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酢酸繊維素繊維および皮膜の吸湿による密度の変化を有機媒質を用いて浮沈法で測定し, さらに水中の密度も測定した。他の繊維の場合と同じように, 密度は数%の吸湿量で極犬を示す。これらの結果から, 試料内部 (有機媒質の入れない部分) の吸湿量pと全吸湿量xの関係を求めた。三酢酸繊維素繊維 (酢化度61.8%) は二酢酸繊維素繊維 (酢化度54%) よりpが少ない。これは前者の結晶化度が高いためであろう。未処理の三酢酸繊維素皮膜 (酢化度60.5%) は二酢酸繊維素皮膜 (酢化度54.7%) とほとんど同じpの値をもつ。これは両皮膜が似た結晶化度をもつためであろう。また, 繊維, 皮膜とも, p-x曲線は徐々に飽和値まで増大する。

The apparent molal volume of amino acids in aqueous solutions increases with the ionic strength of other simple ions. The relation between molal volume and ionic strength was explained according to Kirkwood's theory. From the fact that this relation is equal for various α-amino acid, it was concluded that the hydration of hydrocarbon part was not accompanied with the electrostriction. Thus the two kinds of hydration are epxected for amino acids, or, more generally, for all water-soluble organic substances.

ビニロン製造工程中の3種類のポリビニルアルコール繊維 (D. P. 1600, 3d), すなわち未処理のもの (A), 熱処理したもの (B), およびさらにホルマール化したもの (C) について, 吸湿による密度の変化を浮沈法により測定した。吸湿量0のA, B, Cの密度は25℃でそれぞれ1.298, 1327, 1, 2789/ccであった。密度一吸湿量の関係でA, Bは吸湿量約2%のところに密度の極大があり, 吸湿量の増えるに従って徐々に密度が減少する。しかしCには極大がないようで, また密度の減少する勾配がA, Bより急である。これらの挙動はポリビニルアルコール繊維の吸着水について若干の示唆を与える。

MK-0521 and captopril were orally administered to acute (6 to 8 days after unilateral renal artery constriction) and chronic (2 to 2.5 months after the constriction) 2-kidney Goldblatt hypertensive dogs for 7 to 21 days. MK-0521 lowered the blood pressure to similar extents in the acute and chronic stages of hypertension. The antihypertensive effect of MK-0521 was dose-dependent and persistent even after its cessation. Captopril also produced an antihypertensive effect, although the effect in the chronic stage of hypertension was less prominent than that in the acute stage of hypertension. MK-0521 was more inhibitory on the renin-angiotensin system than captopril. In the acute stage of hypertension, the dogs treated with MK-0521 had increased angiotensin converting enzyme (ACE) activity, while they had decreased plasma angiotensin II level and elevated plasma angiotensin I level and plasma renin activity. These results clarified the inhibitory effect of MK-0521 on ACE. In contrast, in the chronic stage of hypertension, MK-0521 showed no depression of plasma angiotensin II. There were no significant changes in daily urinary volume, and renal clearances of sodium, potassium and creatinine. These results suggest that the major mechanism of the antihypertensive effect of MK-0521 in 2-kidney Goldblatt hypertensive dogs is an inhibition of the ACE. In addition, the different effects in the acute and chronic hypertensive dogs suggest that some differences exist in the mechanisms of maintaining blood pressure between the two stages of 2-kidney Goldblatt hypertensive dogs.

1. The effects of FUT-175 on the development of adjuvant arthritis in rats were studied and compared with those of indomethacin. FUT-175 inhibited both primary and secondary paw lesions in the adjuvant arthritic rats when it was administered orally on a daily basis from the day before through 18th day after adjuvant injection. 2. In addition, FUT-175 inhibited the increase in hemolytic complement in adjuvant arthritic rats in a dose-dependent manner. 3. Indomethacin also showed an inhibitory effect on the development of arthritic lesion, but had no effect on the increase in hemolytic complement in the adjuvant arthritis in rats. 4. Furthermore, FUT-175 inhibited the activities of various proteases in vitro , and then strongly inhibited complement-mediated hemolysis via the classical and alternative pathways, while indomethacin had no effect on them. 5. These results suggest that the anti-inflammatory activity of FUT-175 may differ from indomethacin in the mechanisms of action and, at least in part, due to the anti-complement activity.

FUT-175 inhibited the zymosan-induced rat paw edema in a dose-dependent manner, while indomethacin exhibited no significant activites in this model. FUT-175 also inhibited the decrease in hemolytic complement (CH50) induced by zymosan in vitro, and indomethacin was inactive. These results suggest that FUT-175 has potent in vitro and in vivo nhibitory activity against the activation of the complement system induced by zymosan.

Two-dimensional maps of the Crab Nebula have been synthesized in 22–64 keV range through the modulation collimator experiment. The effective angular resolution is about 15″. The result indicates that the Crab morphology is strictly controlled by the pulsar.

