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Acute myocardial infarction (AMI) remains one of the most serious heart diseases and elucidation of its pathogenesis and advances in treatment strategies have been desired. In 2009, to understand the status of AMI in Fukushima Prefecture for improving treatment outcomes, a new AMI registration survey system was conducted throughout the prefecture. A total of 1,556 cases were registered in the initial 2 years from 2009 to 2010. The hospital-based overall incidence of AMI in Fukushima Prefecture was 37.9 people per population of 100,000 per year. Mortality from AMI within 30 days of onset was 10.2%. We report herein the actual situation of AMI onset and treatment in Fukushima Prefecture based on the initial results of the survey.

The SAR at adenosine (P 1 ) and ATP (P 2 ) receptors is reviewed, with emphasis on recently developed selective agonists and antagonists. These include partial (e.g., N 6 -ethyl-8-cyclopentylaminoadenosine) and full A 1 agonists (e.g., NNC 21-0136, 2-chloro-N 6 -[(R)-(benzothiazolylthio-2-propyl]adenosine), A 2 antagonists (e.g., the non-xanthines: SCH58261, 5-amino-7-(phenylethyl)-2-(2-furyl)-pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine and ZM241385, 4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo[2,3a][1,3,5]triazinyl-amino]ethyl)-phenol; and the 1-propargyl-8-styrylxanthines), and A 3 agonists (e.g., CI-IB-MECA, 2-chloro-N 6 -(3-iodobenzyl)-adenosine-5'-N-methyluron-amide). Novel adenosine receptor antagonists (e.g., BTH 4 , ethyl 3-benzylthio-4,5,6,7-tetrahydro-benzo[c]thiophen-4-one-1-carboxylate) have been discovered through screening libraries of natural products and heterocyclic derivatives. The first A 3 selective antagonists to be identified include derivatives of flavones (MRS 1067), 1,4-dihydropyridines (MRS 1097), triazolonaphthyridine (L-249313), and thiazolopyrimidine (L-268605). Potent P 2 receptor agonists are known. For example, 2-HexylthioAMP is a highly potent agonist at the yet uncloned P2Y receptor in C6 glioma cells. Suramin is a weak and non-selective P 2 blocker, while a truncated derivative, NF023, appears to be selective for P2X receptors. More selective P 2 antagonists are under development, with the cloning of these receptors. [ 35 S]ATP-γ-S has been used as a radioligand for the direct labeling of several subtypes of cloned P2X receptors (P2X 1 -P2X 4 ).

A 6-hr continuous infusion of 2-[p-(2-carboxyethyl)phenylethylamino]-5'-N-ethylcarboxamidoadenos ine (CGS21680), a selective A2a-adenosine agonist, into the subarachnoid space underlying the ventral surface region of the rostral basal forebrain, which has been defined as the prostaglandin (PG) D2-sensitive sleep-promoting zone, at rates of 0.02, 0.2, 2.0, and 12 pmol/min increased slow-wave sleep (SWS) and paradoxical sleep (PS) in a dose-dependent manner up to 183% and 202% of their respective baseline levels. The increments produced by the infusion of CGS21680 at 0.2 and 2.0 pmol/min were totally diminished when the rats had been pretreated with an i.p. injection of (E)-1,3-dipropyl-7-methyl-8-(3,4-dimethoxystyryl)xanthine (KF17837; 30 mg/kg of body weight), a selective A2-adenosine antagonist. In contrast, the infusion of N6-cyclohexyladenosine (CHA), a selective A1-adenosine agonist, at 2 pmol/min significantly suppressed SWS before causing an increase in SWS, and a decrease in PS was also markedly visible. Essentially the same effects of CGS21680 and CHA were observed when these compounds were administered to the parenchymal region of the rostral basal forebrain through chronically implanted microdialysis probes. Thus, we clearly showed that stimulation of A2a-adenosine receptors in the rostral basal forebrain promotes SWS and PS. Furthermore, i.p. injections of KF17837 at 30 and 100 mg/kg of body weight dose-dependently attenuated the magnitude of the SWS increase produced by the infusion of PGD2 into the subarachnoid space of the sleep-promoting zone, thus indicating that the A2a-adenosine receptors are crucial in the sleep-promoting process triggered by PGD2.

An 11C-labeled selective adenosine A2A antagonist, (E)-8-(3,4-dimethoxystyryl)-1,3-dipropyl-7-[11C]-methylxanthine ([11C]KF17837), was prepared by reaction of (E)-8-(3,4-dimethoxystyryl)-1,3-dipropylxanthine and [11C]methyl iodide with decay-corrected radiochemical yield of 19-50%, radiochemical purity of99%, sp. act. of 17-100 GBq/mumol and preparation time of 20-25 min. In mice, the myocardium showed the highest (13.4% ID/g) at 5 min after i.v. injection, which decreased gradually with time. The specific myocardial uptake was visualized by gamma-camera. In the brain region the radioactivity level was higher in the A2A receptors-rich striatum than in the cortex and cerebellum. The specific striatal uptake in rats was clearly demonstrated by PET. These results have shown that [11C]KF17837 is a potential PET radioligand for mapping the adenosine A2A receptors in the heart and brain.

