Multipoint gas-liquid phase detection method based on a thin-film optical waveguide.

Gas-liquid phase detection is an important technique applied in a wide range of industries. In this study, we developed a phase detection method using a film-based optical waveguide. The optical waveguide is a thin and flexible film with multi-light paths that uses multi-microsensors for gas-liquid phase detection.

Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton's Tyrosine Kinase.

Although Bruton's tyrosine kinase (BTK) has been recognized as a validated drug target for the treatment of B-cell malignances, the emergence of clinical resistance to the first-generation covalent BTK inhibitors is becoming a serious concern. As a part of our effort to develop noncovalent BTK inhibitors, a series of novel pyrrolopyrimidines was identified as noncovalent inhibitors of both the wild-type and C481S mutant BTKs. Subsequent lead optimization led to the identification of an orally available, potent, and selective BTK inhibitor (AS-1763) as a next-generation noncovalent BTK inhibitor.

Delayed onset of beating and decreased expression of T-type Ca2+ channel in mouse ES cell-derived cardiocytes carrying human chromosome 21.

The mouse ES cell line hcgp7/#21, which carries a human chromosome 21 (hChr.21), was used as an in vitro model to examine the effects of hChr.21 on cardiomyocyte differentiation.

Web-mediated interspecific competition among spider mites.

Some spider mites, such as Tetranychus spp. and Amphitetranychus spp., create complicated webs (CWs), whereas others, such as Panonychus spp.

Subtype switching of T-type Ca 2+ channels from Cav3.2 to Cav3.1 during differentiation of embryonic stem cells to cardiac cell lineage.

Background: The developmental changes of Ni(2+)-sensitivity to automaticity of Nkx2.5-positive cells derived from mouse embryonic stem cell have been identified, suggesting developmental regulation of expressing Ni(2+)-sensitive T-type Ca(2+) channel, although the mechanism of the change has not been fully studied.

Methods And Results: Transcripts of Cav3.

State-dependent blocking actions of azimilide dihydrochlo-ride (NE-10064) on human cardiac Na(+) channels.

Background: Azimilide reportedly blocks Na(+) channels, although its mechanism remains unclear.

Methods And Results: The kinetic properties of the azimilide block of the wild-type human Na(+) channels (WT: hH1) and mutant DeltaKPQ Na(+) channels (DeltaKPQ) expressed in COS7 cells were investigated using the whole-cell patch clamp technique and a Markovian state model. Azimilide induced tonic block of WT currents by shifting the h infinity curve in the hyperpolarizing direction and caused phasic block of WT currents with intermediate recovery time constant.

Bone-anabolic effect of salmon calcitonin on glucocorticoid-induced osteopenia in rats.

The anabolic effect of salmon calcitonin (SCT) on skeletal tissue was examined on glucocorticoid-induced osteopenia in female rats (12 weeks old). By the administration of methylprednisolone acetate (MPA: 0.1 mg/kg, s.

Bone anabolic effects of PTH(1-34) and salmon calcitonin in ovariectomy- and ovariectomy-steroid-induced osteopenic rats: a histomorphometric and biomechanical study.

Using an experimental model of type 1 osteoporosis under the chronic therapy with an anti-inflammatory steroid, the bone anabolic effect of PTH(1-34) was evaluated by histomorphometrical and biomechanical analysis. Wistar female rats (12-week-old) were ovariectomized and allowed to develop an osteopenic model in the presence or absence of methylprednisolone acetate (MPA: 0.1 mg/kg, s.

Identification of tranilast-binding protein as 36-kDa microfibril-associated glycoprotein by drug affinity chromatography, and its localization in human skin.

To elucidate the molecular mechanism involved in the suppression of keloids and hypertrophic scars by tranilast, we investigated the target protein of tranilast in bovine skin and aorta. A specific tranilast-binding protein was isolated from both tissues by drug affinity chromatography and was identified as 36-kDa microfibril-associated glycoprotein (36-kDa MAGP). Binding of 36-kDa MAGP to tranilast seemed to be specific since 36-kDa MAGP could be eluted from the drug affinity column by tranilast itself and also binding of 36-kDa MAGP to other anti-allergy drugs (amlexanox and cromolyn) is significantly weaker than that to tranilast.

Ultrastructural distribution of 36-kD microfibril-associated glycoprotein (MAGP-36) in human and bovine tissues.

We observed the ultrastructural distribution of MAGP-36 by immunoelectron microscopy in human and bovine tissues. MAGP-36 was present in microfibrils associated with tropoelastin in skin, aorta, and spleen. It was not detected in microfibrils from the ocular zonule and kidney mesangium that were not associated with tropoelastin.

Three distinct anti-allergic drugs, amlexanox, cromolyn and tranilast, bind to S100A12 and S100A13 of the S100 protein family.

To investigate the roles of calcium-binding proteins in degranulation, we used three anti-allergic drugs, amlexanox, cromolyn and tranilast, which inhibit IgE-mediated degranulation of mast cells, as molecular probes in affinity chromatography. All of these drugs, which have different structures but similar function, scarcely bound to calmodulin in bovine lung extract, but bound to the same kinds of calcium-binding proteins, such as the 10-kDa proteins isolated in this study, calcyphosine and annexins I-V. The 10-kDa proteins obtained on three drug-coupled resins and on phenyl-Sepharose were analysed by reversed-phase HPLC.

[Effect of liver hydrolysate on ethanol- and acetaldehyde-induced deficiencies].

Since it has been reported that amino acids have alleviating effects on ethanol- and acetaldehyde-induced toxicity, we investigated the effect of liver hydrolysate derived from bovine liver on ethanol- or acetaldehyde-induced toxicity and deficiency models of mice and rats in the present study. Liver hydrolysate improved the deficiencies of beam walking and food intake of mice in a dose-dependent fashion when challenged with ethanol at the dose of 5 ml/kg, p.o.

