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Biomedical subjects

H Hatakeyama

Publications and source records attributed to H Hatakeyama.

At least 73 records · Page 4Linked to original sources
PubMed1989

[Evaluation of endoscopic local injection of hypertonic saline- epinephrine solution and surgical treatment on hemorrhagic gastroduodenal ulcer].

For the purpose of arresting hemorrhage from gastric and duodenal ulcer we developed a method of endoscopic local injection of hypertonic saline-epinephrine solution (HSE), consisting of 625mEq/L or 1,250mEq/L sodium chloride with 0.05mg/ml epinephrine. During the period between October 1978 and March 1988, a total 246 patients with peptic ulcers underwent treatment for hemostasis by this method. According to our criteria for the assessment of the hemostatic effect, 231(93.9%) of 246 cases achieved permanent hemostasis, 7(2.8%) achieved temporary hemostasis, and no effect was noted 8 cases (3.3%). From June 1975 to March 1988, a total 366 cases with gastric and duodenal ulcers were operated on at our hospital. By applying endoscopic local injection of HSE, the rate of emergency operation for patients with bleeding peptic ulcers was significantly reduced from 13.4%(22/164) to 1.5%(3/202). From these results, we consider that endoscopic local injection of HSE is valuable for hemorrhage from gastric and duodenal ulcer.

Administration, Topical↗
PubMed1988

[Effect of the nonsteroidal anti-inflammatory drug 480156-S on hepatic drug-metabolizing activity and pharmacological action of diazepam and pentobarbital in rats].

Effect of the nonsteroidal anti-inflammatory drug 480156-S on liver drug-metabolizing activity was studied in rats, and its effect was compared with that of cimetidine. Cytochrome P-450-dependent 7-alkoxycoumarin O-dealkylase activity was not affected by a single administration of 480156-S, but the activity, especially the O-demethylase but not the O-depropylase, was suppressed dose-dependently by multiple administrations. Pretreatment of rats with phenobarbital caused a diminution of the inhibitory action of 480156-S. Treatment of rats with cimetidine resulted in a marked decrease in the activity, although it recovered 24 hr later. After the pretreatment of animals with 480156-S or reference drugs, the pharmacological action of diazepam was determined using muscle relaxation and inhibitions of electroshock-induced convulsion and pentetrazole-induced clonic convulsion as the indicators. Prolonged pharmacological activity of diazepam was observed when liver drug-metabolizing activity was lowered by the pretreatment. On the other hand, pentobarbital-induced anesthesia was prolonged by the pretreatment of rats with cimetidine, but the anesthesia was not modified by the administration of 480156-S. These results suggest the inhibitory action of 480156-S on a specific form(s) of P-450 isozyme.

7-Alkoxycoumarin O-Dealkylase↗
PubMed1988

[Endoscopic resection with local injection of hypertonic saline epinephrine for the treatment of early gastric cancer].

We have developed a new method of endoscopic resection of early gastric carcinomas and other tumors. Characteristics of the new method are summarized as follows. 1. In order to prevent bleeding after endoscopic resection of the tumors, local injection of hypertonic saline epine phrine (HSE) solution was applied to the lesion. Even a depressed lesion like II c type early gastric carcinoma was artificially protruded by local injection of HSE solution. 2. Instead of a single fiberscope, double fiberscopes were employed simultaneously for endoscopic resection of the lesion. 3. Prior to resection of the lesion by high frequency current snare method, incision of the mucosa along the marking line around the lesion performed, enabling the area to be resected precisely. 4. Because tissue damage is mild, resected materials removed are suitable for pathological study. Endoscopic resection was performed on a total of 113 cases in early gastric carcinomas; 103 cases among them (91.2%) were curative resections. Ten cases of the rest underwent surgical gastrectomy for the endoscopic non-curative resections. Rate of five-year survival in 103 cases was 85.2%. Endoscopic resection by our method seems to be effective for the treatment of early gastric carcinomas in any lymph node metastasis and in patients at high surgical risk.

Epinephrine↗
PubMed1984

Detection and determination of active metabolites of 1-(2-o-chlorobenzoyl-4-chlorophenyl)-5-glycyl-aminomethyl-3-dimethy l-carbamoyl-1H-1,2,4-triazole hydrochloride dihydrate, (450191-S), in rat tissues, using a radioreceptor assay for benzodiazepines.

