Search

Regioselective alkylation of 2-alkyl-5,6,7,8-tetrahydro-3H-cycloheptimidazol-4-one (1) and 2-alkyl-3H-cycloheptimidazol-4-one (2) was investigated. 3-[2'-(1-tert-Butyl-1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-2-propyl-5,6,7,8-tetrahydro-1H-cycloheptimidazol-4-one (6) was preferentially obtained under the conditions by using NaH in DMF or THF. On the other hand, 3-[2'-(1-tert-butyl-1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-2-propyl-5,6,7,8-tetrahydro-3H-cycloheptimidazol-4-one (5), the synthetic intermediate compound of Pratosartan, was obtained selectively in the presence of n-Bu(4)NBr in toluene by using aqueous sodium hydroxide as a base. In this reaction, it was found that the concentration of the alkaline solution influences its regioselectivity. This selectivity was observed even for aldehyde and ester derivatives.

3-Nitrobenzanthrone (3-NBA) is an extremely potent direct-acting bacterial mutagen that has been detected in diesel exhaust particles, airborne particles and so forth. Recently, 3-aminobenzanthrone (3-ABA) and 3acetylaminobenzanthrone (3-AABA) were identified as metabolites of 3-NBA in mammalian cells. In this study, to clarify the genotoxicity of 3-ABA, 3-AABA and 3-NBA in vitro and in vivo, the mutagenicity and DNA-damaging activity of these chemicals were investigated by the Ames assay and by alkaline single gel electrophoresis (Comet assay), respectively. 3-ABA and 3-AABA were mutagenic toward four Salmonella typhimurium strains, i.e. TA98, TA100, YG1024 and YG1029, in the presence of a mammalian metabolic system (S9 mix). Both chemicals showed the highest mutagenicity toward YG1024, and induced 2180000 revertants/nmol of 3-ABA and 131000 revertants/ nmol of 3-AABA. 3-NBA also showed mutagenicity toward these four strains with and without S9 mix, but the potencies of 3-NBA in these strains were decreased by the addition of S9 mix. In the presence of S9 mix, the mutagenic activities of 3-NBA in four strains were comparable to or lower than those on 3-ABA. 3-ABA, 3-AABA and 3-NBA produced statistically significant DNA damage, which was detected by an increase in the DNA tail moment, in vivo 3 hr after intraperitoneal injection at 160 mg/kg body weight. 3-ABA, 3-AABA and 3-NBA induced significant DNA damage in the liver, kidney, spleen and lung, spleen only, and liver, kidney, lung and bone marrow, respectively. At a lower dose (40 mg/kg), 3-NBA produced significant DNA damage in the lung. These results indicate that 3-ABA, 3-AABA and 3-NBA are not only mutagenic in vitro in bacteria but also genotoxic in vivo in mouse.

KT-362 (5-[3-[2-(3,4-Dimethoxyphenyl)ethyl]aminopropionyl]-2,3,4, 5-tetrahydro-1,5-benzothiazepine fumarate) is an intracellular Ca2+ antagonist. The compound obtained by introducing methyl groups onto the nitrogen (R2) of the side chain of KT-362 showed vasoconstrictive activity. Therefore we synthesized various derivatives, and examined their activities. Substitution at position R2 of the side chain resulted in potent contractile activity, and the optimal alkyl length was two or three carbons. The potency was further increased by the introduction of a chloro group at the R1 position of 2,3,4,5-tetrahydro-1,5-benzothiazepines. One of the synthesized compounds, 8-chloro-5-¿N-ethyl-N-[2-(3,4-dimethoxyphenyl)ethyl]aminopropionyl¿-2,3,4, 5-tetrahydro-1,5-benzothiazepine fumarate (9b), showed an EC50 value of 3.47 x 10(-8) M for contraction of rabbit iliac artery. The action of compound 9b was antagonized competitively by an H1-histamine receptor antagonist, diphenhydramine, and the pA2 value was 7.82. The maximum constriction was inhibited by a Ca2+ entry blocker, nicardipine, but not by an alpha 1-adrenoreceptor antagonist, prazosin. In a Ca(2+)-free medium, tonic constriction induced by 9b disappeared, and only a phasic constriction was observed. Though this phasic constriction was inhibited by diphenhydramine, it was not inhibited by prazosin or nicardipine.

