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Biomedical subjects

M Nakano

Publications and source records attributed to M Nakano.

At least 811 records · Page 45Linked to original sources

Pharmacological activities of synthetic human cholecystokinin-33 of which tyrosine was sulfated by arylsulfotransferase.

The pharmacological activities of synthetic human CCK-33, in which a tyrosine molecule was sulfated by arylsulfotransferase, were investigated in the rat and the guinea-pig. The activities were compared with those of non-sulfated CCK-33 (CCK-33NS), CCK-8 and CCK-4. CCK-33 was about 100 fold more potent than non-sulfated CCK-33(CCK-33NS) but was about 20 fold less potent than CCK-8 in the contraction of the isolated gallbladder of the guinea-pig. In rat pancreatic secretion, intravenous CCK-33 and CCK-8 showed almost the same activity. The potency of each was about 1000 fold more than the individual potency of CCK-33NS, non-sulfated CCK-8 (CCK-8NS) and CCK4. There were no significant differences in gastric acid stimulatory activities among CCK-33, CCK-8, CCK-4, but the activities of CCK-33NS and CCK-8NS were less than those of CCK-33 and CCK-8, respectively. CCK-33 and CCK-8 produced a reduction in the intake of powder chow in doses of 10(-8) and 3 x 10(-8) mol/kg i.p., but CCK-33NS, CCK-8NS and CCK-4 did not. In conclusion, the activities of synthetic human CCK-33 are almost the same as those of CCK-8 on exocrine pancreatic secretion, gastric acid secretion and food intake, but less than CCK-8 on isolated gallbladder contraction.

Animals↗

Comparison of transport of procainamide and N-acetylprocainamide from blood into the intestinal lumen with that into the peritoneal cavity in rats.

Transfer of procainamide and its active metabolite, N-acetylprocainamide (NAPA) from the blood into the intestinal lumen was compared with that into the peritoneal cavity after i.v. administration of procainamide at the dose of 10 mg/kg to rats. The amounts of both drugs transferred from the blood into the intestinal lumen were much greater than those into the peritoneal cavity. The average amounts of procainamide transferred in 2 h into the intestinal lumen and the peritoneal cavity were 12.7% and 1.7% of dose (10 mg/kg), respectively, while those of NAPA were 3.5% and 1.4% of dose. The intestinal and peritoneal clearance values of procainamide were 143.5 and 59.4 ml/h, respectively, and those of NAPA were 32.6 and 13.5 ml/h. The difference in transfer rates across the intestinal and peritoneal membranes may be due to difference in the area of permeative surface and the extent of ionization in the dialysate. Consequently, it is expected that the gastrointestinal dialysis by oral administration of activated charcoal may serve as one of the more useful hemopurification methods than the peritoneal dialysis in procainamide and NAPA intoxication.

Acecainide↗

Release characteristics of a free polyunsaturated fatty acid from an oily lymphographic agent.

The release profiles of a free polyunsaturated fatty acid, alpha-linolenic acid, from solutions in an oily lymphographic agent Lipiodol-Ultra-Fluid (Lipiodol), to rabbit and human plasma, phosphate buffer solution (PBS), and PBS containing bovine serum albumin (BSA) were examined in vitro. The times required for 50% release of alpha-linolenic acid from Lipiodol were about 1 and 1.5 h in the rabbit and human plasma, respectively. Although only a slight amount of alpha-linolenic acid was released from Lipiodol to PBS after 24 h incubation at 37 degrees C, release was markedly enhanced by the addition of BSA to PBS. The amount of alpha-linolenic acid released from Lipiodol into PBS containing 5% BSA increased as the alpha-linolenic acid content in Lipiodol was increased. In all experiments, the release had stopped before all alpha-linolenic acid had been released. The prolongation of alpha-linolenic acid release from Lipiodol is considered a requisite for a selective anticancer effect of Lipiodol containing a free fatty acid on liver cancer.

Animals↗

Pharmacokinetics of theophylline and phenobarbital during peritoneal dialysis compared with intestinal dialysis in rats.