A patient with reentrant ventricular tachycardia exhibited both the orthodromic and antidromic resetting responses at a single intracardiac recording site during programmed extrastimulation of ventricular tachycardia. The transition from orthodromic to antidromic resetting with extrastimulation demonstrated a sudden shortening in conduction interval to an electrogram recording site and unexpected identical morphology of the spontaneous and captured electrograms at that site, indicating atypical antidromic resetting. This newly observed resetting phenomenon with programmed extrastimulation suggests that the fourth entrainment criterion with overdrive pacing may likely be demonstrated in an atypical form; that is, a sudden shortening in conduction interval to an electrogram recording site may occur without any significant change in the bipolar electrogram morphology at that site when overdrive pacing is performed during tachycardia from a single pacing site at two different constant rates.

1. We demonstrate that 8-(noradamantan-3-yl)-1,3-dipropylxanthine (KW-3902) is a very potent and selective adenosine A1 receptor antagonist, assessed by radioligand binding and cyclic AMP response in cells. 2. In rat forebrain adenosine A1 receptors labelled with [3H]-cyclohexyladenosine (CHA), KW-3902 had a Ki value of 0.19 nM, whereas it showed a Ki value of 170 nM in rat striatal A2A receptors labelled with [3H]-2-[p-(2-carboxyethyl)-phenethylamino]-5'-N-ethylcarboxamidoad enosine (CGS21680), indicating 890 fold A1 receptor selectivity versus the A2A receptor. KW-3902 at 10 microM showed no effect on recombinant rat A3 receptors expressed on CHO cells. 3. Saturation studies with [3H]-KW-3902 revealed that it bound with high affinity (Kd = 77 pM) and limited capacity (Bmax = 470 fmol mg-1 of protein) to a single class of recognition sites. A high positive correlation was observed between the pharmacological profile of adenosine ligands inhibiting the binding of [3H]-KW-3902 and that of [3H]-CHA. 4. KW-3902 showed potent A1 antagonism against the inhibition of forskolin-induced cyclic AMP accumulation in DDT1 MF-2 cells by the A1-selective agonist, cyclopentyladenosine with a dissociation constant (KB value) of 0.34 nM. KW-3902 antagonized 5'-N-ethylcarboxamidoadenosine-elicited cyclic AMP accumulation via A2B receptors with a KB value of 52 nM. 5. KW-3902 exhibited marked species-dependent differences in the binding affinities. The highest affinity was for the rat A1 receptor (ki = 0.19 nM) and these values for guinea-pig and dog A1 receptors were 1.3 and 10 nM, respectively.

During retrograde conduction through an accessory pathway (AP) or the atrioventricular (AV) node, earlier activation of the distal recording site than a more proximal site of the coronary sinus (CS) generally indicates retrograde conduction via a distally located AP. Thus, after successful ablation of a left-sided AP, if the distal CS recording site is activated earlier than a more proximal site retrogradely, it is considered to suggest-in the absence of His-bundle recording or more frequently in the setting of poor recording of the low septal right atrial electrogram-a conduction via a second AP (located more distally), and not conduction via the AV node. Yet, we hypothesized that retrograde conduction through the AV node may activate the far distal site of the CS (CSD) earlier than a more proximal site, as the anterior atrial wavefront, coming retrogradely from the AV node and traveling along the anterior mitral annulus, could reach the CSD earlier than a more proximal site. To test this we studied 18 patients with intact retrograde conduction via the AV node, but without evidence of an AP. The CSD was recorded by means of a quadripolar catheter (interelectrode distance of 2-5 mm); retrograde activation sequence at the distal (CSD1-2) versus proximal (CSD3-4) bipolar recording site was determined during ventricular stimulation. In 12 of 18 patients the CSD1-2 recording site was activated 5-10 ms earlier than the CSD3-4 recording site, in 3 of 18 patients the CSD1-2 site was activated 5 ms later than the CSD3-4 site; in the remaining 3 patients both recording sites were depolarized simultaneously. The results indicate that the CSD was often depolarized earlier than a more proximal site by impulses that conducted to the atria retrogradely via the AV node while the quadripolar recording catheter was placed at the CSD. This observation, although not well documented previously, suggests that the sequence of retrograde atrial activation in the CS should be studied carefully in consideration of the actual location of the mapping catheter in order to correctly diagnose the presence or absence of conduction via an AP.

A transparent composite film of poly(vinyl alcohol) (PVA) and silica was obtained through the sol-gel process using tetraethoxysilane (TEOS). By ESCA and X-ray diffraction measurements on the composite, it is confirmed that the PVA and silica were intimately mixed together. The Young's modulus increased with increasing silica content in the PVA, but the tensile strength decreased from 84 for pure PVA to 40 MPa (as the PVA content reaches 50 wt%). A maximum value of 145 MPa was observed for the 80% PVA composite. The composite could be drawn to 2∼3 times its original length under saturated humidity conditions. The modulus and the tensile strength were increased by a factor of two by the drawing of the as-cast composite film. The residuals created by the removal of PVA from the composite films were transparent and showed a surface area of about 500 m2g−1 (in the case of 80% PVA as the original material). The residuals showed permeability for gases. The gas permeability of the residuals rapidly increased with the PVA content in the original materials.