Prof. Watase will be remembered among Japan’s scientific community as a great leader in cosmic ray physics. He was one of the leaders who revitalized activities in Japan’s physics, which was deeply damaged by the war, and helped to build it up to the present level.

FUT-175, 6-amidino-2-naphthyl p-guanidinobenzoate dimethanesulfonate (nafamstat mesilate), a novel synthetic protease-inhibiting agent, was studied to determine its in vitro effects against various proteases and other enzymes, as well as to determine its in vivo protease inhibitory effects. FUT-175 was found to inhibit, in an intense, specific and reversible way, the enzyme activities of trypsin, C1r, C1s, thrombin, kallikrein and plasmin with IC50 values of the order of 10(-6)-10(-8) M. FUT-175 also inhibited complement-mediated hemolysis, including both classical and alternative pathways, sites of inhibition being on C1r and C1s as evidenced by the intermediate-cell technique. In animal model reactions in which the complement system is known to be involved as pathogenetic factors, e.g., Forssman shock, Forssman cutaneous vasculitis, zymosan-induced paw edema, endotoxin shock and local Shwartzman reaction, FUT-175 was highly effective in that, for example, intravenous dosing at 3 mg/kg could completely protect guinea pigs from the lethal Forssman shock. FUT-175 was also found to be effective in trypsin-induced shock in mice, in lethality due to thrombin-thrombosis in mice and in kinin formation in the inflammatory process in rats.

Angiotensin converting enzyme (ACE) inhibitory activity of MK-0521 in dogs and the effects of its single oral administration on blood pressure and the renin-angiotensin system in 2-kidney Goldblatt hypertensive dogs were compared with those of captopril and MK-421. MK-0521 at 0.001-0.1 mg/kg, i.v., or 0.01-1 mg/kg, p.o., attenuated the pressor effect of angiotensin I without affecting that of angiotensin II and augmented the depressor effect of bradykinin. The potency of MK-0521 to reduce the pressor effect of angiotensin I was 9.8 times that of captopril by intravenous administration, and by oral administration, it was 15.9-32.1 times that of captopril and approximately 3 times that of MK-421. When administered orally, the onset of action and the time to peak effectiveness were more rapid than those of MK-421, but slower than those of captopril. Duration of the action of MK-0521 was longer than that of captopril and equal or longer than that of MK-421. The inhibition of ACE was well correlated with serum MK-0521 levels. MK-0521 produced a dose-dependent antihypertensive effect in 2-kidney Goldblatt hypertensive dogs at over 0.3 mg/kg, p.o., without affecting the heart rate. The antihypertensive effect of MK-0521 was persistent and approximately 3 times more potent than that of captopril. MK-0521 inhibited the serum ACE activity and increased the plasma renin activity, while it had a tendency to decrease plasma aldosterone level. These changes were parallel to the time course of the antihypertensive effect. These results suggest that the main mechanism of the antihypertensive effect of MK-0521 is the suppression of angiotensin II production due to the inhibition of the ACE.

Observational results on X-ray bursts obtained by the Japanese X-ray satellite are reviewed in conjunction with the general context of the neutron star model of the burst. Evidence indicates the existence of physically different kinds among type-I bursts which are widely believed to be from a thermonuclear flash occurring on the surface of a neutron star. There are cases which can not be accounted for by a simple nuclear flash model: The flash in a confined region of the surface and a change of the emitting area during the burst are suggested. Two type-I bursts were observed in succession within a short interval which was not of sufficient duration to accumulate the nuclear fuel for a flash. Coordinated optical/X-ray observations of bursts were performed. Optical bursts are tentatively interpreted in terms of the reprocessing of X-rays are at the accretion disk. The results will provide the basis for a discussion of the physical structure of the system. The evolution of the activity of type-II bursts from the rapid burster was observed from its onset for about two weeks and a novel mode of burst activity was discovered.

Several subjects are selected from observational results on X‐ray pulsars and X‐ray burst sources obtained by the Japanese X‐ray astronomy satellite ‘‘Hakucho.’’ Results on Vela X‐1 and A0535+262 which exhibited transient or time vaiable pulsar behavior are discussed. We are lead to speculate that the category of Class‐II X‐ray sources, represented by X‐ray sources in globular clusters, very bright sources within 30° of the galactic center, GCX sources and soft transient sources, may be characterized by its potentiality for bursting whenever certain, yet unknown, conditions are fulfilled. The results on the X‐ray burst may provide keys to evolve the thermonuclear flash model from the simplified original He‐flash version to explain much involved dynamic processes in the neutron star atomsphere. Necessity of reservoirs at the neutron star to store matter as the nuclear fuel or the source of gravitational energy appears to be evident in order to explain observational facts of the bursts. Some of the difficul...