1-(2-o-Chlorobenzoyl-4-chlorophenyl)-5-glycyl-aminomethyl-3- dimethylcarbamoyl -1H-1,2,4-triazole hydrochloride dihydrate, (450191-S), exhibits pronounced central nervous system (CNS) activities similar to those of benzodiazepines, but it has only low affinity for benzodiazepine receptors. However, when 450191-S was administered to rats at a dose of 10 mg/kg, brain extracts markedly inhibited [3H]diazepam binding to the receptors. Thin-layer chromatography (TLC), high performance liquid chromatography (HPLC), and radioreceptor assay (RRA) were used to isolate three metabolites that could inhibit [3H]diazepam binding prominently. These were identified by gas chromatography-mass spectrometry (GC/MS) as compounds having the triazolo-benzodiazepine skeleton. They showed high affinities for benzodiazepine receptors (Ki = 0.9 to 2.1 nM) and exerted potent pharmacological effects similar to those of 450191-S. In addition, their levels in the brain were sufficient to explain the pharmacological activity of 450191-S, which could not be detected in tissue extracts 15 min after administration. These results indicate that the pharmacological activity of 450191-S is largely due to the action of active metabolites, although some points remain to be elucidated to fully account for the large attenuation of the side effect (ataxia) compared with the major effects (anti-convulsant and hypnotic). We also determined the brain levels of metabolites following the administration of 450191-S and evaluated the extent to which each active metabolite contributes to the pharmacological activities of this drug.

Animals↗
PubMed1984

Pharmacological properties of 2-[4-(2-thiazolyloxy)-phenyl]-propionic acid (480156-S), a new non-steroidal antiinflammatory agent.

In terms of antiinflammatory activity in acute and chronic animal models, 2-[4-(2-thiazolyloxy)-phenyl]-propionic acid (480156-S) was more active than ibuprofen but inferior to indomethacin. The analgesic activities of 480156-S measured by the writhing method and the Randall & Selitto method were comparable or superior to those of indomethacin, diclofenac-Na and ketoprofen. 480156-S also had strong antagonistic action against bradykinin, markedly inhibiting all bradykinin-induced edema and pain reactions (tail licking in mice and flexor reflex of rabbit hind limb). On scald-induced pain in which bradykinin is greatly involved, 480156-S had an obviously stronger analgesic effect than any of the reference drugs. As for its effects on prostaglandin (PG), 480156-S weakly inhibited arachidonic acid-induced edema and pain reactions but also inhibited PGE2 synthesis of bovine vesicular gland microsomes.

Animals↗
PubMed1980

Peptidoaminobenzophenones, a novel class of ring-opened derivatives of 1,4-benzoidazepines.

A series of noval peptidoaminobenzophenones has been prepared via several routes and was evaluated for CNS activity. The structure--activity relationships in the series are discussed. In general, dipeptido-N-methylaminobenzophenones showed higher activities than the corresponding NH derivatives. Some compounds had very high activities in antipentylenetetrazole and antifighting tests in mice when orally administered. Very weak toxicity was also found in these compounds. Water solubility of the peptidoaminobenzophenones and their salts were tested. Possible in these compounds. Water solubility of the peptidoaminobenzophenones and their salts were tested. Possible in vivo conversion of peptidoaminobenzophenone by enzymatic cleavage of the terminal amino acid, followed by chemical cyclization to 1,4-benzodiazepine, is also discussed. Such novel open-ring derivatives of 1,4-benzodiazepine may serve as useful CNS agents.

Aggression↗
PubMed1979

The pharmacology of 20681-S and 20682-S, 6-oxo-N-cyclopropylmethylmorphinans, as narcotic antagonist analgesics.