The purpose of this study is to investigate the relation between vibration and heat generation in superconducting magnets (SCMs) for magnetically levitated vehicles, and to determine the SCM structure which reduces heat generation. Thus, two experimental SCMs are designed and produced. First, vibration tests are performed, in which electromagnetic forces due to the ripple magnetic fields from ground coils are applied to the outer vessels of these SCMs. These results clarify vibration modes causing high heat generation in SCMs, i. e., a torsion, a bending, a yawing, and a rolling mode. Second, some eigenvalue analyses involving variation of positions of load supports for an inner vessel are performed, using a simple finite element model. These results are used to determine the optimum supporting method of inner vessels which prevents the resonances with the vibration modes causing high heat generation.

デルタ波の極性と頻拍中の逆行性P波の極性の不一致より複数副伝導路の存在が推定され, アブレーションによりその存在が証明された1例を報告する.症例は房室回帰性頻拍 (1種類) を合併した顕性WPW症候群の男性である.体表心電図ではII, III, aVF誘導にて陰性デルタ波を認め, 副伝導路 (AP) は (左室) 後壁側に存在すると推定された.頻拍中の逆行性P波はII, III, aVF誘導で陽性であった.同症例に対して電気生理学的検査およびカテーテルアブレーションを施行した.頻拍中の最早期興奮部位は左室前側であり, 同部位での2回の通電により頻拍は誘発不能となり, 逆伝導は房室結節経由となったが, 陰性デルタ波は不変であった.切断された左室前側壁のAP以外に, 後壁寄りに川頁伝導のみ可能な2本目のAPの存在することが推定された.最短房室伝導時間を示す左後中隔部位での1回の通電によりデルタ波は消失し, QRS波は正常化した.体表心電図における陰性デルタ波と頻拍時の陽性P波の所見は2本の副伝導路の可能性を示唆しているものと推察された.

Pore structure-controlled silica gels were obtained by calcination (600°C, 1h in air) of silica/poly (ethyene glycol) (PEG) (50/50 wt%) composites. The molecular weight (MW) of PEG used ranged from 200 to 70000. Nitrogen adsorption isotherms of silica gels were measured at -196°C, and the pore characteristics were evaluated. When the MW of PEG was 2000, the values of the specific surface area and average pore diameter showed a maximum and a minimum of 1174 m2/g and 1.33nm. respectively. These results were explained based on the dispersion model for PEG in the composites before calcination. It was assumed that in the MW region below 2000, PEG molecules were associated while PEG molecular chains were entangled with each other in the MW region above 2000. PEG molecules having MW close to 2000 were supposed to be dispersed monomolecularly, and the pore structure of silica gels obtained reflected the structure of the composites.

The composites of silica and poly (vinyl alcohol) (PVA) were prepared by sol-gel process. The composites containing more than 50wt% of PVA could be drawn in water at 50°C. The maximum draw ratio of the composites containing 50 and 80wt% of PVA were about 2.5 and 5.5, respectively. The porous silica gels were obtained by calcination of these composites at 600°C for 6 h. The obtained silica gels showed large specific surface area (700 to 950m2/g) and had micropores and mesopores of diameters of less than 10nm. The average pore size and the pore volume could be changed by drawing the composites before calcination.

Permselective membranes were prepared by grafting of dimethylsiloxane to poly (styrene-co-maleic anhydride) membrane with the reaction of an amino group in DMS and a maleic anhydride group in the copolymer. The grafting reaction penetrated into the copolymer membrane with sharp boundary fronts formed. The gas permeation characteristics of the membrane obtained were close to the values of poly (dimethylsiloxane) membrane. The permeability coefficient was on the order of magnitude of 10−8 [cm3(STP) cm/cm2 s cmHg] for O2 gas, and gave an ideal separation factor of 2.3 for the O2N2 system. The gas permeability was controlled with change of the dimethylsiloxane content and the molecular weight of dimethylsiloxane in the graft membrane. High permselective membranes were prepared with ease by an application of the above grafting technique onto commercial porous membranes. The permeation coefficients of O2 through the membranes were 1.5–6.8 × 10−8 and the ideal separation factors were improved to 4.5-2.4 for the O2N2 system.

Bradycardia-dependent block or activation delay of the atrial tissue has not been documented in the literature. A patient with sick sinus syndrome in whom bradycardia-dependent, as well as tachycardia-dependent, activation delay in the atria was elucidated is reported on. The phenomenon of bradycardia-dependent activation delay was reproducibly demonstrated, both during atrial extrastimulation and incremental atrial pacing from the high right atrium, in the setting of an abnormally prolonged activation interval from the distal stimulating electrodes to the proximal recording electrodes of a quadripolar catheter, which was localized in the high right atrial region. Supernormal conduction seemed to be an unlikely explanation for the observed phenomenon.