A series of 2,3,4,5-tetrahydro-1,5-benzothiazepine and related compounds were prepared, and the intracellular Ca2+ inhibitory effects were examined using methoxamine- or caffeine-induced contraction of isolated rabbit arteries. Structure-activity relationship studies of these compounds are discussed and the results suggest that novel 5-[3-[2-(3,4-dimethoxyphenyl)ethyl]aminopropionyl]-2,3,4,5- tetrahydro-1,5-benzothiazepine fumarate (20d) showed the most potent inhibitory action on the intracellular Ca2+ release.

2-Propyl-8-oxo-1-[(2'-(1H-tetrazole-5-yl) biphenyl-4-yl)methyl]-4, 5, 6, 7-tetrahydrocycloheptimidazole (KT3-671), which has been found to be a potent and selective angiotesin II receptor antagonist, was synthesized in 14 C-labelled form by using potassium[ 14 C]-cyanide. [ 14 C](KT3-671) 9 with a specific activity of 1.74GBq/mmol was prepared in four steps in 29.8% overall radiochemical yield from potassium[ 14 C]cyanide

A gas sensor that utilizes chemiluminescence (CL) during the catalytic oxidation of odour vapours on a sintered aluminium oxide (γ-Al 2 O 3 ) layer is proposed. A new technique is applied to determine continuously the concentration of each constituent in a mixed vapour by a single CL-based sensor. The sensor is heated and cooled periodically in a temperature cycle between 200 and 740 °C at constant heating and cooling rates of ±9 °C s −1 . By measuring the total CL intensities in the heating and cooling courses, we can obtain the concentration of each constituent for a mixed vapour of ethanol and acetone in air. The lowest detection limit of the concentration of these vapours is of the order of 1 ppm.

Sodium 6-isopropyl-3-[4-(p-chlorobenzenesulfonylamino)-butyl]azulene-l-sulfonate (KT2-962) 1, which has been found to be a potent and selective thromboxaneA2 receptor antagonist, was synthesized in 14C-labelled form by using potassium [14C]-cyanide. 14C-labelled 1 with a specific activity of 2.36 GBq/mmol was prepared with no-carrier-added and in nine steps in 64% overall radiochemical yield.

Several 3-substituted-2H-cyclohepta[b]furan-2-one derivatives were prepared and tested in vitro for positive inotropic character. Introduction of an isopropyl group at the 5-position of compound 8a caused an increase of PIC50 (negative logarithm of the dosage which increases the contractile force by 50%) from 4.48 to 5.10. Among the 5-isopropyl-8-alkoxy compounds, the isopropoxy compound 12f had the most potent activity with a PIC50 value of 5.99. Conversion of the ester group at the 3-position to a methylene group and of the alkoxy group at the 8-position to a substituted amino group caused a decrease in activity. The most active compound, 12f, was also found to have a weaker heart rate (HR)-increasing effect compared to milrinone and amrinone.

Sodium 3-ethyl-7-isopropyl-1-azulenesulfonate 1, a new therapeutic agent for stomatitis, pharyngitis and ophthalmia was labelled with carbon-14 in the ethyl group attached to the azulene ring for use in metabolic studies. 14C-labelled 1 with a specific activity of 1.98 GBq/mmol was prepared in four steps in 39.3% overall chemical yield from [1 -14C]acetic acid sodium salt.

1,4,5,6,7,8-hexahydrocycloheptimidazoles and 4,5,6,7-tetrahydro-8-oxo-cycloheptimidazolones were synthesized as potential angiotensin-II (AII) receptor antagonists. One of these, 11c, KT3-671, was more potent than losartan with a pA2 value of 10.04 and At1 specific with an IC50 of 0.8 nM. In an in vivo study, it had long lasting action on blood pressure in RHR rat at a dose of 3 mg/kg.

