Studies on anti-inflammatory agents. V. Synthesis and pharmacological properties of 3-(difluoromethyl)-1-(4-methoxyphenyl)-5- [4-(methylsulfinyl)phenyl]pyrazole and related compounds

A series of novel 1,5-diphenylpyrazole derivatives bearing hydrophilic substituents was prepared. The anti-inflammatory and analgesic activities of these compounds were evaluated by using the adjuvant arthritis and Randall-Selitto assays in rats, and the structure-activity relationships were studied. The optimal compound was 3-(difluoromethyl)-1-(4-methoxyphenyl)-5-[4-(methylsulfinyl)phenyl]pyraz ole (10) with oral ED50 values of 0.31 and 2.6 mg/kg on adjuvant-induced arthritis and carrageenin-induced foot edema, respectively. Compound 10 showed analgesic activities not only toward inflamed paw but also toward normal paw (ED30 = 0.55 and 1.8 mg/kg, respectively) in the Randall-Selitto assay, and moreover, 10 was effective in the tail-pinch assay (ED50 = 21 mg/kg) similarly to morphine. The asymmetric synthesis and pharmacological properties of the enantiomers of 10 are also reported.     

Determination and survey of starting materials, intermediates, and subsidiary colors in food color of azo dye by high performance liquid chromatography

The number of official inspection of coal-tar dyes and their lakes from April in 1996 till March in 1997 were 581 in total. The quantity which passed inspection amounted to 164.5 ton in Japan. The production of color in each month was summarised in Table1, and by each producing company in Table2. The food coal-tar dye produced in the largest quantity was Food Yellow No. 4, occupying 43.4% in this period.     

Effect of voluntary exercise on maximal oxygen uptake in young female Fischer 344 rats

The effect of voluntary exercise on maximal oxygen uptake (VO2 max) was studied in young female Fischer 344 rats. After 10 weeks of wheel-running training, the absolute VO2 max and VO2 max relative to body mass increased without a decline in body mass. The running speed eliciting VO2 max, heart and soleus muscle mass, and succinate dehydrogenase (SDH) activity in the soleus muscle also increased. These results suggest that voluntary exercise is an effective means of increasing the aerobic exercise capacity of young female Fischer 344 rats.     

Role of adsorbed iodine into poly(vinyl alcohol) films drawn in KI/I2 solution

We have investigated the microstructure of the poly(vinyl alcohol) (PVA) films using small- and wide-angle X-ray scattering (SAXS and WAXS, respectively) techniques. The samples were uniaxially drawn in water or KI/I₂ aqueous solution and then dried in an air-oven at 333 K for 1 h prior to SAXS and WAXS measurements. It was found that for the films drawn in KI/I₂ solution PVA chains in the microfibrillar structure are more extended upon the film drawing compared to the case of the films drawn in pure water, which is resulted from the correlation function analysis on the SAXS data. Adsorbed iodines into the film were anticipated to act as junction points between the microfibrils via the formation of the PVA-iodine complexes.     

A new method for scanning electron microscopic visualization of dermal elastic fibres.

Autoclaving sections of dermis for 8 h followed by fixation, dehydration and xylol-air drying yields a pure preparation of elastic fibres for scanning electron microscopy which retains the native architecture of this component. Elastic fibres were intertwined in a complex fashion with numerous branches. Fibres were predominantly cylindrical in the upper dermis and became larger and more elliptical in the deeper dermis. This method produces a means to study of organization of elastic fibres in a variety of disorders in which dermal changes are prominent.     

Vision-based active sensor using a flexible beam

Proposes a vision-based active sensing system, termed vision-based active antenna. This is composed of a camera, a flexible beam whose force-deformation characteristic is known, and an actuator for rotating the beam. The camera observes the beam deformation, including the contact information, while the beam is in contact with an object. By solving a set of equations based on the information acquired through the camera, the sensor can detect the contact location, the contact force, and the stiffness of the object, even though the contact point is hidden by occlusion. For two particular versions, we show some experimental results to verify the basic idea     

Position control for a linear slider with twin linear drives

In this paper, position control of a linear slider with twin linear drives is considered. Recently, for high‐speed response, several linear motors have been used for linear slider systems. In such a linear slider, if the linear drives are controlled individually, their position responses may undergo vibrational disturbance by interaction with the output of the motors. To control this vibration, this paper presents a dynamic model of a linear slider system which consists of two motion systems decoupled by coordinate transformation, and proposes a feedback controller which is designed for these two decoupled systems. The effectiveness of the proposed method is confirmed by experiments. © 2004 Wiley Periodicals, Inc. Electr Eng Jpn, 147(4): 68–76, 2004; Published online in Wiley InterScience ( www.interscience.wiley.com ). DOI 10.1002/eej.10291     

Water Vapor Permeability of Poly(L‐lactide)/Poly(D‐lactide) Stereocomplexes

PLLA/PDLA blend films with only stereocomplex crystallites as a crystalline species together with pure PLLA and PDLA films with only homo‐crystallites as a crystalline species were prepared, and the effects of enantiomeric polymer blending, crystalline species, and crystallinity on the water vapor permeability were investigated. The WVT coefficient P of PLLA/PDLA blend films was 14–23% lower than that of pure PLLA and PDLA films in the crystallinity X_c range of 0–30%. Amorphous PLLA/PDLA blend films have a much lower P than pure PLLA and PDLA films. The dependence of P on X_c for blend films was stronger for X_c = 0–30% than for X_c = 30–100%. This dependence is discussed using the Nielsen model and the concept of “restricted” (or “restrained”) and “free” amorphous regions.

     

Studies on the contents of water-soluble chlorides and water-soluble sulfates in food color aluminum lakes

Japan's Specifications and Standards for Food Additives, 7th Edition (JSFA-VII) does not set limits for total contents of water-soluble chlorides and water-soluble sulfates (water-soluble inorganic salts) in food color aluminum lakes (FC-Als). However, the regulatory limit is 2% in JECFA and CFR. We used column switching suppressor-type ion chromatography (CSS-IC) for determination of anions. The total contents of water-soluble inorganic salts in FC-Als (112 qualified samples) were determined using the modified CSS-IC from fiscal year 1998 to fiscal year 2003. Total contents of water-soluble inorganic salts in four samples exceeded 2%. From an international point of view, it is desirable that the total content of water-soluble inorganic salts in FC-Al should again be regulated in Japan.     

GASIFICATION OF WASTE TYRE AND PLASTIC (PET) BY SOLAR THERMOCHEMICAL PROCESS FOR SOLAR ENERGY UTILIZATION

Waste tyre and plastic such as polyethylene terephthalate can be utilized as a useful material for conversion of solar energy into chemical energy by solar thermochemical gasification into synthesis gas (CO+H₂) using concentrated solar energy. In the present paper, the gasification of waste tyre (C: 86 wt.%, H: 8.4 wt.%) and of PET (C₁₀H₈O₄)_n, were studied using ZnO as a donor of oxygen in the infra-red furnace at 1373 K. For the gasification of tyre, most of the chemically bound hydrogen was converted into H₂ (62%) and CH₄ (29%) gases, while 71 mole% of the inherent carbon was gasified to CO (36%), CH₄ (29%), C₂H₄ (2%), and CO₂ (4%) in 200 s of the decomposition reaction. The CO₂:CO ratio was about 1/10, indicating that the carbon in the waste tyre can be converted effectively to gaseous fuels. In the experiment without ZnO, the conversion efficiency of C and H were decreased to 17% and 77%, respectively. However an appreciable effect of ZnO on the enhancement of the gasification of PET was not observed.