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Biomedical subjects

K Hirose

Publications and source records attributed to K Hirose.

At least 415 records · Page 23Linked to original sources
PubMed1985

A descriptive epidemiological study of hematopoietic neoplasms in Japan.

In 1982, the number of deaths from hematopoietic neoplasms was 5,885 for males and 4,237 for females, which corresponded to about 6% of all malignant neoplasms. The increase in the age-adjusted death rate in the last 10 years was highest for lymphatic leukemia (1.8 times), followed by multiple myeloma (1.7 times), malignant lymphomas (1.3 times) and myelogenous leukemia (1.1 times). In the old-age group, i.e., over 70, the death rate for all types of hematopoietic neoplasms markedly during this period, particularly for multiple myeloma. In children, however, an increase in lymphatic leukemia and a decrease in decrease in myelogenous leukemia were observed. Geographical marked excess in the death rates for malignant lymphomas and lymphatic leukemia in the Kyushu district, especially in the middle- and old-age groups. This may be attributed to the high incidence of adult T-cell leukemia/lymphoma in the southwestern part of Japan. The age-adjusted death rate for malignant lymphomas was slightly higher in rural areas than in urban areas in males in Kyushu.

Adolescent↗
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

Primary mucoepidermoid carcinoma in the thyroid gland. A case report including an ultrastructural and biochemical study.

An extremely rare mucoepidermoid carcinoma of the thyroid gland was found in a 44-year-old woman. By light microscopic examination, the tumor consisted of mucous cells and squamoid cells, and was similar to that occurring in any other organs. By electron microscopic examination, the mucous cells displayed prominent mucous droplets, and showed no evidence of colloid production in their cytoplasms. Abundant tonofilaments in aggregates were observed in the squamoid cells. Biochemically, thyroxine (T4) and triiodothyronine (T3) were not detectable in the tissue of this tumor. These findings indicate that this mucoepidermoid carcinoma does not retain the functional properties of thyroid follicular cells; namely, no evidence was found to substantiate a follicular epithelial origin of this tumor.

Adenocarcinoma↗
PubMed1984

A genetic variant of Emery-Dreifuss disease. Muscular dystrophy with humeropelvic distribution, early joint contracture, and permanent atrial paralysis.

A 38-year-old woman, a product of consanguineous parents, had been observed to have limited neck flexion and elbow joints contracture since early childhood. In addition, she experienced humeropelvic muscular weakness and atrophy, so that she was unable to walk by age 27. At 34 years of age, she required a permanent pacemaker to treat complete atrioventricular block with ventricular bradycardia. A myocardial biopsy confirmed cardiomyopathy. The clinical features of the present case are similar to those of the Emery-Dreifuss syndrome; however, this case may be inherited through an autosomal recessive trait.

Adult↗
PubMed1984

Synthesis and neuroleptic activity of N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-5-sulfonamidobenzamide s.

A series of some novel N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamides involving replacement of the sulfamoyl group in sulpiride with a sulfonamido group was synthesized and tested for dopamine receptor blockade. In comparison with sulpiride, several compounds were considerably more potent than sulpiride as dopamine receptor blockers. The structure-activity relationships are discussed.

Animals↗
PubMed1984

[Pharmacological studies of a new sleep-inducer, 1H-1,2,4-triazolyl benzophenone derivatives (450191-S) (I). Behavioral analysis].

The behavioral effects of 450191-S and its metabolites were investigated in mice, rats, cats and rhesus monkeys, and they were compared with those of related benzodiazepines (BDZ) such as diazepam and nitrazepam. Oral administration of 450191-S consistently caused sedation without excitability in mice and rats, and it was only 1/2 to 1/266 as potent as the BDZ in producing motor incoordination as assessed by traction, rotarod performance and inclined screen tests in mice, induced much less ataxia in cats and monkeys, and inhibited respiration in anesthetized cats. The locomotor activities of mice and rats measured by Animex and the open field test were not affected by 450191-S, but rearing and preening decreased with 450191-S as with the BDZ. 450191-S was equipotent with nitrazepam and 2 to 6 times more potent than diazepam and estazolam in potentiating chlorprothixene-induced hypnosis and thiopental-Na-induced anesthesia. These effects were not different with successive 14-day administration of 450191-S. Anti-pentylenetetrazol, picrotoxin and bicuculline convulsions of 450191-S had the same potency as nitrazepam, but caused much less anti-electroshock convulsion than the BDZ. 450191-S had potent antianxiety activity as observed by anti-aggressive and anti-conflict activities and had almost the same effect as diazepam on operant behavior. The metabolites M-1, M-2, M-A and M-3 showed approximately the same potency as 450191-S in inducing anesthetic potentiation and antianxiety activity, but they were much more potent in causing disturbance of the somatic functions. These results indicate that 450191-S possesses inhibitory effects on the central nervous system, including a potent sleep-inducing effect, and is characterized by markedly weak muscle relaxant activity and motor incoordination.

Aggression↗
PubMed1984

[Pharmacological studies of a new sleep-inducer, 1H-1,2,4-triazolyl benzophenone derivative (450191-S) (V). General pharmacological activities].