Modification of sulfonamide moiety in non-prostanoid thromboxane A 2 (TXA 2 ) receptor antagonist, KT2-962 with double amide, sulfonamide-amide, (thio)semicarbazone, inverse sulfonamide and N-sulfonylcarboxamide is described. Unlike prostanoid TXA 2 antagonists, the importance of sulfonamide moiety for the activity of non-prostanoid TXA 2 receptor antagonist, KT2-962 was confirmed.

Thermoluminescence caused by adsorbates (adsorption thermoluminescence) appears in the process of heating Al2O3 powder that had previously adsorbed the vapour of an organic solvent, such as ethanol or acetone, at room temperature. The profiles of the thermoluminescence spectrum and glow curve depend on the kind of adsorbed vapour. The total amount of emitted light L depends on the concentration of the vapour in air, and L increases with an increase in the duration of adsorption. The adsorbates that act as the origin of the thermoluminescence are accumulated through a Langmuir-type adsorption process of very low activation energy (about 0.02 eV). These characteristics of the adsorption thermoluminescence enable us to discriminate and determine very low concentrations of these vapours. For example, L is proportional to the concentration of acetone vapour below 20 ppm for an adsorption time of 10 min, and the 1 ppm of vapour can be measured with good reproducibility.

Several 3-substituted-2H-cyclohepta[b]furan-2-one derivatives were prepared and tested in vitro for positive inotropic character. Introduction of an isopropyl group at the 5-position of compound 8a caused an increase of PIC50 (negative logarithm of the dosage which increases the contractile force by 50%) from 4.48 to 5.10. Among the 5-isopropyl-8-alkoxy compounds, the isopropoxy compound 12f had the most potent activity with a PIC50 value of 5.99. Conversion of the ester group at the 3-position to a methylene group and of the alkoxy group at the 8-position to a substituted amino group caused a decrease in activity. The most active compound, 12f, was also found to have a weaker heart rate (HR)-increasing effect compared to milrinone and amrinone.

For intracavitary high dose-rate radiation therapy, a thermoluminescent [TL] sheet for in vivo measurement of spatial dose distribution around source has been recently developed. The TL sheet was found to have a linear response with a very wide dynamic range from at least 0.002 cGy to 5000 cGy for 60 Co γ-rays. This TL sheet (40 cm × 50 cm × 200 Am), which is composed of Teflon mixed with BRSO 4 :Eu doped powder, is very flexible and can be cut to the desired size. In addition, this sheet is easy to handle because of its insensitivity to room light. The spatial dose distribution is displayed in a color mode by using a newly developed TL sheet readout system. For a clinical application, the TL sheet was wrapped on an applicator for intracavitary radiation therapy of a rectal cancer and was inserted into the rectum. The location of the TL sheet could be confirmed with diagnostic X ray film. After irradiation with high dose-rate 60 Co source, the in vivo relative dose distribution on the surface of the rectum was determined. This TL sheet provided a convenient means of measuring the relative dose distributions around 60 Co sources of various patterns in intracavitary radiation therapy.

The metabolites of sodium 3-ethyl-7-isopropyl-1-azulenesulfonate (KT1-32, 1), a candidate as an anti-ulcer drug, and related compounds were synthesized. The effects of the compounds on anti-peptic activity were determined as compared to that of 1.

Central collisions of 32S and 16O with Pb at 200 GeV amu have been studied by the emulsion spectrometer in the CERN-EMU05 experiment. The emission angles, momenta and charge signs of the secondary particles are measured. The position of a track in an emulsion plate should be measured by using a microscope to determine the momenta of more than 500 charged secondaries in an event. A new coordinate measurement system has been developed by using a video image processor connected to the microscope. In this system, the position, direction and length of a track in a coated emulsion are expressed as a vector which is linked with the motion of micro X-Y stage and is superimposed on an emulsion image on a TV monitor. By using this system, the data acquisition rate has become about ten times faster than that by using only an emulsion image and the momentum resolution has become higher than that. Moreover, this system is effective for identifying tracks emitted in more than 45°.

