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Observations of tropical convection and cloud clusters with two X-band Doppler radars were carried out on Manus Island, Papua New Guinea for two and a half months from 12 November 1992 during the Intensive Observation Period (IOP) of the TOGA-COARE. Several different types of clouds were observed by Doppler radars during the period, such as squall lines, convective clouds and stratiform clouds associated with cloud clusters, isolated convective clouds over the island in the day time, etc. Outlines of the observations on Manus Island and brief reviews of the results of these observations are described. Preliminary summaries of the analyses on the observations are: 1) A warm rain process dominates at the beginning stage of radar echo development and the maximum radar reflectivity is recognized at this stage, 2) The maximum echo top height is observed within 3 hours from the first echo, 3) The maximum echo area within the radar range was analyzed a few to several hours later than the time of maximum echo top height corresponding to the size of cloud cluster, 4) In the long-lasting stratiform echo, updrafts independent from those below the melting layer were identified above the melting layer. It is concluded that further studies utilizing these observational data may reveal the structure and the evolution mechanism of tropical cloud clusters.

Background The guidelines recommend combination therapy for patients who are unable to achieve target BP with monotherapy; some fixed dose therapies including an angiotensin II receptor blocker (ARB) and diuretics are available in Japan. However, to date there have been few reports on this long-term treatment and the patient profiles suited for this combination remain ambiguous. Method The Aichi Research on Combination therapy for Hypertension Study was a multicenter, open-label, prospective observational study that investigated the efficacy and safety of 1-year treatment with the losartan-hydrochlorothiazide (HCTZ) combination tablet in patients with hypertension uncontrolled by either ARB monotherapy or combination therapy with a calcium channel blocker (CCB). An ARB was switched to a losartan-HCTZ tablet after a pre-observation period. Results A total of 614 of 648 patients were evaluable (mean age, 66.3 years; 52.8% men; mean baseline blood pressure, BP, 157.7/87.9 mmHg). The BP had decreased significantly to 138.0/78.2 mmHg by month 3 (p

The intramolecular cyclization of an allyl halide having a carbonyl group proceeded smoothly via an allyl anion in the presence of Me3SiSnBu3 and CsF in DMF. The resultant products were converted into useful compounds for the synthesis of natural products.

Suppurative knee joint infection probably due to intraarticular steroid injection, has been increasing recently. In this study, we report the results of a follow-up survey conducted in eleven patients (chiefly those with over five-year course after onset) who were referred to our hospital from other medical institutions during the past ten years.For clinical assessment knee joint function was evaluated on the basis of the “SANDAIGAKU” tentative plan. On X-ray medial and lateral joint spaces were determined bilaterally on the frontal image of lower limbs in the standing position, and PF joint spaces were measured on the lateral image. Evaluation was made for each item before disease onset, one year after surgery, and at the time of final follow-up.All eight patients who could be followed up for over five years have experienced no recurrence of the suppurative arthritis after surgery, and their gait ability was relatively satisfactory. Total scores of the “SANDAIGAKU” tentative plan improved in four patients, declined by 15 points or less in three patients, and significantly declined in one patient. Medial joint space was 3.9mm on average before surgery, 2.6mm one year after surgery and 0.9mm at the time of the final survery. Lateral joint space was also reduced in size in chronological order from 4.6mm to 3.9mm and 2.0mm, respectively. PF joint space also chronologically decreased from 2.5mm to 1.3mm and 0.6mm, respectively.

Background Concern over the potential cardiotoxicity of anti-malarial drugs inducing a prolonged electrocardiographic QT interval has resulted in the almost complete withdrawal from the market of one anti-malarial drug - halofantrine. The effects on the QT interval of four anti-malarial drugs were examined, using the guinea pig heart. Methods The guinea pig heart was isolated, mounted on a Langendorff apparatus, and was then perfused with pyruvate-added Klebs-Henseleit solutions containing graded concentrations of the four agents such as quinidine (0.15 - 1.2 μM), quinine (0.3 - 2.4 μM), halofantrine (0.1 - 2.0 μM) and mefloquine (0.1 - 2.0 μM). The heart rate-corrected QaTc intervals were measured to evaluate drug-induced QT prolongation effects. Results Quinidine, quinine, and halofantrine prolonged the QaTc interval in a dose-dependent manner, whereas no such effect was found with mefloquine. The EC50 values for the QaTc prolongation effects, the concentration that gives a half-maximum effect, were quinidine < quinine ≈ halofantrine. Conclusions In this study, an isolated, perfused guinea pig heart system was constructed to assess the cardiotoxic potential of anti-malarial drugs. This isolated perfused guinea pig heart system could be used to test newly developed anti-malarial drugs for their inherent QT lengthening potential. More information is required on the potential variation in unbound drug concentrations in humans, and their role in cardiotoxicity.