The transfer rates of theophylline and phenobarbital from blood into the peritoneal cavity were investigated after their intravenous administrations at a dose of 10 mg/kg each in rats. Appreciable amounts of both drugs were transported into the dialysate with their transfer rates decreasing as the serum concentrations declined. The average amount of theophylline transferred into the dialysate was 17% and 24% of dose in 2 and 4 h, respectively, while that of phenobarbital was 13% and 45% of dose in 2 and 8 h, respectively. The amounts appeared to be greater than those transported into the intestinal lumen which was previously reported by the authors. Peritoneal dialysis decreased the serum half-life and the area under the serum concentration-time curve (AUC) value of theophylline from 2.1 to 1.5 h and from 38 to 26 micrograms.h/ml, respectively and increased the total body clearance by 47% as compared with the control. The dialysis also decreased the serum half-life and the AUC value of phenobarbital from 8.3 to 5.3 h and from 116 to 83 micrograms.h/ml, respectively and increased the total body clearance by 112% as compared with the control. Overall, the effectiveness of peritoneal dialysis in removing theophylline and phenobarbital appears to be not very different from that of intestinal dialysis with oral activated charcoal which has been previously reported by the authors in spite of the difference in transport into the intestinal lumen and peritoneum.

Animals↗

Croconazole metabolism in rats.

1. Following subcutaneous administration of 1-(2-(3-chlorobenzyloxy)phenyl)vinyl)-1H-imidazole (croconazole) to rats, four metabolites were identified by comparison of their mass and n.m.r. spectra, g.l.c., and t.l.c. with those of synthetic compounds and enzyme hydrolysis. These compounds are o-hydroxyacetophenone sulphate (M1S), 1-(1-(2-hydroxyphenacyl)vinyl)-1H-imidazole sulphate (M12S), 2-(3-chlorobenzyloxy)phenacyl alcohol (M2), and 2-(3-chlorobenzyloxy)benzoic acid (M9-1). 2. At 10 mg/kg dosing of croconazole the elimination rate of the unchanged drug from plasma was faster in male than in female rats. 3. The percentage of excretion of M12S in 24 h urine was 17% for males and 7.5% for females, and that of M1S was 6.6% for males and 6.5% for females. The percentage of excretion of M2 in 24 h bile was 14% for males and 22% for females, and that of M9-1 was 3.7% for males and 1.6% for females.

Animals↗

[The basic study of autologous peripheral stem cell transplantation--useful application of KLI and G-CSF].

There has been increasing interest in autologous peripheral stem cell transplantation (APSCT) in the treatment of malignant disease because it is a convenient method and may have a lower risk of tumor cell contamination than autologous bone marrow transplantation (ABMT). Recently, it is reported that the number of peripheral blood stem cells increase during recovery phase of hemopoiesis after chemotherapy, and further increase is reported on the case of treatment with G-CSF. But influences of G-CSF to the residual malignant cells is still unknown. In this report, we have used clonal cell culture and kappa-lambda imaging (KLI) analysis to trace the level of CFU-GM, BFU-E, and malignant B-cell population (mBp) in peripheral blood before and after treatment with rhG-CSF. The peak level of CFU-GM in peripheral blood was a 2-fold increased when rhG-CSF was administered, and this peak appeared 5-7 days earlier than that in the case without rhG-CSF. MBp was detected in bone marrow, however, no mBp was detected before and after treatment with rhG-CSF in peripheral blood. These findings suggest that APSCT is acceptable for this patient in case of minimal bone marrow involvement. And KLI analysis might be an effective method for detecting residual malignant cells in bone marrow and peripheral blood.

Adult↗

Improvement of biliary enzyme levels and itching as a result of long-term administration of ursodeoxycholic acid in primary biliary cirrhosis.