General pharmacological activities of 450191-S were studied in various species of animals and compared with those of reference benzodiazepines (BDZ). 450191-S at doses of 10 mg/kg slightly decreased (-5 degrees C) the rectal temperature of rabbits. 450191-S decreased respiratory and heart rates in anesthetized cats, but the effects were less than those of diazepam or triazolam. 450191-S increased respiratory and heart rates in conscious dogs, but had no effect on the blood pressure, electrocardiogram and autonomic nervous system in cats and dogs. The drug displayed a slight spasmolytic activity in the small intestine of guinea pigs and a slight inhibitory effect on isolated non-pregnant and pregnant uteri of rats. These effects were less than those of diazepam or nitrazepam. Below doses of 25 mg/kg, 450191-S did not affect urinary volume and electrolyte excretions in rats. It also decreased brain norepinephrine (NE) turnover rates in rats, but decreased NE and dopamine turnover rates in mice. These effects of 450191-S were less than those of nitrazepam. 450191-S was found to be minimally irritating to the ocular mucosa in rabbits and did not irritate the stomach and small intestine in rats. These effects were also compared with those of active metabolites of 450191-S, M-1, M-2, M-A, M-3 and M-4, and the superiority of the mother compound over its metabolites was clarified.

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↗
PubMed1983

Comparison of inhibitory effects of substituted benzamides and classical neuroleptics on operant behavior in rats and squirrel monkeys.

The operant behavioral effects of the substituted benzamides metoclopramide, sultopride and sulpiride were compared with those of chlorpromazine and haloperidol using lateral hypothalamic self-stimulation of the brain in rats and Sidman avoidance responding in rats and squirrel monkeys. All the drugs inhibited both phenomena dose-dependently in rats. The order of potency was: haloperidol greater than chlorpromazine greater than metoclopramide greater than sultopride greater than sulpiride. Sulpiride only produced moderate inhibition even at 128 mg/kg s.c. All drugs also suppressed Sidman avoidance in squirrel monkeys, which were far more sensitive than rats to the inhibitory effects of all three benzamides. In monkeys, sulpiride 8 mg/kg i.m. apparently suppressed Sidman avoidance with a delayed onset and a prolonged duration, which contrasted with the rapid onset and short duration of metoclopramide action. Thus, long-term observation of the behavioral effects of benzamides in squirrel monkeys may provide more precise information on the clinical antipsychotic efficacy of substituted benzamides.

Animals↗
PubMed1983

Relative in vitro effectiveness of 17 alpha, 20 beta-dihydroxy-4-pregnen-3-one and other pregnene derivatives on germinal vesicle breakdown in oocytes of ayu (Plecoglossus altivelis), amago salmon (Oncorhynchus rhodurus), rainbow trout (Salmo gairdneri), and goldfish (Carassius auratus).

The relative effectiveness of several pregnene derivatives, which had previously been identified in the ovaries of ayu (Plecoglossus altivelis), on germinal vesicle breakdown (GVBD) was investigated in vitro using folliculated oocytes of four species of teleosts, ayu, amago salmon (Oncorhynchus rhodurus), rainbow trout (Salmo gairdneri), and goldfish (Carassius auratus). Although some species differences existed in the relative effectiveness of each steroid on GVBD, 17 alpha, 20 beta-dihydroxy-4-pregnen-3-one (17 alpha, 20 beta-diOHprog) was consistently the most potent inducer of final oocyte maturation. Both progesterone and 17 alpha-hydroxyprogesterone were effective at relatively high concentrations. Of the 5 beta-reduced metabolites, 17 alpha, 20 beta-dihydroxy-5 beta-pregnan-3-one was almost as effective as 17 alpha, 20 beta-diOHprog in oocytes of amago salmon and rainbow trout, while the other 5 beta-reduced compounds (3 alpha-hydroxy-5 beta-pregnan-20-one, 17 alpha-hydroxy-5 beta-pregnane-3,20-dione, 3 alpha, 17 alpha-dihydroxy-5 beta-pregnan-20-one, 5 beta-pregnane-3 alpha, 17 alpha, 20 beta-triol, and 5 beta-pregnane-3 beta, 17 alpha, 20 beta-triol) were almost or totally ineffective at the concentrations tested (1-0.001 micrograms/ml). These bioassay results, together with previous findings on the capacity of the ovary to produce 17 alpha, 20 beta-diOHprog, indicate that 17 alpha, 20 beta-diOHprog is the natural maturation-inducing steroid hormone common to three species of Salmoniformes, ayu, amago salmon, and rainbow trout. These results, however, only suggest that 17 alpha, 20 beta-diOHprog is involved in maturation of goldfish oocytes, since supportive physiological and biochemical data are lacking. Possible regulatory roles of 5 beta-reduced metabolites on steroid-induced oocyte maturation are discussed.

Animals↗
PubMed1983

Carcinoma in situ of germ cells and subsequent development of an invasive seminoma in a hyperprolactinaemic man.

A 25-year-old man was first seen complaining of impotence and found to have a pituitary tumour and hyperprolactinaemia. Both testes were small and atrophic, but a testicular tumour was not apparent. Biopsy of the right testis was performed, and the pathology report described thickening of the seminiferous tubule walls and impaired spermatogenesis. The patient refused to undergo an operation for his pituitary tumour and was lost to follow-up. 5 years later, the same patient presented with enlargement of his right testis, and this and the pituitary tumour were excised. The testicular tumour was classified as seminoma, and the pituitary tumour as an adenoma with low malignancy. Re-examination of the previous specimen of his right testis revealed foci of carcinoma-in-situ. This is an additional example of the growth of an invasive germ cell tumour from non-invasive carcinoma-in-situ of the testis.

Adenoma↗