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Biomedical subjects

H Satoh

Publications and source records attributed to H Satoh.

At least 919 records · Page 51Linked to original sources
PubMed1982

The central anti-serotonin activity of zotepine, a new neuroleptic, in rats.

2-Chloro-11-(2-dimethyl-aminoethoxy) dibenzo [b, f] thiepin (zotepine) is a new neuroleptic drug which is structurally different from known neuroleptics. Zotepine, chlorpromazine, propericiazine, and cyproheptadine inhibited hyperthermia induced by dosing with fenfluramine in rats in a warm environment (26-28 degrees C). Fenfluramine is known to induce hyperthermia by mediation of central serotonin. Zotepine had a 10 times or greater potency than chlorpromazine, propericiazine and cyproheptadine in inhibiting the hyperthermia. Thioridazine did not inhibit the hyperthermia, whereas haloperidol accelerated the hyperthermia. Zotepine was also the most potent inhibitor of 3H-serotonin binding to rat cortical synaptosomes in vitro. However, cyproheptadine had the strongest anti-serotonin activity in rat fundus preparations, while zotepine and other neuroleptics showed the same order of potency. These results showed that zotepine is a unique neuroleptic with potent central anti-serotonin activity. The central anti-serotonin activity of zotepine is discussed in connection with its lesser extrapyramidal side effects in humans.

Animals↗
PubMed1982

Effects of anti-inflammatory drugs on triple vaccine-induced pleurisy in rats.

Effects of various anti-inflammatory drugs on triple vaccine-induced pleurisy, a model of delayed hypersensitivity, were examined and compared with those on carrageenin-induced pleurisy in rats. Steroidal drugs depressed markedly the volume of exudate and the number of leucocytes in both types of pleurisy. Gold compounds also depressed both types of pleurisy. Non-steroidal anti-inflammatory drugs were apt to show depressive effects on carrageenin-induced pleurisy, especially on increased exudate volume. BW755C produced a depressive effect on carrageenin-induced pleurisy, but on triple vaccine-induced pleurisy, BW755C produced only a slight depressive effect. Cyproheptadine produced a slight depressive effect on carrageenin-induced pleurisy, but not on triple vaccine-induced pleurisy. Promethazine had a slight depressive effect on both types of pleurisy. D-penicillamine and levamisole did not show any depressive effects on triple vaccine-induced pleurisy. The results show that reported mediators in carrageenin-induced pleurisy (prostaglandin, serotonin, leukotriene B, etc.) are not relevant to triple vaccine-induced pleurisy. Specific lymphokines and/or degradated products of complement may participate in the latter. This triple vaccine-induced pleurisy seems to be a good model for screening non-steroidal anti-inflammatory drugs which have steroidal-like activity.

Animals↗
PubMed1982

Role of food in gastrointestinal ulceration produced by indomethacin in the rat.

This study was undertaken to determine the role of food in indomethacin-induced gastrointestinal lesions. Following a 24- or 48- fast, rats were given various amounts of rat Chow pellets or various types of diets (high-bulk non-nutritive diet, equicaloric liquid diet, or liquid diet containing cellulose) for 1 h. One half hour after the feeding, 30 mg/kg of indomethacin was administered subcutaneously, and 6 h later the animals were killed and gastrointestinal lesions measured. In the fasted rat, indomethacin produced lesions predominantly in the gastric corpus. In the rat that was fed Chow pellets, indomethacin produced lesions in both the gastric antrum and small intestine. By increasing food intake, the corpus lesions decreased while antral and intestinal lesions increased. In the rat that was fed cellulose or sawdust pellets, indomethacin produced lesions in all three areas. In contrast, indomethacin did not produce any lesions in the liquid diet group. However, when cellulose was added to the liquid diet, indomethacin produced lesions in both the antrum and small intestine, the lesions increasing in proportion to increasing concentrations of cellulose. It is concluded that in indomethacin-induced gastrointestinal lesions: (a) the nutritional component of food prevents the formation of corpus lesions, and (b) the solid component of food, whether nutritive or not, plays an essential role in the formation of antral and intestinal lesions.