Two cases of Merkel cell carcinoma cured by intratumor injection of natural human tumor necrosis factor.

Two patients were treated with intratumor injection of natural human tumor necrosis factor for recurrent or primary Merkel cell carcinoma. In both patients, local chemotherapy achieved complete tumor regression without causing ulceration or scarring. These results suggest that intratumor injection of natural human tumor necrosis factor may be very effective for the treatment of Merkel cell carcinoma.

Treatment of nevus Ota: combined skin abrasion and carbon dioxide snow method.

Thirty-seven patients with nevus Ota were treated by skin abrasion-carbon dioxide snow therapy. Data obtained from 24 patients (including 5 infants) who completed treatment were analyzed to determine the number of treatment courses and to assess the outcome by color and histologic type. The 5 infants completing treatment received a mean of 10 courses of carbon dioxide snow therapy.

The effect of Beraprost sodium on the survival of subcutaneous transferred jejunum after vascular pedicle interruption in a rat model.

Beraprost sodium, a stable PGI2 analog, having antiplatelet aggregation and vasodilating actions, was tested in a rat subcutaneous heterotopic jejunal model for its ability to improve survival after vascular pedicle interruption. Forth Sprague-Dawley rats were divided into four groups: Group 1 (control, ligation of pedicle on postoperative day 5); Group 2 (Beraprost sodium, ligation on day 5); Group 3 (control, ligation on day 7); and Group 4 (Beraprost sodium, ligation on day 7). The resulting viability rates were: Group 1 = 0 percent, Group 2 = 40 percent, Group 3 = 30 percent, Group 4 = 90 percent.

Pectoralis major myocutaneous flaps in rats.

A new neurovascular, island, myocutaneous flap, including the pectoralis major, was created in a rat model. This model is useful for the observation of muscle degeneration and skin changes due to ischemia or denervation. Although this model requires a delay procedure, it allows the flap, that can be used as a free myocutaneous flap, to be raised reliably.

[Effect of efonidipine hydrochloride, a calcium channel blocker, on the experimental cerebral ischemia/anoxia].

The anti-ischemic and anti-anoxic effects of efonidipine, a dihydropyridine calcium antagonist, were studied in several models for cerebral ischemia and anoxia in mice and rats, and the effects were compared with those of nicardipine and flunarizine. Both efonidipine and flunarizine showed protective effects in the models of KCN-induced anoxia and complete ischemia induced by decapitation in mice 6 hr after the treatment, while nicardipine did not show such a long-lasting effect. Efonidipine (1 mg/kg, i.

Effects of citalopram, a synthetic serotonin uptake inhibitor, on indoleamine and catecholamine concentrations in the cerebrospinal fluid of freely moving rats.

We studied changes in the concentrations of 5-hydroxytryptamine (5-HT), other indoleamines, and catecholamines in the cerebrospinal fluid (CSF) of freely-moving rats that had been administered citalopram, +/-1-[3- (Dimethylamino)propyl)-1-(4-fluorophenyl)-1, 3-dihydro-5-isobenzo-furancarbonitrile hydrobromide), a selective inhibitor of 5-HT uptake. In a microdialysis experiment, the intracerebral extracellular free 5-HT increased significantly, peaking 60 to 90 min after citalopram (30 mg/kg p.o.

Comparative study of auricular dimensions for the normal auricles of microtia patients, their parents, and normal individuals.

We measured the dimensions of the normal auricle in microtia patients and those of both auricles in their parents, and compared the findings with data obtained in normal individuals. The physiognomical auricular length and width dimensions of the normal auricles in microtia patients were significantly smaller than those in normal individuals. The auricular length of the parents of microtia patients was also significantly smaller than in normal individuals.

[Effects of NC-1100, a calcium channel blocker, on experimental cerebral ischemia/anoxia in rodents].

The anti-ischemic and anoxic effects of NC-1100, a piperazine type calcium channel blocker, were investigated in various cerebral ischemia and anoxia models in mice, gerbils and guinea pigs. Minimal effective doses of NC-1100 were 8 mg/kg, i.p.

Experimental study of subcutaneously transferred intestine: effect of the presence of serous membrane on acceptance rate.

The serous membrane is considered suspect as one of the obstacles responsible for delaying the acceptance of free jejunal grafts. A model was created of subcutaneous transfer of jejunum from which the serous membrane had been experimentally removed and the authors compared acceptance rates for intestine with and without a serous membrane. Results showed acceptance rates of 0 percent, 37.

An experimental study of ischemia following subcutaneous heterotopic intestinal graft: influence of arterial or venous occlusion.

A subcutaneously transferred intestinal model was prepared in the rat and experimental observations were conducted of serial histologic changes in the intestine and of acceptance rates, when the artery or vein in the pedicle was ligated at various times after transfer. Results showed 50 percent take in the artery-ligated group and 12.5 percent in the vein-ligated group, when performed 5 days after transfer; 87.

Interleukin 1-induced sequential myelorestoration: dynamic relation between granulopoiesis and progenitor cell recovery in myelosuppressed mice.

The myelorestorative effect of recombinant human interleukin 1 alpha (IL-1 alpha) was studied in mice treated with anticancer drugs. The treatment of mice with 5-fluorouracil (5-FU; 250 mg/kg body weight) or cyclophosphamide (CPA; 100 mg/kg) considerably decreased bone marrow or splenic colony-forming units in culture (CFU-C) or neutrophils in blood. The daily administration of IL-1 alpha (100 ng/mouse/day) after 5-FU treatment markedly accelerated the recovery of bone marrow CFU-C.