Development and optimization of a new synthetic process for lorcaserin

A two-step process to synthesize racemic lorcaserin was developed from 2-(4-chlorophenyl)ethanol via formation of bromide or tosylate derivatives. These derivatives were reacted with allylamine in neat conditions to provide pure N-(4-chlorophenethyl)allylammonium chloride. This compound was cyclized in neat conditions using aluminum or zinc chloride to give racemic lorcaserin. After resolution of enantiomers, the wrong enantiomer was racemized and recycled to give new R-lorcaserin.     

Field test of an automated radio‐telemetry system: tracking local space use of aerial insectivores

Documenting local space use of birds that move rapidly, but are too small to carry GPS tags, such as swallows and swifts, can be challenging. For these species, tracking methods such as manual radio‐telemetry and visual observation are either inadequate or labor‐ and time‐intensive. Another option is use of an automated telemetry system, but equipment for such systems can be costly when many receivers are used. Our objective, therefore, was to determine if an automated radio‐telemetry system, consisting of just two receivers, could provide an alternative to manual tracking for gathering data on local space use of six individuals of three species of aerial insectivores, including one Cliff Swallow (Petrochelidon pyrrhonota), one Eastern Phoebe (Sayornis phoebe), and four Barn Swallows (Hirundo rustica). We established automated radio‐telemetry systems at three sites near the city of Peterborough in eastern Ontario, Canada, from May to August 2015. We evaluated the location error of our two‐receiver system using data from moving and stationary test transmitters at known locations, and used telemetry data from the aerial insectivores as a test of the system's ability to track rapidly moving birds under field conditions. Median location error was ~250 m for automated telemetry test locations after filtering. More than 90% of estimated locations had large location errors and were removed from analysis, including all locations > 1 km from receiver stations. Our automated telemetry receivers recorded 17,634 detections of the six radio‐tagged birds. However, filtering removed an average of 89% of bird location estimates, leaving only the Cliff Swallow with enough locations for analysis of space use. Our results demonstrate that a minimal automated radio‐telemetry system can be used to assess local space use by small, highly mobile birds, but the resolution of the data collected using only two receiver stations was coarse and had a limited range. To improve both location accuracy and increase the percentage of usable location estimates collected, we suggest that, in future studies, investigators use receivers that simultaneously record signals detected by all antennas, and use of a minimum of three receiver stations with more antennas at each station.     

The Effects of Mobile Phone Radiofrequency Radiation on Cochlear Stria Marginal Cells in Sprague–Dawley Rats

To investigate the possible mechanisms for biological effects of 1,800 MHz mobile radiofrequency radiation (RFR), the radiation-specific absorption rate was applied at 2 and 4 W/kg, and the exposure mode was 5 min on and 10 min off (conversation mode). Exposure time was 24 h short-term exposure. Following exposure, to detect cell DNA damage, cell apoptosis, and reactive oxygen species (ROS) generation, the Comet assay test, flow cytometry, DAPI (4′,6-diamidino-2-phenylindole dihydrochloride) staining, and a fluorescent probe were used, respectively. Our experiments revealed that mobile phone RFR did not cause DNA damage in marginal cells, and the rate of cell apoptosis did not increase (P > 0.05). However, the production of ROS in the 4 W/kg exposure group was greater than that in the control group (P < 0.05). In conclusion, these results suggest that mobile phone energy was insufficient to cause cell DNA damage and cell apoptosis following short-term exposure, but the cumulative effect of mobile phone radiation still requires further confirmation. Activation of the ROS system plays a significant role in the biological effects of RFR. Bioelectromagnetics. © 2020 The Authors. Bioelectromagnetics published by Wiley Periodicals, Inc.     

High-performance liquid chromatography-based method to evaluate kinetics of glucosinolate hydrolysis by Sinapis alba myrosinase

Isothiocyanates (ITCs) are one of several hydrolysis products of glucosinolates, plant secondary metabolites that are substrates for the thioglucohydrolase myrosinase. Recent pursuits toward the development of synthetic non-natural ITCs have consequently led to an exploration of generating these compounds from non-natural glucosinolate precursors. Evaluation of the myrosinase-dependent conversion of select non-natural glucosinolates to non-natural ITCs cannot be accomplished using established ultraviolet–visible (UV–Vis) spectroscopic methods. To overcome this limitation, an alternative high-performance liquid chromatography (HPLC)-based analytical approach was developed where initial reaction velocities were generated from nonlinear reaction progress curves. Validation of this HPLC method was accomplished through parallel evaluation of three glucosinolates with UV–Vis methodology. The results of this study demonstrate that kinetic data are consistent between both analytical methods and that the tested glucosinolates respond similarly to both Michaelis–Menten and specific activity analyses. Consequently, this work resulted in the complete kinetic characterization of three glucosinolates with Sinapis alba myrosinase, with results that were consistent with previous reports.