The intramolecular cyclization of an allyl halide having a carbonyl group proceeded smoothly via an allyl anion in the presence of Me3SiSnBu3 and CsF in DMF. The resultant products were converted into useful compounds for the synthesis of natural products.

A novel 1,3-diene synthetic method from alkyne and ethylene was developed using ruthenium-catalyzed enyne metathesis. The reaction procedure is very simple: A CH 2 Cl 2 solution of alkyne was stirred at room temperature under ethylene gas (1 atm.) in the presence of a catalytic amount of ruthenium benzylidene complex. The yield was good and the conversion yield was high. Dienes having functional groups such as a keto-carbonyl group, silyloxy group, ester, and ketal were synthesized from the corresponding alkynes and ethylene. In this reaction, the alkyne having a hetero atom at the propargylic position gave a good result and ether oxygen or amine nitrogen that coordinate strongly to the ruthenium catalyst prevents the reaction.

A series of novel N -acylsulfonamide analogs were synthesized and evaluated for their binding affinity and antagonist activity for the EP3 receptor subtype. Representative compounds were also evaluated for their inhibitory effect on PGE 2 -induced uterine contraction in pregnant rats. Among those tested, a series of N -acylbenzenesulfonamide analogs were found to be more potent than the corresponding carboxylic acid analogs in both the in vitro and in vivo evaluations. The structure activity relationships (SAR) are also discussed.

本研究では,徒手筋力計を用いた複数動作の最大等尺性筋力の総和における正常人値を求め,臨床における本法の有用性を示すことを目的とした.平均的体格者120名(20～79歳)を正常人調査の対象とした.仰臥位における頸部屈曲,上肢外転,下肢伸展挙上の3項目について測定を行い,男女別,年代別の3項目総和筋力の正常人値を求めた.臨床においては,ミオパシーなどの全身的筋力低下の症例に本法を経時的に行い,総和筋力は病状をよく反映した.徒手筋力計は,取り扱いの簡便さが最大の利点であり,その信頼性についても測定手技の熟練により大きな問題はない.3項目総和筋力は,ミオパシー症例などの臨床評価に有用である.

The regulation of gene expression after the introduction of an exogenous gene is a problematic aspect of gene therapy. The purpose of this study was to use doxorubicin to regulate exogenous gene expression in a vector containing the cytomegalovirus (CMV) promoter. The pQBI25 vector, which encodes the CMV promoter and the cDNA for red-shifted green fluorescent protein (rsGFP), was transfected into a rat skin fibroblast cell line (FR cells). The pEGFP vector, encoding the CMV promoter and enhanced green fluorescent protein (EGFP) cDNA, was transfected into human hepatoma HepG2 cells. FR-pQBI25 cells were then continuously exposed to doxorubicin and methotrexate for 96 and 48 h, respectively; HepG2-pEGFP cells were continuously exposed to doxorubicin for 48 h. The levels of c-fos, c-jun and rsGFP mRNA, as well as the levels of rsGFP protein, in the FR-pQBI25 cells were found to be significantly higher following exposure to doxorubicin. However, the level of rsGFP protein was not changed by exposure to methotrexate. The level of EGFP protein in the HepG2-pEGFP cells was also significantly higher following exposure to doxorubicin. To examine the effect of cessation of doxorubicin exposure, FR-pQBI25 cells that had been exposed to doxorubicin for 48 h were re-plated in fresh medium without doxorubicin for a further 48 h. The increased levels of c-fos, c-jun and rsGFP mRNA and rsGFP protein seen after treatment with doxorubicin had reduced by 48 h after the cessation of exposure to doxorubicin. These findings suggest that CMV-driven exogenous gene expression may be regulated by doxorubicin.

A series of (4beta-substituted)-L-prolylpyrrolidine analogs lacking the electrophilic nitrile function were synthesized and their dipeptidyl peptidase IV (DPP-IV) inhibitory activity and duration of ex vivo activity were evaluated. Structural optimization of a N-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine analog 8, which was found by high-speed analog synthesis, was carried out to improve the potency and duration of action. A representative compound 26 was evaluated to assess its effect on the plasma glucose level after the oGTT (oral glucose tolerance test) in normal rats. Structure-activity relationships (SAR) are also presented.

A novel catalytic activation of the leaving group in the S(N)2 reaction is achieved as an extension of our mercuric triflate-catalyzed reactions. Derivatives of anilinoethyl 4-pentynoate reacted smoothly with catalytic amounts of Hg(OTf)(2) to give indoline derivatives in excellent yield with efficient catalytic turnovers under very mild conditions. The reaction of optically pure secondary alcohol derivatives resulted in inversion of stereochemistry, which is a definitive feature of the S(N)2 reaction. The procedure is applicable for benzoazepine synthesis.