Sodium 3-ethyl-7-isopropylazulene-1-sulfonate 1, which has been found to be a potent and chemically stable agent having anti-inflammatory and anti-ulcerous activity, was synthesized in 14C-labelled form by using potassium [14C]-cyanide. 14C-Labelled 1 with a specific activity of 9.02 mCi/mmol was prepared in eight steps in 21.9% overall chemical yield from 3-(t-butyldiphenylsilyloxy)propyl tosylate 10.

放射線照射されていない固体において, 表面へのガス吸着に起因する熱ルミネッセンスを生じる現象(吸着ルミネッセンス)について調べた。BaSO_4 : Eu粉末への水, エタノール, アセトン等の蒸気の吸着によるルミネッセンスは, Eu^の励起準位からの緩和発光による615nmの線スペクトルと可視全域に広がる帯スペクトルとから成り, 線スペクトルと帯スペクトルの強度比および帯スペクトルの形状は吸着種に依存して異なる。吸着ルミネッセンスにおよぼす履歴効果と, ルミネッセンススペクトルの温度依存, 雰囲気変化に対する過渡応答等について計測した。, The thermoluminescence of unirradiated solids originated from adsorption of gases (adsorption thermoluminescence) has been examined. The luminescence of BaSO_4 : Eu phosphors results from the adsorption of water, ethanol and acetone vapor. The luminescence has a main line spectrum at 615nm and a sub band spectrum ranging from 400 to 700nm. The main line spectrum corresponds to the de-exitation emission of Eu^, whereas the sub band spectrum does not appear in normal thermoluminescence. The ratio of the intensity of the main and sub spectrum and/or the structure of the band spectrum are dependent on adspecies. Sustained emission is observed when the vapor of these organic solvents are introduced into synthesized air. These observations suggest that the measurement of adsoption luminescence spectrum may realize the analysis of environmental gases. The effect of the sample history on adsorption thermoluminescence, the temperature dependence of the luminescence spectrum and the transient response of the luminescence to alterations in the gas environment are measured. It may be concluded that the adsorption thermoluminescence which appeared for samples stored in the atmosphere results from the recombination radiation between electrons trapped into the surface states originated from chemisorbed water and free holes released from the surface states originated from chemisorbed oxygen.

A series of alkylazulene-1-sodium sulfonate derivatives which has an isopropyl group at 6-position were synthesized, and their anti-ulcer activities were examined in Shay pylorus-ligated rats. The values of lipophilicity (log P) as a parameter of these new azulene derivatives were also examined in reference to the structure-activity relationship. The optimum value of log P, which showed maximal anti-ulcer activity, was about -0.46. Among the derivatives of azulene examined, 3-ethyl-6-isopropylazulene-1-sodium sulfonate (compound IXb:XT1-785) exhibited the most potent inhibitory action against Shay ulcer, and its anti-peptic activity was similar to that of 3-ethyl-7-isopropylazulene-1-sodium sulfonate (KT1-32). It also had more activity than guaiazulene sodium sulfonate (GAS). Furthermore, KT1-785 was extremely stable under heating as compared to GAS.