Animals↗
PubMed1982

Effect of 1-(2-chloroethyl)-3-isobutyl-3-(beta-maltosyl)-1-nitrosourea on experimental tumors.

The antitumor activity of 1-(2-chloroethyl)-3-isobutyl-3-(beta-maltosyl)-1-nitrosourea (TA-077), a novel water-soluble nitrosourea derivative, against leukemia L1210, Ehrlich carcinoma, sarcoma 180, Lewis lung carcinoma, Yoshida sarcoma, rat ascites hepatomas and Walker 256 carcinosarcoma was examined and compared with those of 3 reference nitrosourea antitumor agents, 1-(2-chloroethyl)-3-(beta-D-glucopyranosyl)-1-nitrosourea, 3-[(4-amino-2-methyl-5-pyrimidinyl)methyl]-1-(2-chloroethyl)-1-nitrosourea hydrochloride and 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea. TA-077 exhibited a broad antitumor spectrum against the above tumors. Among these 4 nitrosoureas, TA-077 produced the best therapeutic ratios (OD/ILS30) against leukemia L1210, irrespective of the administration route and schedule employed. The ratio obtained by consecutive treatment (ip) was superior to that by single administration, a unique characteristic of this novel nitrosourea agent. The inhibitory effect of TA-077 on the growth of non-syngenic tumors (solid form) was also significant in all administration routes employed (ip, iv and po). Furthermore, TA-077 showed a marked life-prolonging effect on both early and advanced forms of Lewis lung carcinoma.

Animals↗
PubMed1982

Canine-effective plasma concentrations of antiarrhythmic drugs on the two-stage coronary ligation arrhythmia.

Seven drugs were tested for their antiarrhythmic effects on ventricular arrhythmias 24 and 48 hr after two-stage coronary ligation in conscious beagles. Venous blood samples were drawn for plasma drug assays. Minimum effective plasma concentrations of drugs were calculated from derived concentration-time curves. Effective drugs and their minimum effective concentrations for the suppression of arrhythmias 24 and 48 hr after coronary ligation were: disopyramide, 4.2 and 2.3 micrograms/ml; procainamide, 26.4 and 27.0 micrograms/ml; phenytoin, 8.4 and 6.4 micrograms/ml; and a new beta-blocker, N-696, 7.6 and 8.7 micrograms/ml. The concentrations of disopyramide and phenytoin were almost the same as those reported for human antiarrhythmic concentrations, but those of procainamide were higher than those reported for man. Lidocaine, verapamil and a new beta-blocker, OPC-1427, were ineffective. Membrane-stabilizing effects seem to be important in suppressing the canine two-stage coronary ligation arrhythmia.

Animals↗
PubMed1982

[The propensity to malignant changes in heterozygous moles].

There are at least two mechanisms of origin for complete mole, each with different genetic implications; 1) the fertilization of an empty egg by a haploid sperm and its subsequent duplication (homozygous mole), 2) the fertilization of such an egg by two haploid sperms, which produces an heterozygous constitution of allelic genes (heterozygous mole). The present study was undertaken to investigate whether the difference of origin would determine whether the moles underwent malignant transformation or not. By using of chromosomal, enzymatic and HLA polymorphisms, 35 moles were confirmed to be androgenetic in origin. Among them fifteen homozygous and 4 heterozygous moles were identified. The persistency of high HCG titration of the urine in the mother was observed in all 4 cases from the latter (4/4-100%), though the percentage of the development of sequelae in the former was low (1/15-6.7%). The diagnosis of destructive mole was established in the uterine lesion of 2 heterozygous moles by pathological examination. These two patients had lung metastases. A high incidence of sequelae after the expulsion of heterozygous moles suggests that the heterozygous constitution of allelic genes plays an important role in the process of malignant transformation of trophoblasts.