His-Purkinje系及び副伝導路の逆伝導においていわゆる過常伝導現象が観察された潜在性WPW症候群の1例を報告する.症例は55歳の女性で動悸発作の精査のため入院となった.電気生理学的検査時, 右房, 左房刺激では△波の出現をみなかった.心房頻回刺激法, 心房期外刺激法により通常型房室結節リエントリー性頻拍と右前中隔部位の潜在性Kent束を介する房室リエントリー性頻拍が誘発された.心室期外刺激法の際, 予期せぬ室房伝導時間の短縮現象が観察された.連結期500msec～380msecでは逆行性His束波までの伝導時間 (S2-H2時間) の短縮に伴い室房伝導時間が短縮し, また連結期330msec～320msecでは, S2-H2'時間は延長していたが室房伝導時間は短縮していた.前者はHis-Purkinje系の逆伝導における過常伝導が, 後者は副伝導路の逆行性過常伝導が推測された.副伝導路の逆行性過常伝導は稀に報告されているが, His-Purkinje系における逆行性過常伝導はいまだ報告がなく, 極めて稀な現象であると考えられた.

PURPOSE The objective of this assessment is to identify prognostic factors of recurrence and disease progression of primary superficial transitional cell carcinoma of the bladder. PATIENTS AND METHODS TUR-Bt was performed in 150 patients with initial superficial bladder cancer, of which pathological diagnosis was pTa or pT1 transitional cell carcinoma. The recurrence and progression free survival was examined. The clinicopathological factors analyzed were as follows: grade, pT, tumor size, tumor number and tumor form. RESULTS Median follow-up period was 39 months (range 3-184). The age distribution was from 25 to 98 years old with the average of 67. The patients were 122 males and 28 females. Recurrence was observed in 72 patients. The 5-year recurrence free rate for all cases were 41.6%. The factors found to be of significance for the prognosis for recurrence were tumor size (1 cm

Evacuated feces after intraperitoneal administration of selective adenosine receptor antagonists were evaluated in rats. The selective adenosine A 1 receptor antagonists, 1,3-dipropyl-8-cyclopentylxanthine (DPCPX) (100–300 μg/kg i.p.) and ( R )-7,8-dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1 H -imidazo[2,1- i ]purin-5(4 H )-one (KF20274) (30–300 μg/kg i.p.), significantly increased defacation, whereas the selective adenosine A 2 receptor antagonist 4-amino-8-chloro-1-phenyl[1,2,4]triazolo[4,3- a ]quinoxaline (CP-66,713) failed to cause a significant increase at up to 10 mg/kg i.p. The defacation caused by DPCPX (100 μg/kg) was markedly alleviated by (2 S )- N 6 -(2- endo -norbornyl)adenosine (( S )-ENBA) (30–300 μg/kg s.c.), a selective adenosine A 1 receptor agonist, but not influenced by 2-[ p -(2-carboxyethyl)phenethylamino]-5′- N -ethylcarboxamidoadenosine (CGS 21680) (30–1000 μg/kg s.c.), a selective adenosine A 2 receptor agonist. These results suggest that endogenous adenosine plays a physiological role in sustained inhibition of defecation via adenosine A 1 receptors.

A microporous silica/FeOn catalyst was prepared by calcination with poly(vinyl alcohol) (PVA). The surface area of the catalyst increased with the content of PVA in original composite. Because of the cylindrical shape of the pore, it was assumed that in the composite PVA chains existed in bundles of 20-30. The silica/FeOn composite showed catalytic activity for H2 isomerization. The rate of isomerization followed first-order reaction kinetics and the activity increased almost proportionally to the surface area, which corresponded to PVA content in the original composite. The Arrhenius plot showed a positive slope, in contrast to ordinary reactions. The activation energy was apparently -2 kJ/mol. This result is explained on the basis of the paramagnetic susceptibility of FeOn, which decreases with increasing temperature.

Objectives. This study attempted to determine the prevalence and electrocardiographic (ECG) lead distribution of T wave “humps” (T2, after an initial T wave peak, T1) among families with long QT syndrome and control subjects.Background. T wave abnormalities have been suggested as another facet of familial long QT syndrome, in addition to prolongation of the rate-corrected QT interval (QTc), that might aid in the diagnosis of affected subjects.Methods. The ECGs from 254 members of 13 families with long QT syndrome (each with two to four generations of affected members) and from 2,948 healthy control subjects (age ≥ 16 years, QTc interval 0.39 to 0.46 s) were collected and analyzed. Tracings from familes with long QT syndrome were read without knowledge of QTc interval or family member status (210 blood relatives and 44 spouses).Results. We found that T2 was present in 53%, 27% and 5% of blood relatives with a “prolonged” (≥ 0.47 s), “borderline” (0.42 to 0.46 s) and “normal” (≤0.41 s) QTc interval, respectively (p < 0.0001), but in only 5% and 0% of spouses with a borderline and normal QTc interval, respectively (p = 0.06 vs. blood relatives). Among blood relatives with T2, the mean [±SD] maximal T1T2 interval was 0.10 ± 0.03 s and correlated with the QTc interval (p < 0.01); a completely distinct U wave was seen in 23%. T2 was confined to leads V2and V3in 10%, whereas V4, V5, V6or a limb lead was involved in 90% of blood relatives with T2. Among blood rotatives with a borderline QTc interval, 50% of those with versus 20% of those without major symptoms manifested T2 in at least one left precordial or limb lead (p = 0.05). A T2 amplitude > 1 mm (grade III) was observed, respectively, in 19%, 6% and 0% of blood relatives with a prolonged, borderline and normal QTc interval with T2 in at least one left precordial or limb lead. Among the 2,948 control subjects, 0.6% exhibited T2 confined to leads V2and V3, and 0.9% had T2 involving one or more left precordial lead (but none of the limb leads). Among 37 asymptomatic adult blood relatives with QTc intervals 0.42 to 0.46 s, T2 was found in left precordial or limb leads in 9 (24%; 5 with limb lead involvement) versus only 1.9% of control subjects with a borderline QTc interval (p < 0.0001).Conclusions. These findings are consistent with the hypothesis that in families with long QT syndrome, T wave humps involving left precordial or (especially) limb leads, even among asymptomatic blood relatives with a borderline QTc interval, suggest the presence of the long QT syndrome trait.