N-alpha-[(S)-1-carboxy-3-phenylpropyl]-L-lysyl-L-proline (MK-0521) is a new non-sulfhydryl-containing angiotensin converting enzyme (ACE) inhibitor. The present investigation describes its ACE and other enzymes inhibitory properties and compares it to those of captopril, MK-421 and MK-422 in vitro. MK-0521 inhibited rat pulmonary ACE by 50% (IC50) at a concentration of 3 nM and was 6.13 times more potent than captopril. The IC50 values of MK-421 and MK-422 against ACE were 2,000 nM and 3.5 nM, respectively. MK-0521 had practically no inhibitory activities against carboxypeptidase A, carboxypeptidase B, leucine aminopeptidase, papain, pepsin and trypsin. The kinetic study on the inhibitory activity of M-0521 against ACE using Lineweaver-Burk plots indicated that MK-0521 exerted competitive ACE inhibition. The dialysis study conducted on the ACE-MK-0521 complex revealed that the inhibitory effect of MK-0521 against ACE was reversible. In the guinea pig ileum, MK-0521 potentiated the contractile effect of bradykinin and depressed the contractile effect of angiotensin I. These effects on bradykinin and angiotensin I were 33.11 and 2.63 times more potent than that of captopril, respectively. The present results suggest that MK-0521 may show a potent hypotensive effect in vivo.

The present status of observations of the diffuse cosmic X-rays is discussed. The energy spectrum in the energy range 1–100 keV has been well established. The flux around 0.25 keV appears to be rather high. The basis of the classical argument that the integration of normal galaxies in the universe is not sufficient to explain the diffuse X-ray flux is re-examined. Recent observations around 0.25 keV are discussed and results are compiled.

We performed a couple of balloon experiments to measure the size and the location of Cyg-X-1 using the techniques of the modulation collimator [1]. The angular periods of the modulation collimator were 26′ and 10′ for the respective flights corre­sponding to the approximate angular resolutions of the size determination and location, 3′ and l′ respectively. Preliminary results of the experiment with 3′ resolution are reported here.*

Modulation collimators have been used in recently reported work to determine the angular sizes and celestial positions of the X-ray sources Sco X-1 and Taurus XR-1 (Crab Nebula) with precisions of 15″ to 30″. The measurements were made by means of four-grid collimators, star photography and optical imaging of the collimators. In the present paper we discuss (1) the principles and uses of various forms of the modulation collimators as they pertain to X-ray astronomy, (2) several methods for determining the celestial positions of X-ray sources with these collimators, (3) the techniques for the alignment and calibration of these detection systems, (4) an image-forming collimator, and finally, (5) some of the optical properties of these grid systems. The modulation collimator is quite versatile and is particularly suited for measurements from spacecraft with relatively poor pointing capability. Thus it should be a useful tool in X-ray astronomy for some years to come.

THE purpose of this article is to present a preliminary report on a new cosmic X-ray source. The source was observed near Sco X-1 during recent rocket flights to observe Sco X-1 simultaneously with ground-based optical telescopes. It is very likely that we observed the source reported to have appeared between July 6 and July 9 by Conner et al. in an IAU telegram issued on July 30, 1969.

Angular diameters of X-ray source regions in Scorpio and Sagittarius constellations by rocket measurement with collimator

FUT-175 has been reported by S.Fujii et al.1) to inhibit strongly Clr, Cls, trypsin and thrombin as well as kallikrein and plasmin. In the present study, effects of FUT-175 on the complement and kallikrein system were investigated in vitro and in vivo. The in vitro complement-mediated hemolysis via classical pathway activation was performed as described by Mayer et al., and the systemic Forssman shock in guinea pigs was induced by the method of Glovsky et al. The in vitro kinin formation was performed with glass powder in rat plasma. The anti-inflammatory effects of FUT-175 were also studied on kaolin- and scald-induced edema of rat paws. FUT-175 markedly inhibited the complement-mediated hemolysis, the IC50 being 4.5 × 10−8 M, and protected the guinea pig from the systemic Forssman shock at doses of 0.3 - 3 mg/kg, i.v., in a dose-dependent manner. FUT-175 also inhibited the in vitro kinin formation with the IC50 of 1.1 × 10−7 M (glass powder) and reduced the kaolin- and scald-induced edema formation at doses of 30 - 300 mg/kg, p.o..

Collimator with wide fields of view detectors designed for extraterrestrial X-ray source measurements

X-ray source in Crab Nebula size and position, showing visible light distribution having common center within 15-inch precision of measurement and finite angular extent

THE discovery of galactic X-rays by Giacconi et al.1, confirmed by Friedman et al.2, which was quite unexpected from our present understanding of physical processes in astronomical objects, has induced a variety of theoretical investigations3. Among various mechanisms so far proposed to explain the X-ray sources, the neutron-star hypothesis suggested by several authors4 seems to present a reasonable combination of the radiative power, the distance, the life and the frequency of occurrence of the X-ray sources although the existence of neutron stars is still open to question.

Optical identification of position of X-ray astronomical source Sco X-1, noting similarity of certain properties with old novae