Ursodeoxycholic acid (UDCA) was administered to 10 patients diagnosed as having primary biliary cirrhosis (PBC) after liver biopsy. Eight patients were anicteric, and two were icteric cases. One patient was in stage I, seven were in stage II, one in stage I-III, and one in stage III-IV of Scheuer's classification. Six hundred milligrams of UDCA were administered orally after meals three times daily to all of the patients for more than 1 yr. The period of UDCA administration ranged from 6 to 41 months. The major findings are as follows: 1) in six out of seven patients with pruritus, itching disappeared 1 month after administration of UDCA; 2) both serum alkaline phosphatase and gamma-glutamyltranspeptidase levels began decreasing significantly the first month after the onset of UDCA treatment, and continued decreasing throughout the treatment; 3) GOT and GPT levels also decreased significantly during the administration of UDCA, compared with before-treatment levels; 4) in one icteric patient with portal hypertension, although serum biliary enzyme levels improved after treatment, serum bilirubin level got worse, and the patient died of esophageal variceal hemorrhage. In another icteric case, biliary and bilirubin levels improved slightly after treatment; 5) antimitochondrial antibody titer decreased in four cases, but IgM levels and other immunological parameters were not changed; 6) serum UDCA increased significantly during UDCA treatment; in particular, glyco-UDCA occupied up to 40% of the total bile acid and CDC decreased to 25%; 7) portal inflammation activity decreased in all five patients who had undergone follow-up liver biopsy, more than 1 yr after UDCA administration--bridging fibrosis decreased in three cases; and 8) no side effects were observed in any of the cases. Although large-scale, randomized, controlled, double-blind tests are necessary, it is speculated that the long-term administration of UDCA is a safe and effective treatment for the improvement of biliary enzyme levels and pruritus in anicteric PBC.

Adult↗

Inhibitory effects of azelastine on superoxide anion generation from activated inflammatory cells measured by a simple chemiluminescence method.

Blood was drawn from healthy human volunteers and neutrophils and eosinophils were purified on a Conray-Ficoll and a Percoll gradient, respectively. Rat mast cells were also purified on a Percoll gradient. Superoxide anion (O2-) generation from the cells were measured by 2-methyl-6-[p-methoxy-phenyl]-3,7-dihydroimidazo[1,2-a]pyrazin+ ++-3-one (MCLA)-dependent luminescence. Addition of 0.5 mumol/l MCLA and a stimulatory agent, such as phorbol myristate acetate, N-formyl-methionyl-leucyl-phenylalanine (fMLP) and compound 48/80, to a suspension of each cell caused a marked luminescence which was inhibited by 0.5 mumol/l superoxide dismutase (SOD). Azelastine (A-5610) significantly inhibited the O2- generation from each activated inflammatory cell in a dose-dependent manner. When eosinophils were activated by fMLP in the presence of cytochalasine (CB), azelastine abolished the luminescence stronger than that from the fMLP-stimulated cells in the absence of CB.

Animals↗

[Correlation of cerebro-cardiovascular findings to mortality of middle-aged and elderly in a population from a fishing village in Shizuoka Prefecture].

Six hundred and eighteen men and 993 women ranging in age from 30-69, living in Kamo Village, Shizuoka Prefecture, underwent baseline health examinations in 1964-1966. During the follow-up period of 20-years, 175 men and 170 women died. The most frequent cause of death was malignant neoplasms (57 men and 45 women), followed by stroke (47 men and 44 women) and heart disease (29 men and 37 women). The relationship of 22 cerebro-cardiovascular disease variables investigated in the baseline examination to stroke and heart disease mortalities, and, in addition, to cancer and all-cause mortalities were analyzed using Cox's proportional hazard model. In univariate analysis controlled for age and sex, systolic and diastolic blood pressures, albuminuria, hypertensive and sclerotic changes in fundus oculi, body mass index, atrial fibrillation, and use of antihypertensive drugs had significant positive relationships to stroke mortality. As for heart disease mortality, albuminuria, glucosuria, high R wave, and ST and/or T changes in ECG were positively and significantly related. Only Q.QS in ECG significantly correlated with cancer mortality. Variables showing significant relationship to all-cause mortality were systolic and diastolic blood pressures, albuminuria, glucosuria, hypertensive changes in fundus oculi, Q.QS, high R wave, ST and/or T changes, atrial fibrillation, use of antihypertensive drugs, and history of stroke. In multivariate analysis (step-wise) of all examination variables including age and sex, stroke mortality was significantly related to age, atrial fibrillation, use of antihypertensive drugs, and hypertensive changes in fundus oculi. Age, albuminuira, and ST changes in ECG were significantly related to heart disease mortality. Age, sex, and Q.QS in ECG were significantly related to cancer mortality. The relationship of age, sex, albuminuria, Q.QS, and ST changes in ECG to all-cause mortality was significant.

