221 ppb, with a range of 1-3,175 ppb. The ratio of the indoor to outdoor NO 2 concentrations was above 1 for 95% of the rinks sampled, indicating the presence of an indoor NO 2 source (mean indoor:outdoor ratio = 20). Estimates of short-term NO 2 concentrations indicated that as many as 40% of the sampled rinks would have exceeded the World Health Organization 1-hour guideline value of 213 ppb NO 2 for indoor air.Statistically significant associations were observed between NO 2 levels and the type of fuel used to power the resurfacer, ABSTRACTAn international survey of nitrogen dioxide (NO 2 ) levels inside indoor ice skating facilities was conducted. One-week average NO 2 concentrations were measured inside and outside of 332 ice rinks located in nine countries. Each rink manager also completed a questionnaire describing the building, the resurfacing machines, and their use patterns. The (arithmetic) mean NO 2 level for all rinks in the study was 228 ppb, with a range of 1-2,680 ppb, based on a sample collected at breathing height and adjacent to the ice surface. The mean of the Brauer, Lee, Spengler, Salonen, Pennanen, Braathen, Mihalikova, Miskovic, Nozaki, Tsuzuki, Rui-Jin, Xu, Qing-Xiang, Drahonovska, and Kjaergaard Journal of the Air & Waste Management AssociationVolume 47 October 1997 the absence of a catalytic converter on a resurfacer, and the use of an ice edger. There were also indications that decreased use of mechanical ventilation, increased number of resurfacing operations per day, and smaller rink volumes were associated with increased NO 2 levels. In rinks where the main resurfacer was powered by propane, the NO 2 concentrations were higher than in those with gasoline-powered resurfacers, while the latter had NO 2 concentrations higher than in those using diesel. Rinks where the main resurfacer was electric had the lowest indoor NO 2 concentrations, similar to the levels measured outdoors.