KF17837 is a novel selective adenosine A2A receptor antagonist. Oral administration of KF17837 (2.5, 10.0 and 30.0 mg/kg) significantly ameliorated the cataleptic responses induced by intracerebroventricular administration of an adenosine A2A receptor agonist, CGS 21680 (10 micrograms), in a dose-dependent manner. KF17837 also reduced the catalepsy induced by haloperidol (1 mg/kg i.p.) and by reserpine (5 mg/kg i.p.). These anticataleptic effects were exhibited dose dependently at doses from 0.625 and 2.5 mg/kg p.o., respectively. Moreover, KF17837 (0.625 mg/kg p.o.) potentiated the anticataleptic effects of a subthreshold dose of L-3,4-dihydroxyphenylalanine (L-DOPA; 25 mg/kg i.p.) plus benserazide (6.25 mg/kg i.p.). These results suggested that KF17837 is a centrally active adenosine A2A receptor antagonist and that the dopaminergic function of the nigrostriatal pathway is potentiated by adenosine A2A receptor antagonists. Furthermore, KF17837 may be a useful drug in the treatment of parkinsonism.

In patients with dual atrioventricular (AV) nodal pathways, double ventricular responses to a single atrial depolarization have been shown to occur, but virtually only during a trial pacing in sinus rhythm. We report on a patient with a slow-fast form of AV nodal reentrant tachycardia who exhibited double ventricular responses following extrastimulation during AV nodal reentrant tachycardia. The phenomenon of double ventricular responses during the tachycardia was demonstrated by ex trastimulation from the proximal coronary sinus. Retrograde unidirectional block in the slow pathway, and an anterograde effective refractory period that was shorter in the fast pathway than that in the slow pathway, are suggested.

High rigidity type superconducting magnet (SCM) is developed and tested by electromagnetic vibration simulator which simulate the actual running condition. To reduce the increase of heat load by the vibration of cryostat, several kind of design concepts are chosen. It is recognized by the experiment result that the most effective design concept is to increase the characteristic frequency in twisting mode of inner vessel with the high rigidity outer vessel.

左上大静脈遺残, 心房中隔欠損症および肺静脈還流異常と診断された52歳の女性に, 動悸の精査を目的として心臓電気生理学的検査を施行したところ, 機序の異なる2種類のlongRP′頻拍 (SVTI, SVT2) が誘発された.SVT1は基本周期450msecの右室期外刺激法により誘発され, 頻拍周期は370msecで, 最早期心房興奮部位はヒス東電位図上の下位中隔右房であった.室房伝導曲線は減衰伝導を示した.頻拍中右室単一刺激法で, ヒス束の不応期に加えられた刺激が心房を捕捉したことにより, 前中隔部位に存在する減衰伝導性の“slowKent”束を経由する房室リエントリー性頻拍 (AVRT) と診断した.SVT2は右房連続刺激法により誘発され, 頻拍周期340mseGで, 最早期心房興奮部位は冠静脈洞入口部近位であった.頻拍中右室単一刺激はすべての連結期で頻拍をリセットしなかった.本例は二重房室結節伝導路を示し, SVT2の機序として稀有型房室結節リエントリー性頻拍が強く示唆されたが, 後中隔部位の“slowKent”束を介するAVRTの可能性は完全には否定し得なかった.

In order to obtain a fundamental knowledge of polymer blends, the rheological and thermal properties of two model blend-systems, (i) styrene-ethylene·butylene-styrene block copolymer (SEBS) and polystyrene (PS) and (ii) SEBS and polyethylene (PE), were investigated. And the effects of the interactions between the common segments of the component polymers on these properties and the mixed structures were discussed.(1) The molten blends of SEBS and PS showed abnormal increases in the viscosities and the moduli and the remarkable decrease in the activation energy of flow at some mixed compositions. The flow curves of these blends exhibited remarkable yielding behaviors at low strain rate region. In these cases, the shear viscosity-shear rate curves of the blends did not coincide with the complex viscosity-angular velocity curves, and this result suggested, from the Cox-Merz rule, the existence of some heterogenous mixed structures in the molten state. Furthermore, these blends kept the high moduli even at low angular velocity region, suggesting the longer relaxation time due to the formation of some heterogeneous high order-structures. (2) In the SEBS/PE blends, such abnormal rheological behaviors could not be recognized but the approximately additive relations with the blend compositions were observed. (3) From the thermal analysis, the partial compatibilities between the component polymers through the common segment-units were recognized in both of the SEBS/PS and the SEBS/PE blend-systems. (4) From these results of the rheological behaviors and the thermal analysis, the complicated mixed structures of the SEBS/PS blends, due to the partial solubility of the PS chains into the St-domains of the SEBS and the consequent enlargement of the domain structures, were proposed.