Adult↗

[Prediction of length and width of upper central incisor tooth in multivariate face information].

The possibility of accurately estimating a tooth crown length and width from measured distance of various face points was examined by using Multiple Correlation Analysis. The multiple correlation coefficient between a tooth crown length and the face point was 0.3137 and the residual standard error was 0.820; that between a tooth crown width and the face point was 0.3917 and its standard error was 0.467, obtained by substituted sample data for multiple regression equation.

Analysis of Variance↗

[Observation of occlusal force in prosthetic crown cementings].

The method of pressure force in crown cementing was examined. Continuous occlusal force was always supported by the patients' personal occlusal force in cementing crowns. We found that continuous occlusal force continuously decreased as the occlusal force increased, and the decreasing morphologies were classified into four types, 'Rapid decrease', 'Step-wise decrease', 'Intermediate decrease' and 'Gradual decrease'.

Bite Force↗

Erythrocyte superoxide dismutase in various hematological diseases.

We measured superoxide scavenging activity (SSA) of erythrocytes with the recently developed chemiluminescence method by Nakano et al in Down syndrome and various hematological diseases. Hematological disorders were aplastic anemia, myelodysplastic syndrome, multiple myeloma, malignant lymphoma and chronic myelogenous leukemia. The SSA of erythrocytes was 1.7 times higher in Down syndrome, which was consistent with values reported in the previous publications. The erythrocyte SSA in patients of multiple myeloma treated with interferon-alpha was higher than that in healthy volunteers. The erythrocyte SSA in myelodysplastic syndrome, malignant lymphoma and chronic myelogenous leukemia did not differ from that in healthy volunteers. The mean value of erythrocyte SSA in aplastic anemia also remained within normal range. However, when an individual's hemoglobin concentration was compared with his or her own erythrocyte SSA, there was a clear correlation between them. Namely erythrocyte SSA increased when anemia was severe. There was no correlation between erythrocyte SOD activity and ageing.

Down Syndrome↗

[Dermal patch anesthesia to prevent pain from dermal puncture--10% lidocaine aqueous gel with 3% glycyrrhetinic acid 3-0 hemiphthalate disodium].

The clinical efficacies of 10% lidocaine aqueous gel with and without 3% glycyrrhetinic acid 3-0 hemiphthalate disodium (GAHPh) applied as a skin patch for reduction of pain from venous cannulation were evaluated in a double blind study. Twenty-four adult patients, who were scheduled for surgery under general anesthesia, gave informed consent to participate in this study. The patients were allocated randomly into two groups: one for a dermal patch GAHPh (GAHPh group) and the other for a dermal patch without GAHPh (plain group). Approximately 0.3g of either gel with or without GAHPh, soaked in a round sponge (25mm in diameter, 1mm in thickness), was applied over the selected vein on the arm and was covered with an adhesive plastic film (Tegaderm). Pain score was graded by the number of painful spots out of the 5 tests in the treated skin area. In patients with a pain score under 1, venous cannulation was carried out without an intradermal injection of a local anesthetic and pain associated with the cannulation procedure was graded by patients on a scale of 5, where 0 = no pain, 1 = little pain, 2 = moderate pain, 3 = painful, 4 = very painful. The mean application time periods were 59.3 min for the GAHPh group and 60.3 min for the plain group. Transient local redness was observed in 8 patients after removal of the gels; 3 in the GAHPh group and 5 in the plain group. The mean pain score (1.3 +/- 1.5) in the GAHPh group, was significantly lower than that (2.5 +/- 1.7) in the plain group (P less than 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Cutaneous↗