Details of structure–activity relationships (SAR) for P2 moiety of a P1 2-cyanopyrrolidine dipeptidyl peptidase IV (DPP-IV) inhibitor 4a including stereochemistry are presented. Based on this information, a series of P1 (N-alkyl)aminoacetonitrile analogs 9–20 possessing optimal P2 structure were synthesized and evaluated as inhibitors of DPP-IV. Among them, a representative compound 11, N-(cyanomethyl)-N-ethyl- l -prolinamide, was further evaluated to determine its effect on the plasma glucose level. Also 4a, 10, and 11 were evaluated for their isozyme selectivity to predict their safety problems.

Regulation of gene expression after gene introduction is a problematic aspect of gene therapy. Transcription regulates gene-specific transcriptional factors, which bind to regulatory regions in the promoter. The cytomegalovirus long terminal repeat (CMV-LTR) has a TPA response element (TRE) as a binding site for activator protein 1 (AP-1), which is induced by oxidative stress. The purpose of this study was to regulate exogenous gene expression in a vector with CMV-LTR using oxygen radicals.We used two plasmids (1) pQBI25 encoding CMV-LTR and red-shift green fluorescent protein (rsGFP) cDNA and (2) pRc/CMV-SOD encoding CMV-LTR and human Cu, Zn-superoxide dismutase (SOD) cDNA. FR cells were transfected with pQBI25 (FR-pQBI25 cells), and L2 cells were transfected with pRc/CMV-SOD (L2-pRc/CMV-SOD cells). Each type of cell was exposed to oxygen radicals using paraquat for 24 h. Levels of c-fos, c-jun and rsGFP mRNAs were determined using reverse transcription polymerase chain reaction (RT-PCR). Levels of rsGFP protein were measured by fluorometry. Total SOD activity was measured using the nitrite method.Levels of c-fos, c-jun (AP-1 composition protein) and rsGFP mRNA were induced significantly by oxygen radical exposure in FR-pQBI25 cells. A positive correlation was observed between levels of c-fos mRNA and rsGFP mRNA and also between levels of c-jun mRNA and rsGFP mRNA. Levels of rsGFP protein were also induced significantly. Total SOD activity was induced significantly by oxygen radical exposure in L2-pRc/CMV-SOD cells.This study suggests that gene expression driven by the CMV- LTR promoter may be regulated by oxygen radicals.

(4, 4-Dibromobut-3-enyl)benzene 5-Phenylpent-2-yl-1-ol Acetic acid 5-phenylpent-2-ynyl ester Acetic acid 2-methylene-3-phenethylbut-3-enyl ester Butyllithium Keywords: 1,3-dienes; ethylene; alkynes; waste disposal; ruthenium catalyst; purification

Synchrotron radiation has been utilized for producing the intensity difference in resonant X-ray magnetic scattering (RXMS) of ferrimagnetic BaTiMnFe10O19 at the BL-6C beamline of the Photon Factory. The energy of incident X rays was selected as E = 7.1245 keV within the threshold region of Fe K absorption edge from the observation of X-ray magnetic circular dichroism (XMCD). An asymmetrical ratio between RXMS intensities in left- and right-handed circular polarizations makes it possible to determine the magnetic crystal structure. The residual functions of Σ(ΔRobs − ΔRcalc)2 related to the ratio were used to evaluate magnetic moments for individual Fe sites in the least-squares calculations, refined as multiplicity parameters of atomic scattering factor. The canting angles of the spin of Fe atoms have been derived for BaTiMnFe10O19, which are 90°, 0° and 31° for octahedral 2a, 4f2 and 12k sites, respectively.

本研究の目的は12誘導心電図で診断困難な陳旧性下壁梗塞例が体表面電位図あるいはベクトル心電図でどの程度診断可能かを検討する事である。12誘導心電図aVFに幅0.02秒以上0.04秒未満, 深さR波の1/4未満のQ波を示す43例を対象とし, これらの症例を心臓カテーテル検査所見等に基づいて梗塞群 (24例) と非梗塞群 (19例) に分けた。梗塞群の体表面電位図ではQRS開始後10～20msecにかけて極小が左背部から背部下方, あるいは背部下方から右胸部下方へと動くのが特徴的であった。一方, 非梗塞群では極小は同じ時期に背部から右胸部上方, あるいは左前胸部から背部下方へと移動した。QRS開始後10msecと20msec時の極小の位置に基づく電位図の下壁梗塞診断基準を設定するとsensitivityは83%, specificityは95%であった。一方, YoungとWilliamsのベクトル心電図診断基準ではsensitivityは79%, specificityは26%であった。

A large pseudolumen due to dissection arose during percutaneous coronary angioplasty. The true lumen was compressed critically. However, no infarction took place because of good collaterals. During medical follow-up, the patient's angina vanished suddenly. The repeat angiography showed healing of the dissection and patency of the coronary artery.