The metabolism of azuletil sodium (AZE, KT1-32, sodium 3-ethyl-7-isopropyl-l-azulenesulfonate 1/3hydrate), a novel anti-ulcer agent, was studied after oral administration of 14C-KT1-32 to male rats. The intact KT1-32 and six metabolites were found in the urine of male rats and were identified by high performance liquid chromatography (HPLC) using a radioisotope detector. The sum of radioactivities of these identified metabolites accounted for 94% of the total radioactivity in the urine. These metabolites were isolated by various solid extraction cartridges. The structural elucidation of the isolated metabolites was carried out by 1H-NMR spectroscopy and mass spectrometry with electron ionization mode after converted them into the n-propylester-dimethyl ethylsilyl ether derivatives, especially mass spectrometry was very useful to characterize each of these metabolites. M3, only one conjugate, was found to be as the sulfate of the ω-1 hydroxylated metabolite of the ethyl group in KT 1-32. All of these metabolites, except M3, were identified by the comparison of their spectral data with those of the authentic compounds, indicating that the preferential ω-1 hydroxylations of KT1-32 took place on the alkyl groups in 3 and 7 positions and did not on the azulene ring itself.

Effective preparation of cycloheptimidazol-4-ones was developed. The reactions of 2-tosyloxytropone (5) with amidines (6) carried out under simple conditions such as aq. NaOH in toluene at 35 degrees C afforded the corresponding cycloheptimidazol-4-ones (3) in low yield. However, by adding tetra-n-butylammonium bromide (n-Bu(4)NBr) to this reaction system, the yield was improved dramatically. The reaction conditions were screened in detail.

Three hydroxylated metabolites of 2-propyl-3-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-5,6,7,8-tetrahydro-3H-cycloheptimidazol-4-one (Pratosartan), which is a selective angiotensin II receptor antagonist, were synthesized in confirmation of their structures and in studies of their pharmacological properties. An MTPA ester of the human main metabolite was identified with the synthesized compound by comparing (1)H-NMR spectra, MS spectra, and HPLC retention time. The structure of the human main metabolite was confirmed to be (S)-(-)-2-(1-hydroxypropyl)-3-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-5,6,7,8-tetrahydro-3H-cycloheptimidazol-4-one ((S)-(-)-1). Also, the rat main metabolites were confirmed to be 8-hydroxylated compound (2) and 5-hydroxylated compound (3). These metabolites showed lower antagonistic activity than that of the parent compound.

In order to examine the correlation between activity and hydrophilicity of the side chain of sodium 3-[4-(4-chlorobenzenesulfonylamino)butyl]-6-isopropylazulene -1-sulfonate (KT2-962), a non-prostanoid TXA2/PGH2 receptor antagonist, one or two hydroxyl groups were introduced into the isopropyl moiety. A series of 6-hydroxylated-isopropylazulenes were synthesized by regioselective oxidation of 6-isopropylazulenes and their in vitro and in vivo antagonistic activities were studied. Both the primary and tertiary alcohols, monohydroxylated derivatives, exhibited potent biological activities comparable to unmodified 6-isopropylazulenes both in vitro and in vivo. In contrast, the activities of 1,2- and 1,3-diols of 6-substituted derivatives, markedly decreased, but recovered by O-isopropylidenation of the dihydroxyl moiety. These findings indicate that the moderate hydrophobicity of substituent at the 6-position of the azulene ring might be required for the activity and the size of the substituent at this position, not so rigid for keeping potent biological activity.

An adsorption-luminescent sensor enables us to discriminate and determine the vapor of odor substances by measuring temperature dependence of luminescence from the sensor (powder of (gamma) -Al2O3) which previously adsorbed odor vapor in the air. Profiles of the adsorption luminescence (AL) spectra as a function of temperature for butanol, acetone, and n- butyric acid are apparently different from each other, and these vapors of 1 to 100 ppm in concentration in the air can be determined from the total luminescence intensity. The study of photoluminescence (PL) observed for the sensor after contact with these odor vapors implies that AL is peculiar chemiluminescence during catalytic oxidation of odor vapor which produces water and surface hydroxide.© (1993) COPYRIGHT SPIE--The International Society for Optical Engineering. Downloading of the abstract is permitted for personal use only.