It has been demonstrated that L-3hydroxy-6-oxo-N-cyclopropylmethylmorphinan methansulfonate (20681-S) and L-3,14-dihydroxy-6-oxo-N-cyclopropylmethylmorphinan methansulfonate (20682-S), have antinociceptive and narcotic antagonistic properties. In the rodent antinociceptive test, the action of 20681-S was more potent and of longer duration than that of morphine and of cyclazocine after subcutaneous or oral administration. The antinociceptive effect of 20682-S ranked between that of morphine and that of pentazocine in the mouse acetic acid-writhing test. Both compounds possessed potent narcotic antagonistic activities, 20682-S being more active than naloxone and oxilorphan and 20681-S being equipotent with cyclazocine. The latent side effects (respiratory depression and fall in blood pressure) and the acute toxicity of 20681-S and 20682-S, were less than those of reference narcotic antagonists or of narcotic antagonist analgesics.

Analgesics↗
PubMed1978

Development of inactivated vaccine for Akabane disease.

Virus inactivated by formalin or beta-propiolactone was superior to that inactivated by ether and heating in immunogenicity to mice. There were no significant differences in the antibody response of mice among such adjuvants as aluminum phosphate gel, aluminum hydroxide gel, and sodium arginate gel. When cattle were immunized with vaccine inactivated by formalin and adsorbed to aluminum phosphate gel, an excellent effect was obtained by injection with two doses of 3 ml each given at a 4-week interval. It was also suggested that mice and guinea pigs might be available for the potency test of vaccine. When calves and pregnant goats were injected with vaccine in the same manner as mentioned above, they were prevented from viremia and fetal infection caused by challenge virus. Even when stored at 4 degrees C for 12 months, vaccine was found to retain its stabilized immunogenicity. When pregnant cows were injected with vaccine in the field, the positive rate of neutralizing antibody was 88.5% in the 2 months after the first injection. When other pregnant cows were injected twice with vaccine, this rate was 34.6, 100, 65.4, and 45.8% in the 1, 2, 6, and 10 months, respectively, after the first injection. In another experiment, the antibody levels attained declined rather rapidly in several months. A single dose of vaccine given one year later provoked a rapid antibody response. The vaccination caused no clinical symptoms, abnormal birth, or decrease in milk yield in these cows.

Animals↗
PubMed1976

Resolution and complementation of the labile L-leucine-pyruvate transaminase. An intermediate during enzyme formation under nitrogen starvation in Gluconobacter suboxydans.

L-Leucine-pyruvate transaminase (mol. wt. 70 000) in Gluconobactersuboxydans synthesized during nitrogen starvation contained a labile form which changed to the stable one later. The labile enzyme (mol. wt. 70 000) dissocated to the two proteinaceous components: a cationic one (mol. wt. 10 000--20 000) and an anionic one (mol. wt. 50 000--60 000), during column chromatography on DEAE-cellulose. The enzyme activity was reconstructed when they were mixed. The reconstructed enzyme had almost the same molecular size and enzymatic properties as the labile and the native stable enzymes.

Drug Stability↗
PubMed1976

Relation of certain infrared bands to conformational changes of cellulose and cellulose oligosaccharides.

The i.r. spectra of D-glucose and cellulose oligosaccharides up to cellopentaose have been compared with those of cellulose at various temperatures between that of liguid nitrogen and approximately 250 degrees. Significant changes in frequency and intensity of the bands at approximately 3400 cm -1 were observed. The a 1372 cm -1/a2900 cm -1 ratio for each carbohydrate studied decreased gradually as the temperature was increased above ambient. The change of the band intensities at 1429 and 893 cm -1 with temperature was also investigated. The observed spectral changes are assumed to be associated with changes of hydrogen bonding.

Cellulose↗
PubMed1976

Studies on the isothermal crystallization of D-glucose and cellulose oligosaccharides by differential scanning calorimetry.

Isothermal crystallization from the glassy state of D-glucose and cellulose oligosaccharides (e.g., cellobiose, cellotriose, and cellotetraose) has been studied by differential scanning calorimetry. The crystallization of amorphous D-glucose and oligosaccharides was very difficult in the absence of traces of water. Amorphous cellobiose and cellotetraose crystallized far more rapidly than amorphous D-glucose and cellotriose. The activation energy for the crystallization of cellobiose and cellotetraose was approximately 10-12 kJ. mol(-1), while that for D-glucose and cellotriose was approximately 1-2 kJ. mol(-1). An odd-even effect seemed to be associated with the crystallization process of these saccharides.

Calorimetry↗