In order to prove the tension mooring system is safe and useful, Japan Marine Science and Technology Center performed the TLP sea test by utilizing the prototype floating platform. The previous papers of this study discussed the design of the tension mooring system on basis of the results of theoretical considerations and model tests, and introduced the outline of the sea test.This paper discusses on the measuring system and data analysis in the TLP sea test and the dynamic response characteristics of the TLP.The tension measuring system which utilizes the combination of conventional chain-guide wheel and compressive load cell was proved to give the varying tensions about twice larger than the theoretically expected ones. The reason of this overestimation is supposed to be that under the static initial tensions, the varying tensions attenuate while going around the chain-guide wheel and then the load cell measures the larger load out of balance.This inference was proved to be true through the direct measurement of the loads of the chain at both sides of the wheel in the second sea test (1987).The significant values of the varying tensions are estimated and compared well with the theoretical values.The horizontal movement of the TLP is another topic in this study. The surge/sway acceleration of the TLP were measured by utilizing the pitch/roll inclination meters. The yawing motions were measured by the monitor TV camera installed on the deck of the TLP.

The tension mooring of the floating ocean structures seems promising to expand the ocean space exploitation. This kind of mooring method becomes relatively inexpensive in deep ocean, and has many advantages such that it can suppress the motion of the floating structures and needs only minimum mooring space.This paper presents the results of the fundamental study on the tension mooring. A semisubmersible model with 4 footing columns is tautly moored by the rubber-chain cable in the regular waves. The results of the study are following.(1) The rubber-chain cable has a nonlinear load-elongation characteristics. The static characteristics before stress relaxation is applicable to the dynamic analysis.(2) The heaving and pitching motions of the floating structures are negligible, but the surging motion increases as the wave length does.(3) The frequency responses of the tension fluctuations of the cable do not depend on the material in case of the large initial tension. The axial rigidity of the rubber-chain cable is, however, much less than that of the wire cable so that in designing the rubber-chain tension mooring system, we must carefully set the natural frequency of the system sufficiently out of the wave spectrum.(4) The snap load easily occurs when the initial tension is small.(5) The analysis model is applicable to the design of the tension mooring system. It predicts, however, much larger snap load. The authors expect that the analysis model will be improved by including the nonlinear hydrodynamic forces.

正常30例, 異常Q波を有する陳旧性前壁梗塞30例, 異常Q波を有しない陳旧性前壁梗塞32例の体表面電位図を記録し, その極小の位置をQRS開始後5msec毎に比較検討した。正常群と梗塞群の極小の位置は, QRS開始後5, 10, 15, 20, 25msecにおいて危険率0.1%以下の有意差を示した。正常群と, 心電図上診断が容易な異常Q波を有する陳旧性前壁梗塞群あるいは心電図で診断困難な異常Q波を有しない陳旧性前壁梗塞群とはQRS開始後15msecの極小の位置で最もよく区別された。QRS開始後15msecにおいては, 異常Q波を有する梗塞群30例全例の極小が, また, 異常Q波を有しない梗塞群32例では26例の極小が前胸部に位置し, これと異なり正常例では30例中29例の極小が背部に位置した。これらの所見は, 陳旧性前壁梗塞の有無の診断における電位図の有用性を示唆する。

In 24 patlents with old inferoposterior myocardlal infarction, body surface isopotentlal maps were compared with left ventriculographlc findings. In 10 patients with asynergy restricted to the inferior and/or posterolateral segment, surface potential abnormalities due to Infarction were observed during specific phases of QRS and In specific portions on the chest surface depending on the locstton and extent of ventricular severe asynergy (akinesls and dyskinesls). However, the remaining eight patients with coexisting severe asynergy in the anterior, apical, or septal segment showed surface potentlal maps quite different from those of the former patients. It is suggested that body surface lsopotentlal maps are a useful clinical tool for detecting the location and extent of ventricular severe asynergy In patlents with old lnferoposterlor myocardlal infarction. (AM HEART J 104:1262, 1982.)

Body surface isopotential maps were recorded in 30 normal subjects and 32 patients with clinical evidence of old anterior myocardial infarction but without ECG findings of infarction. Position of the minimum in maps was compared at 5 msec intervals from the onset of QRS between the normal and infarction groups. A significant difference in the mean position of the minimum was observed at 5, 10, 15, 20, and 25 msec (p less than 0.001). The minima for the two groups achieved their clearest separation at 15 msec. Twenty-six of the 32 infarction patients showed the minima on the anterior chest, but 29 of the 30 normal subjects showed the minima on the back. These findings suggest the highly specific usefulness of body surface maps for the diagnosis of the presence of old anterior infarction undetectable by 12-lead ECGs.

A newly devised, inexpensive paracentesis gun is described. It is made by modifying a plastic dart gun. Instructions for assembling the gun are given as well as a description of its safe usage in rabbit eyes.