To determine the optimal temperature for catheter heat mapping without damaging cardiac tissue, we studied the electrophysiologic and histologic responses of the atrioventricular (AV) conduction system exposed to a specific range of temperatures. In 18 closed-chest dogs, an electrode catheter with a thermistor, tip was positioned transvenously at the AV junction. Radiofrequency current (RFC) was applied in incremental temperature steps until transient 2nd-degree AV block was induced. Catheter tip temperature (CTT) was measured at each step. RFC was immediately discontinued when AV block occurred. AV conduction was evaluated before and 4 weeks after the procedure. Acute transient 2nd-degree AV block was induced in 45 applications, during which the average CTT was 48.7 +/- 2.7 degrees C. In another 40 applications in which 2nd degree AV block was not induced, the average CTT was significantly lower [46.3 +/- 2.5 degrees C] (p0.001). Eleven of 16 dogs showed acute 2nd-degree AV block, but had normal AV conduction at 4 weeks (Group A). In the other 5 dogs, 1st-degree AV block was seen at 4 weeks (Group B). The lowest CTTs in Groups A and B were 45 and 49 degrees C, respectively. Histologic findings in 2 dogs from Group A revealed that 10-15% (by area) of the AV node was fibrotic. These findings suggest that the induction of fully reversible AV block can be achieved by titration of RFC, during the application of RFC to the AV junction. In conclusion, RF energy was used to produce a tip temperature of between 45 degrees C and 49 degrees C, which induced reversible and significant interruption of conduction of in tissue in the AV junction, and presumably also in target sites in clinical RF ablation.

A 15-year-old girl developed a rare case of subdural hygroma after foramen magnum decompression for Chiari type 1 malformation manifesting as rapid symptom deterioration around 10 days after uncomplicated operation with uneventful immediate postoperative course. Progressive enlargement of the subdural hygroma in both supra- and infratentorial spaces was followed by the development of hydrocephalus. Syringomyelia improved shortly after the first operation but then deteriorated with massive presyrinx formation. Reoperation with wide opening of the arachnoid membrane lead to a rapid resolution of the hydrocephalus and the presyrinx. The present case shows that wide opening of the arachnoid membrane is an effective therapeutic option.

We present a rare case of chondroma originated from the dura mater of the cerebral convexity in a 16-year-old girl. Radiologic findings are reported with emphasis on computed tomography and magnetic resonance imaging scans, and histogenesis is briefly discussed.

A series of quinolinecarboxylic acid derivatives has been previously described as a new class of 5-HT3 receptor antagonists due to deviation of a carbonyl moiety from the place of an aromatic ring in their minimum-energy conformations. These derivatives were evaluated in a wrap-restraint stress-induced defecation model in rats. Reference compounds, ondansetron (1), granisetron (2), and YM060 (4), potently inhibited a stress-induced increase in stools excreted from fed rats (ID50 = 0.27, 0.12, and 0.0052 mg/kg, po, respectively). However, quinoline derivatives exhibited different activities depending on structural class. 4-Hydroxyquinoline-3-carboxylic acid derivatives 5 and 6a possess high affinity for the 5-HT3 receptor (Ki = 6.1 and 1.5 nM, respectively) and exhibit potent activity in the Bezold-Jarisch (B-J) reflex test (ED50 = 0.0017 and 0.000 10 mg/kg, i.v., respectively), but they did not effectively inhibit the increase in fecal pellet output at the dose of 1 mg/kg, po. On the other hand, most of 1-substituted 2-oxoquinoline-4-carboxylates 10 showed less potent activity in the B-J reflex test than 1 or 2 but inhibited restraint stress-induced defecation more potently than 1 or 2. The ID50 value of endo-8-methyl-8- azabicyclo[3.2.1]oct-3-yl 1-isobutyl-2-oxo-1,2-dihydro-4- quinolinecarboxylate 10e was 0.013 mg/kg, po. With respect to the selected compounds 6a and 10e, effects of 5-HT- and thyrotropin-releasing hormone (TRH)-induced defecation, castor oil-induced diarrhea and wrap-restraint stress-induced colonic propulsion in rats were examined. These 5-HT3 receptor antagonists did not effectively inhibit castor oil-induced diarrhea, which has been reported not to be mediated via the 5-HT3 receptor. Although 10e showed 800-fold decreased potency compared with 4 in the B-J reflex test, 10e exhibited activity as potent as 4 in 5-HT- and TRH-induced defecation assays; 10e exhibited 7-fold increased potency compared with 4 in wrap-restraint stress-induced colonic propulsions. From these results, 10e appears to interact selectively with 5-HT3 receptors in the gastrointestinal system and might be effective in the therapy of irritable bowel syndrome (IBS).