Adult↗
PubMed1982

[Evaluation of the therapeutic effect of HCFU (1-hexylcarbamoyl-5-fluorouracil) on non-resectable stomach cancer].

The present study was aimed at investigating the efficacy of a new oral anticancer agent, HCFU, that is, (1-hexylcarbamoyl-5-fluorouracil), against 14 cases of unresectable gastric cancers which were confirmed by the laparotomy. The daily dose was 600mg and given continuously as long as the patients could take the drug orally. The efficacy was examined by X-ray photographs according to the criteria for the judgement of direct effect of the chemotherapy for solid malignant tumor. For the diffuse invasive type of gastric cancer, the changes in the X-ray finding such as stiffness and poor elasticity of gastric wall and malignant relief were also taken into consideration for the judgement. Among 9 patients, in whom the efficacy was measurable, two cases showed "partial response (PR)", two cases were diagnosed as "no change (NC)" and other 5 cases were diagnosed as "progressive disease (PD)". Among 2 partial responders, 1 case showed 85.3% decrease of the tumor size on the X-ray film and the other, who had diffuse invasive gastric cancer, showed much improvement on the X-ray film described above. The survival was around 5 months in "progressive disease" group. On the other hand, the patients with the good response to HCFU such as PR patients and NC patients could obtain a relatively longer survival period.

Adenocarcinoma↗
PubMed1982

[Antineoplastic spectrum of mitoxantrone in rat ascitic hepatoma].

The antitumor activity of mitoxantrone, a new anthraquinone derivative, was examined on 11 cell lines of ascitic hepatoma in Donryu rats. The antitumor effect of mitoxantrone was slightly weaker than other anthracycline agents. However, since the balance of antitumor effect and toxicity shows a somewhat different pattern between man and rat, it is inappropriate to conclude the value of this agent from our present test alone. The real effectiveness in man will become apparent only when this agent is used human tumors.

Animals↗
PubMed1982

[TAC-278. A new 5-FU derivative, by the oral route for its efficacy and safety in 36 patients with advanced cancers].

Tumor regression was observed in only one patient. Twelve (33%) of the 36 patients reported adverse effects: gastrointestinal symptoms in 8, CNS symptoms in 3, and others in 1. The antitumor efficacy of TAC-278 was insufficient while incidence of adverse effects was similar to other 5-FU derivatives in man and the clinical usefulness of the drug was hardly found. TAC-278 has been developed with an aim to give higher plasma concentrations of 5-FU in man. Even at a dose causing adverse effects, however, the clinical efficacy of TAC-278 was unsatisfactory. The study is a meaning tal eince the results suggest that there might be a more important factor than blood concentration of 5-FU to enhance an antitumor effect of 5-FU derivatives.

Adult↗
PubMed1982

[Visualization of intramyocardial blood flow distribution with contrast echomyocardiography].

To assess intramyocardial blood flow distribution by the contrast echocardiographic technique, we studied the effect of intracoronary injections of contrast agents on the echo intensity of the myocardium. As fundamental experiments, we made injections of ICG, urografin, artificial blood (FC-43) and microsphere into the coronary artery in open chest dogs and observed the changes in echo density of the myocardium. Bolus injection of 10 ml ICG into the coronary artery produced little change in the myocardial echo intensity, but bolus injection of 10 ml urografin, FC-43 and microsphere into the left circumflex coronary artery (LCX) and left anterior descending coronary artery (LAD) immediately increased the echo intensity of the left ventricular posterior wall (LVPW) and interventricular septum (IVS), respectively. Enhanced echo areas correlated well with the regions perfused by LCX and LAD, respectively. Clinically, we recorded two-dimensional echocardiograms during coronary arteriography (CAG) in 10 patients. In six of the 10 patients, the echo intensity of IVS increased during left CAG and in four of eight patients the echo intensity of LVPW increased during right CAG. Contrast echomyocardiography, contrast enhanced echocardiography of the myocardium, proved a useful technique for the evaluation of intramyocardial blood flow.

Animals↗