A series of novel azulene-1 carboxylic acid derivatives 28-30, azulene-1 sulfonic acid sodium salts 41a-c, and related compounds were synthesized. These compounds were tested for TXA2 receptor antagonistic activity. The inhibitory concentrations (IC50) of these compounds for vascular contraction (TXA2 tau receptor) and platelet aggregation (TXA2 alpha receptor) induced by (15S)-15-hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5(Z),13(E)- dienoic acid (U-46619) were obtained. Azulene-1-sulfonic acid sodium salts 41a-c were over 3 times more potent than azulene-1-carboxylic acids 28-30. The most potent compound, 41b was 4 orders of magnitude more potent than a TXA2 antagonist, BM13,177, in inhibiting vascular contraction (tau receptor) and had an IC50 of 9.0 x 10(-10) M. Compound 41b was also found to be a tau receptor selective antagonist (IC50 of contraction/IC50 of aggregation = 378) and to have no TXA2 synthetase inhibitory activity at concentrations up to 10(-4) M and no partial agonistic activity at concentrations up to 10(-5) M in rabbit aorta (tau receptor) and up to 10(-4) M in rabbit platelet-rich plasma (alpha receptor). In a radioligand binding assay using rabbit gel-filtered platelets, compound 41b had a high-affinity binding for the TXA2 receptor. In an in vivo study, compound 41b inhibited U-46619-induced sudden death in mice at a dose of 0.3 mg/kg and its duration of action was over 8 h when administered orally at 3 mg/kg.

アンダーセン・エヤ・サンプラーを用いて粒径を分けて採取した大気浮遊塵の中性子放射化分析を行ない, その成分元素の粒径分布を測定した。試料は京都市内で1974年12月下旬から1975年1月中旬にわたって採取した。Al, Sc, Fe, Ti, Thの大気中濃度は浮遊塵の粒径が大きい場合に高く, 粒径が小さくなるにつれて急激に減少した。一方, Zn, Sb, Br, Cl, Vはこれとは全く逆の傾向を示し, 粒径が小さくなるにつれて急激に増大した。又, K, Na, Mn, Eu, Ce, W, Coでは粒径による大気中濃度の大きな変化は認められなかった。これらの元素は, それぞれ, 主として土壌粒子に由来するもの, 人工的な発生源に起因するもの, 及び, 両者の混合したものに対応するものと推論した。

大容積・高分解能Ge(Li)半導体検出器を用いた中性子放射化分析法により, 岡山及び倉敷地区の四測定点で1974年4月に1ケ月間連続して採取した大気浮遊塵中に含まれる元素の濃度を求めた。試料はローボリーム・エアサンプラーを用いてメンブレンフイルター上に集め, 京都大学原子炉の熱中性子で放射化し, 電子計算機によるガンマ線スペクトルの解析の結果, 17種類の元素について, その濃度を決定した.またこれの元素の大気中濃度の地点別変化の相違を, 1974年3月京都で採取した試料の測定値と合せて考察した., Neutron activation analysis with large volume high resolution Ge(Li) detector was applied to obtain concentrations of elements in airborne dust samples which were continuously collected for a month at four stations in Okayama and Kurashiki districts in April, 1974. The samples were collected on menbrane filters using open type low volume air samplers and activated with thermal neutrons in Kyoto University Research Reactor. The concentratons were determined for seventeen elements and their differences with respect to the sampling stations were discussed in connection with data measured in Kyoto district in March, 1974.

We have succeeded to detect 1.0～0.9 TeV electromagnetic cascade showers with Norikura TL [thermoluminescent] chamber using the spatial photon counting system. We have reported the feasibility of a new detector, the TL sheet in super-slow heavy particle searches.