Adenosine A2a receptors have been localized to GABAergic striatopallidal neurons, but their functional role is unknown. To address this question, the modulation of endogenous GABA release by adenosine A2a receptors was examined in slices of rat globus pallidus. The selective adenosine A2a receptor agonist CGS-21680 (3.0-10 nM) significantly increased electrically stimulated release (overflow) of GABA, with 10 nM CGS-21680 resulting in a 44% increase compared with the control. Both the nonselective adenosine receptor antagonist 8-phenyltheophylline (10 microM) and the selective A2a receptor antagonist KF-17837 (100 nM) abolished the CGS-21680-induced increase in GABA overflow. Higher concentrations of CGS-21680 (0.10-1.0 microM) decreased GABA overflow by approximately 25%. 8-Phenyltheophylline (10 microM) antagonized these effects, whereas KF-17837 (100 nM) did not, suggesting actions of CGS-21680 on other adenosine receptors at these concentrations. These results demonstrate that activation of adenosine A2a receptors augments electrically stimulated release of GABA from globus pallidus slices and suggest a mechanism by which adenosine may modulate GABAergic output from the striatopallidal efferent system.

New applications such as CAD, AI, and hypermedia require direct representation and flexible use of complex objects, behavioral knowledge, and multimedia data. To this end, we have devised a knowledge base management system called Jasmine. An object-oriented approach in a programming language also seems promising for use in Jasmine. Jasmine extends the current object-oriented approach and provides the following features. Our object model is based on functional data models and well-established set theory. Attributes or functions composing objects can represent both structural and behavioral knowledge. The object model can represent incomplete and generic knowledge. The model can support the basic storage and operations of multimedia data. The facets of attributes can flexibly represent constraints and triggers. The object manipulation language can support associative access of objects. The structural and behavioral knowledge can be uniformly treated to allow the user to specify complex object operations in a compact manner. The user-defined and system-defined attributes can be uniformly specified to ease user customization of the language. The classes and instances can be uniformly accessed. Incomplete knowledge can be flexibly accessed. The system has a layered architecture. Objects are stored in nested relations provided by extensive DBMS as a sublayer. User query of objects is compiled into relational operations such as select and join, which can be efficiently processed using hashing. The behavioral knowledge is compiled into predicate and manipulation function interfaces that can directly access tuples in a buffer.— Authors' Abstract

A series of 4-hydroxy-3-quinolinecarboxylic acid derivatives (6) and 4-hydroxy-2-oxo-1,2-dihydro-3-quinolinecarboxylic acid derivatives (7) were designed and synthesized as 5-HT3 receptor antagonists. Molecular modeling studies suggested that the 3-carbonyl moiety in 6 was almost coplanar to the plane of an aromatic ring, but in 7 there was a 30 degrees deviation. 4-Hydroxy substitution in quinoline derivatives enhanced affinity for the 5-HT3 receptors, and endo-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-4-hydroxy-3- quinolinecarboxamide (6f) exhibited the most potent activity in the Bezold-Jarisch (B-J) reflex test (ED50 = 0.1 micrograms/kg, iv) among quinoline derivatives 6. Although 4-hydroxy-2-oxo-1,2-dihydro-3-quinolinecarboxamide derivatives (7a) exhibited higher affinity (e.g., 7d: Ki = 0.48 nM) for the 5-HT3 receptors than ondansetron (Ki = 7.6 nM) or granisetron (Ki = 2.1 nM), these amides showed less potent activity in the B-J reflex test than the reference compounds. Interestingly, the ester derivatives 7c, 7f, and 7h eliminated affinity for the 5-HT3 receptors. These unusual structure-activity relationships and the deviation of the 3-carbonyl moiety from the plane of an aromatic ring suggest that the active conformation of 7a might be different from the proposed one for the preceding 5-HT3 antagonists. Thus, 6f was chosen for further studies. No receptor binding for a variety of ligands was significantly antagonized by 6f. Comparing the ratios of the ED50 value in the B-J reflex test (rat, iv) with the LD50 value in acute lethal toxicity (mouse, iv), 6f was proved to have a 600-fold wider margin of safety than ondansetron. Compound 6f dose-dependently attenuated both the incidence and frequency of emetic episodes induced by cisplatin in the dog (ED50 = 14 micrograms/kg, iv) more potently than ondansetron (ED50 = 210 micrograms/kg, iv). Compound 6f (KF-20170) is now under further investigation as a drug for treating gastrointestinal disorder.

Alkylation of 6-thiotheophylline (1) under the aprotic basic condition affords S-alkylated 6-thiotheophylline (3) together with an N7 -alkylated product 4. There is a tendency that the more reactive the alkylating agents are, the higher the yields of S-alkylated products are. On the other hand, treatment of 6-thiotheophylline (1) with epichlorohydrin afforded an unexpected product, 7-(2,3-thioepoxypropyl)theophylline (6), neither an S-alkylated compound 3g nor an N7 -alkylated compound 4g. The chemical structure was determined by nmr spectroscopic analysis.

