Pharmacological properties of YM461, a new orally active platelet-activating factor antagonist

The antagonistic effect of YM461 [1-(3-phenylpropyl)-4-[2-(3-pyridyl)thiazolidin-4-ylcarbonyl]piperazine fumarate] against platelet-activating factor (PAF) was examined in severalin vitro andin vivo systems. We found that YM461 inhibited [³H]PAF binding to rabbit platelet membranes with a pK_i value of 8.90. YM461 inhibited PAF induced rabbit and human platelet aggregation with pA₂ values of 7.52 and 7.29, respectively; the slopes of the Schild plots were 1.07 and 1.01, respectively. However, YM461 at 10⁻⁴M did not affect rabbit and human platelet aggregation induced by ADP, collagen, arachidonic acid or epinephrine. YM461 inhibited PAF induced death in mice with an ED₅₀ (50% effective dose) value of 0.35 mg/kgp.o. YM461 at doses above 0.3 mg/kgi.v. inhibited PAF induced hypotension in rats. YM461 showed a dose-dependent inhibition of PAF induced hemoconcentration in rats with ED₅₀ values of 0.15 and 0.21 mg/kgp.o., respectively, at 0.5 and 1 hr after oral administration. The anti-PAF effect of YM461 persisted more than 6 hr after 3 mg/kgp.o. in rats. YM461 inhibited the bronchoconstriction induced by PAF with an ED₅₀ value of 1.2 mg/kgp.o. in anesthetized guinea pigs. Furthermore, the compound at doses above 3 mg/kgp.o. significantly inhibited antigen-induced anaphylactic asthma in conscious guinea pigs pretreated with mepyramine and propranolol. These results indicate that YM461 is a selective, potent and orally active PAF antagonist. Based on a paper presented at the Third International Conference on Platelet-Activating Factor and Structurally Related Alkyl Ether Lipids, Tokyo, Japan, May 1989.     

Microcrystalline silicon solar cells fabricated on polymer substrate

Low temperature fabrication of microcrystalline silicon solar cells was studied. It was found that reasonable performance is available even limiting substrate temperature at 100°C. Applying this technique to thermoplastic polymer substrates, a conversion efficiency of 6% was achieved.     

Compact ellipsometer employing a static polarimeter module with arrayed polarizer and wave-plate elements

A portable ellipsometer with a compact static polarimeter using an arrayed polarizer, an arrayed wave plate, and a CCD image sensor is developed. A high level of repeatability at a measurement speed of 0.3 s is demonstrated by measurement of SiO(2) films ranging from 2 to 300 nm in thickness deposited on an Si wafer. There is the potential to realize an ultracompact ellipsometer module by integrating the optical source and receiver, suitable for deployment in a variety of manufacturing equipment and measurement instruments.     

Simultaneous projection and detection system of four different frequencies for microwave imaging reflectometry in Large Helical Device

A simultaneous projection/detection system of four different frequencies for microwave imaging reflectometry (MIR) was developed for three-dimensional observation of electron density fluctuations in the Large Helical Device (LHD). The microwave with four frequency components at 60.410, 61.808, 63.008, and 64.610 GHz is projected in a continuous-wave mode to illuminate the target LHD plasma. A two-dimensional horn-antenna mixer array (2D HMA) receives the reflected wave from the plasma as well as the wave from the local oscillator operating at 55.800 GHz. The first intermediate frequency (IF) signals at 4.610, 6.008, 7.208, and 8.810 GHz were confirmed to be obtained by downconversion of these microwaves using the 2D HMA. Each of these first IF components is filtered from each other and downconverted again for the superheterodyne detection. It was confirmed that both the amplitudes and the phases of the detected signals reflect the fluctuations in LHD plasmas.     

Electron cyclotron emission diagnostics on KSTAR tokamak

A new electron cyclotron emission (ECE) diagnostics system was installed for the Second Korea Superconducting Tokamak Advanced Research (KSTAR) campaign. The new ECE system consists of an ECE collecting optics system, an overmode circular corrugated waveguide system, and 48 channel heterodyne radiometer with the frequency range of 110-162 GHz. During the 2 T operation of the KSTAR tokamak, the electron temperatures as well as its radial profiles at the high field side were measured and sawtooth phenomena were also observed. We also discuss the effect of a window on in situ calibration.     