熱ルミネッセンス(TL)の2次元読み取りシステムについては, 前年度紀要に報告した.今回は, さらに詳しくシステムの特性を報告する.又, 解析系とビデオテープレコーダとの同期がとれるようにしたことにより活用範囲が大幅に拡大した.特にTLのような"transient"現象には一旦ビデオに収録した後, 繰り返し読み取ることにより精密解析が可能になる.又同様にシステムの特性を調べる上で有効であった., Some detailed properties of the spatial distribution read-out system for thermoluminescence (TL), which have been proposed by us, are reported. Then, the video-tape recorder is fully used : its reproducibility makes us to measure a "transient" phenomenon of TL "repeatedly". And, the recorder synchronized with an analizing system makes us to cut-out any part of a picture accumulated from reproduced frame(s) and to analize it. The cause for the super-linear characteristics of the image intensifier used has been surveyed. And. a calibration method for the super-linearity is proporsed.

This paper gives an outline of the PSPD (pure single particle detecting) telescope which is being used in a search for fractionally charged particles in cosmic rays at sea level. A special feature of this experiment is the accurate d E /d x measurement and the detecting of pure single particles. For this purpose, multicell proportional chambers and the PSPD counters are used. The procedures and systems for data selection are also described.

1973年3月から1974年4月にわたる約1年間に, メンブレーン・フィルターを装着した開放型ローボリウム・エヤ・サンプラーを用いて, 京都市内及び岡山市近辺の汚染環境の異なる6地点で採取された大気浮遊塵の中性子放射化分析を行ない, その中に含まれる微量元素の濃度及び季節変化を求めた, 更に, これらの結果より, 大気汚染の態様の比較を行ない, 汚染元素の起源について考察した。

倉敷市及び蒜山高原で, 1976年8月上旬にアンダーセン・エア・サンプラーを用いて捕集した大気浮遊塵の機器的中性子放射化分析を行ない, 23種類の元素につき大気中濃度及びその粒径分布を求めた。更にこれらの量の解析から大気汚染の態様を考察した.その結果からAl, Sc, Th, Feは大粒径粒子に属し, 土壌粒子と考えられる.これに反し, Sb, Zn, Br, V, Seは微粒子に多く含まれ, 化石燃料の燃焼等に起因するものと考えられる.またMn, Cl, Na, K, As, La, Ce, Co, Hg等は特定の傾向を示さず, 複数の発生源によるものと考えられる.地点間では倉敷市に於ける元素濃度は蒜山高原の数倍に達し, 特にFe, Mn, Zn, Clに顕著な相違がみとめられた., Multielement components of airborne dust and their particle-size distributions were investigated using instrumental neutron activation analysis. Air sampling was done with a eight stage Andersen sampler in Kurashiki-City, an industrialized urban area, and in Hirusen heights, a rural area about 100km north of the city, in August, 1976. Some elements associated with larger size dust particles (viz. Al, Sc, Th, and Fe) appeared to be mainly soil-derived, whereas other elements associated with the smaller size fractions (e.g. Sb, Zn, Br, V and Se) appeared to be originated from significant anthropic sources such as combustion of fossil fuels. The remaining elements showed no characteristic particle-size distributions and saggested to have composed sources. Observed concentrations for Zn, Mn, Fe and Cl as well as V, Cr and La were considerably higher in Kurashiki-City than in Hirusen heights.

熱ルミネッセンス[TL]2次元読み取りシステムを開発した。このシステムを使った応用として, 人工のTL-sheet(BaSO_4 : Eu)を用いて高エネルギー宇宙線シャワーの検出を行なった例と, 天然の試料(鍾乳石, 花崗岩)のTL空間分布を測定した例を示す., A spatial distribution read-out system of thermoluminescence [TL] is developed. This system is applied to artificial TL-sheets (BaSO_4 : Eu) for detecting high energy cosmic ray showers and to inhomogeneous materials for measuring natural TL spatial distributions of stalactite and Mannari-granite.