A 20T large bore superconducting magnet has been developed at the National Research Institute for Metals. In this paper, operation results of this magnet are reported. Cooling down to 1.8K was successfully carried out. Magnetic fields of 15T in a 314mmφ chamber, of 18.06T in a 160mmφ bore and of 20.33T in a 44mmφ bore could be generated. Even after the quenches of two inner coils, they could be re-energized immediately. This fact indicates that this magnet provides an ideal environment for high-field coil experiments. Operation results also proved that saturated superfluid helium can be applied as a coolant for large scale superconducting magnets.

A 20T large bore superconducting magnet has been developed at the National Research Institute for Metals. In this paper, design for its cooling system is mainly discussed. As a coolant for this magnet, saturated superfluid helium has been applied. Two separated chambers where two coils are placed, respectively, are evacuated with rotary pumps. A liquid helium tank is equipped with each chamber over the coils. This tank functions as a reservoir of liquid helium and source of cooling gas for power leads. Two outer coils are designed to be cryogenically stabilized in saturated superfluid helium.

A series of 5-(4-aryl- or 4-arylcarbonylpiperazin-1-yl)-5-deoxy-1,4: 3,6-dianhydro-L-iditol 2-nitrates was prepared in order to obtain orally active, nitrate-type vasodilators with reduced side effects. Our drug design was based on a small reduction in the lipophilicity compared to that of 5-deoxy-5-[4-(3-phenylthiopropyl)piperazin-1-yl]-1,4: 3,6-dianhydro-L-iditol 2-nitrate (1, KF14124). Compounds 4h (aryl = benzimidazol-2-yl), 4i (arylcarbonyl = nicotinoyl), and 4w (arylcarbonyl = 3-furoyl) showed potent anti-ischemic activity in a lysine-vasopressin-induced angina pectoris model (rats), and their structure-activity relationships are discussed. Compound 4i exhibited potent vasodilation of the coronary artery in anesthetized dogs and also exhibited potent preload reduction in a heart failure model (dogs) as compared with isosorbide dinitrate (2), nicorandil (3), and KF14124 (1). Furthermore, 4i showed much weaker acute lethal toxicity and less central nervous system depression than 1 in mice. Thus, 4i (KW-3196) is under development as a vasodilator and a drug for treating angina pectoris.

A convenient synthesis of new heterocycles such as 7,8-dihydro-1H-imidazo[2,1-i]purin-5(4H)-ones (2, n = 0) and 5,6-dihydro-1H-imidazo[2,1-b]purin-9(8H)-ones (3) was described. The syntheses of 2 and 3 were accomplished by treatment of 6-methylthio-7H-purin-2(3-H)-ones 7 or 2-benzylthio-1-methyl-9-triphenylmethyl-9H-purin-6(1H)-one (15) with appropriate aminoalcohol followed by dehydrative cyclization using thionyl chloride. Compound 15 was efficiently prepared by benzylation of 6-hydroxy-2-mercaptopurine (12) followed by tritylation and N-methylation.

A convenient and regioselective synthesis of a new heterocycle, 5-phenyl-1H or 3H-imidazo[4,5-c][1,8]-naphthyridin-4(5H)-one 1-a or 1-b, is described. Methyl 2-anilinonicotinate 15 was transformed into the valuable intermediate, N-phenyl-3-azaisatoic anhydride 4 using trichloromethyl chloroformate (TCF). Treatment of 4 with the anion of ethyl nitroacetate gave 4-hydroxy-3-nitro-1-phenyl-1,8-naphthyridin-4(5H)-one 3. Compound 3 was chlorinated, aminated, reduced, and cyclized to afford 5-phenylimidazo[4,5-c][1,8]naphthyridin-4(5H)-one 1. Regioselective substitution at the 1 or 3-position in the imidazole moiety of 1 was achieved by minor changes of the above scheme.

A new heterocycle, 5-butyl-1-methyl-1 H -imidazo[4,5-c]quinolin-4(5 H )-one has been synthesized using palladium-catalyzed cyclization. A yield of the cyclization was optimized by changing base, additive and reaction temperature.

New tricyclic heterocycles, 9 H - s -triazolo[3,4- i ]purin-5-(6 H )-ones( 2, 3 ), were prepared from 6-methylthio-7 H -purin-2(3 H )-ones ( 5a, 5d )

In synthetic studies of imidazo[4,5- c ]quinolin-4(5 H )-one derivatives, which exhibit a potent antiasthmatic activity, an unusual rearrangement was observed, where the methyl group migrates from the N-1 to the N-3 position on the imidazole during the reaction of Chapman rearrangement of 1-methyl-4-phenoxy-1 H -imidazo[4,5- c ]quinoline 2 .

A convenient synthesis of a new heterocycle, 5,6,7,8-tetrahydropyrido[2,1-b]purin-10-one 1 was described. 4-Amino-N-(5-chloropentanoyl)-5-imidazolecarboxamide 3a was successively cyclized to 1 with polyphosphoric acid at 150 o . Methylation of 1 under basic condition proceeded selectively at N-1 to afford 6 as the sole product