Levee damage and bridge scour by 2019 typhoon Hagibis in Kanto Region,Japan

Typhoon Hagibis made landfall in Japan at 19:00 JST on 12th October 2019. The heavy rainfall caused by the typhoon was mostly concentrated within a 24-hour period; it brought devastating damage to eastern Japan. This report focuses on the flood-induced levee damage and bridge scour generated by the typhoon in the Kanto region. The levee breaches occurred mainly in the northern part of the region. They were concentrated along the Kuji and Naka Rivers and tributaries of the Tone and Arakawa Rivers. In most breached locations, the cause of the damage was the landward overtopping of the river water. Surface erosion on the slope of the protected side and/or slope failure on the protected side due to seepage-induced instability were the main causes of the levee breaches. Apart from the flooding induced by the inundation of the river water, inland flooding was also found. Damage to a river bridge due to local scour revealed the importance of considering the movement of sandbars in river channels, i.e., changes in the river flow conditions, when assessing the risks of bridge scour.     

Effect of Long Chain Fatty Acids on Organocatalytic Aqueous Direct Aldol Reactions

In an organocatalyzed, aqueous direct aldol reaction, the addition of a long chain fatty acid (1 mol%) such as stearic acid or erucic acid improved the aldol product yield and the enantioselectivity with low catalyst loading (1 mol%). The small particle size of the emulsion (less than 1 μm) was a key to the enhanced reactivity as shown by dynamic light scattering (DLS) analyses.     

Structural elucidation of a tadalafil analogue found in a dietary supplement

A tadalafil analogue was detected in a dietary supplement marketed for tonic effect, along with hydroxyhomosildenafil and aminotadalafil. The tadalafil analogue was isolated by preparative thin layer chromatography (TLC) and its structure was elucidated using high-performance liquid chromatography (HPLC), liquid chromatography electrospray ionization-mass spectrometry (LC-ESI-MS), Fourier transform-ion cyclotron resonance-mass spectrometry (FT-ICR-MS) and nuclear magnetic resonance (NMR) spectroscopy. The compound was determined to be methyl-1-(1,3-benzodioxol-5-yl)-2-(chloroacetyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate.     

An Adaptive Capacity Allocation Scheme in Telephone Networks

This paper discusses adaptive capacity allocation for high-usage groups (direct routes) in telephone networks so as to best maintain performance for each hour's traffic load. We present two algorithms for this adaptive allocation scheme. The first, called a capacity allocation algorithm, determines capacity allocation in a manner that minimizes the maximum value of point-to-point blocking probabilities for each hour's traffic load. The second, called a frame assignment algorithm, determines the channel connection pattern with a minimum of changes from the old pattern, for a new capacity allocation.     

Small Conductive Particle Detection with a Microwave Resonant Cavity

The recent miniaturization and increased complexity of electrical devices have increased the influence of impurities on device performance, especially the influence of small conductive particles with a size on the order of micrometers. Therefore, the inspection of devices during the manufacturing process has become important. In this study, changes in the resonance properties of a microwave cavity were used to detect a metal particle. The decrease in the resonant frequency for a 100‐µm stainless steel sphere was about 0.1 MHz, which was less than 1 ppm of the resonant frequency used. This frequency change is too small to detect directly in the output of a particle detector. Transmission measurements (the scattering parameter S21) at a frequency that was a few megahertz higher than the resonant frequency where the S21 changes sharply were used to magnify signal changes resulting from the introduction of a small conductive particle. A resonant frequency of 13.3 GHz and a frequency 3 MHz higher were chosen for obtaining measurements in the present study. By applying a filtering technique, it was shown that the minimum detectable sphere size is around 50 µm. This sensitivity was experimentally shown to be uneven along the long axis of the cavity. The unevenness was related to the electrical field strength of the standing wave at the resonant frequency. For practical industrial inspection of devices, multiple frequencies should be employed in view of the present discussion. © 2013 Wiley Periodicals, Inc. Electr Eng Jpn, 186(2): 61–67, 2014; Published online in Wiley Online Library ( wileyonlinelibrary.com ). DOI 10.1002/eej.22490