A number of carbacyclins having bicyclic substituents on the omega-chain have been synthesized and tested for antiplatelet aggregation activity in vitro (against collagen-induced aggregation of rat platelet), for reduction of systemic blood pressure in vivo (ability to reduce the blood pressure in anesthetized rat by iv injection), and for cytoprotective activity (protection against ethanol-induced rat gastric lesion). The most effective compound for each activity was [3aS-[2E,3a alpha,4 alpha (3R),5 beta,6a alpha]]-5-[hexahydro-5- hydroxy-4-[3-hydroxy-3-(2-indanyl)-1-propynyl]-2(1H)-pentalenylidene+ ++] pentanoic acid (compound 11a), while some 1,4-benzodioxan analogues had selectivity for organ-protective activity, and indan analogues showed selectivity in their antiaggregation activity.

Phton counting methodにより, 宇宙線測定用TL(Thermoluminescence)-sheet[BaSO_4 : Eu]の発光特性を調べた.[I]放射線照射によるSignal light[SL]は, UV-域にピークがある.[II]TL-sheetを長時間曝露したり, 手荒く扱った際に生ずるObstructive light[OL]は, yellowとblueにpeakがある.[III][OL]の原因であるObstructive radiation[OR]はO_2の関与する表面現象に起因する.[IV-1]窒素雰囲気中で加熱計測をすれば, [OR]を抑えることができる.[IV-2]適当なバンドパスフィルタを用いれば[OL]を減少させることができる.TL-sheetを用いた高エネルギー宇宙線観測に対して, これら[IV-1,2]の方法の導入は, (a)"大量のシートも容易に取扱うことができる."(b)"[OR]によるbackgroundを小さくするので, シャワーエネルギーの計測しきい値を下げることができる."等の点で有効である., We have investigted emission light characteristics of the thermoluminescence [TL]-sheet [BaSO_4 : Eu]. More, we have introduced the rejecting methods for the obstructive light [OL] of these sheets. [I] Signal light [SL] emission spectra due to high energy γ, β and cosmic rays irradiations were observed in ultra-violet regions (that peak is about 370 nm). [II] In the case of rough treatments of TL-sheets or locating them for long time, we observed the OL emission in addition to the SL emission. These OL spectra are two bands of 570 nm (yellow) and 450 nm (blue). [III] The OL emission due to the obstructive radiation [OR] is caused by surface phenomena concerned with O_2 for the TL-sheet [BaSO_4 : Eu]. [IV-1] The glow curves, in which the OR emission suppressed are obtained in a nitrogen atmosphere. [IV-2] By using moderate band pass filter, the OL can be cut easily. For high energy cosmic ray researches by using TL-sheets, these methods [IV-1,2] are effective as follows ; a) One can treat easily TL-sheets in large quantities. b) Deminishing backgrounds due to the OR emission, one can observe shower energies of lower threshold values.

We have developed a spatial distribution readout system of thermoluminescence (Tl) sheets, which realizes in more detail the two dimensional (2-D) photon counting. The thermal fading effect of the Tl sheet has been investigated and the cosmic ray flux at 16000 m altitude causing background in the Tl sheet has been obtained by the 2-D photon counting.

A cosmic-ray counter telescope (OKAYAMA telescope) has been operated at several zenith angles at sea level. Several millions of clean single events have been analysed. About thirty candidates of (4/3)e charged leptons were found at around 40° zenith angles. The distribution of the arrival directions of these candidates in the celestial sphere was found to be anisotropic.

A cosmic-ray counter telescope (Okayama Telescope) has been operated at various zenith angles in order to look for fractionally charged particles at sea level. Several millions of clear single events have been analyzed. At zenith angles around 40°, several candidates of ( 4 3 )e charged particles were found, while at other zenith angles few candidates were found. To examine these results, we have constructed an improved telescope to measure d E /d x and to trace the track in crossed planes. This paper gives the characteristics and the first analysis of the data obtained with the improved telescope.

The directional correlation between the 1.119 MeV gamma-ray and the 0.887 MeV gamma-ray in 46Ti has been studied. The experimental data agree well with a theoretical curve for the 4(Q)2(Q)0 sequence. The attenuation of the angular correlation coefficient in our measurement is not so marked as to explain that experienced by Boehm and Rogers in their measurement of the beta-gamma circular polarization correlation on the same isotope.