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Biomedical subjects

K Hirose

Publications and source records attributed to K Hirose.

At least 433 records · Page 24Linked to original sources
PubMed1983

The term "Takayasu's disease" should be abolished.

The case described by Takayasu and referred to in later years by the term "Takayasu's disease" is a condition radically distinct from the currently established Takayasu-Ohnishi's disease in that the original case report indicates no constitutional or systemic abnormalities and refers to the regional blood flow abnormalities with annular anastomoses of the central retinal blood vessels. The term "Takayasu's disease" should, therefore, be abolished. It was coined heedlessly by his juniors, including the author, without an exhaustive search of the literature. It was of no concern to Takayasu himself. I propose the term "aortic arch arteriostenosis syndrome" (Okamura 1938 and Yui 1943) to be used for the disease of which the pathogenetic mechanism has been established with a general trend of acceptance of its multifactorial etiology.

Adult↗
PubMed1982

Differential effects of sulpiride and metoclopramide on brain. Homovanillic acid levels and shuttle box avoidance after systemic and intracerebral administration.

Sulpiride (SUL) is more efficacious in antipsychotic activity than metoclopramide (MET), although both appear to possess almost equal affinities for dopamine (DA) receptors. We studied the effects of SUL and MET on the brain homovanillic acid (HVA) level and shuttle box avoidance to clarify their differential modes of action on the blockade of DA receptors. SUL was several times less potent than MET, which was about 50 times less potent than the control drug haloperidol (HAL), for increasing HVA at 4 h after s.c. administration. However, SUL was about 50 times more potent than MET and about equipotent to HAL, at 2 h after drug administration into the lateral ventricle. The potency of SUL by intraventricular administration was 20-fold or more than that by intracisternal administration. HAL and MET did not show such a discrepancy. The HVA level reached the maximum 1 h after intraventricular administration of MET or HAL, while s.c., intracisternal or intraventricular administration of SUL caused a gradual increase in the HVA level with the maximum being reached after 6-8 h. In shuttle box avoidance, MET was about 25 times more potent than SUL by intraperitoneal administration but about 200 times less potent than SUL, which was about 10 times more potent than HAL, by intraventricular administration. These results suggest that SUL causes a potent, long-lasting blockade of DA receptors, while MET has only a weak, short-lasting action. These findings may be related to the differences in their clinical efficacy.

Animals↗
PubMed1982

Amino acid amide derivatives of 2-[3-(aminomethyl)-4H-1,2,4-triazol-4-yl]benzophenones, a novel class of annelated peptidoaminobenzophenones.

A series of the title compounds was prepared via condensation of the 3-(aminomethyl)triazolylbenzophenone (5) with N-protected amino acids, followed by deprotection, amination of the 3-[(chloroacetamido)methyl]triazolylbenzophenone (6a,b), or reduction of the relevant azide derivative (6c). Some of the title compounds were also derived directly from the quinazolines 3 or 4 by acid-induced rearrangement, followed by deprotection. These new amino acid amide derivatives of the triazolylbenzophenones (2) were evaluated for central nervous system (CNS) activity. Members of this class of compounds exhibited a high level of CNS activities. For example, 2',5-dichloro-2-[3-[(glycylamino)methyl]-5-methyl-4H-1,2,4-triazol-4-yl] benzophenone (2c) was as active as triazolam, with an ED50 of 0.58 mg/kg (mice, po), against antifighting activity in the foot shock-induced fighting test. Other triazolylbenzophenone derivatives (2a-f) showed similar pharmacological activities.

Anesthesia↗
PubMed1982

Development of glomerular lesions in experimental long-term diabetes in the rat.

Exact parameters for relevant glomerular structures in the course of streptozotocin diabetes in rats with 1 to 18 months' duration were obtained with stereological methods. Renal cortical tissue from diabetic (D) and control animals (C) was processed for light- and electron microscopy and measurements were performed on systematically sampled glomeruli. The thickness of the basement membrane (BM) increased with age in both groups, but the rate of increase was 50% higher in D: 19 +/- 1.2 nm/month (mean +/- SD) vs. 13 +/- 0.9 nm/month, P = 0.0003. The time course of other structural quantities was characterized by the acute changes constituting the glomerular hypertrophy, earlier shown to develop within the first few days of diabetes. All these changes were confirmed in the present study: In the earliest phase the diabetic rats showed an increased total volume of glomeruli, mesangium, and mesangial BM material, as well as an increased surface of the capillary walls. However, none of these differences between the groups showed progression with increasing duration. Mesangial changes corresponding to those of the glomerulopathy in long-term diabetes were not demonstrable within the experimental period. The streptozotocin diabetic rat, therefore, is not useful as a model of advanced diabetic glomerulopathy. But the BM thickness follows the same predictable time course as in human diabetes insofar as moderately advanced cases are concerned. BM thickness is the parameter of choice when a potential effect of different variables on the development of diabetic glomerulopathy is under study.

Animals↗
PubMed1982

Inhibition of metabolic cooperation in Chinese hamster cells by organochlorine pesticides.

Effects of organochlorine pesticides on the metabolic cooperation in the hypoxanthine-guanine-phosphoribosyl-transferase system using wild-type 6-thioguanine-sensitive V79 cells and variant 6-thioguanine-resistant cells were surveyed. The metabolic cooperation was inhibited by 1,1,1-trichloro-2,2-bis(p-chlorophenyl)ethane (DDT), 1,1-dichloro-2,2-bis(p-chlorophenyl)ethane (TDE), 1,1,1-trichloro-2-(o-chlorophenyl)-2-(p-chlorophenyl)ethane (o,p'-DDT), 1,1,1-trichloro-2,2-bis(p-methoxyphenyl)ethane (methoxychlor), aldrin, dieldrin, endrin, heptachlor, alpha-isomer of benzene hexachloride (alpha-BHC), and gamma-BHC, but not beta-BHC. The present results suggest that the pesticides which inhibited the metabolic cooperation may be tumor promoters.

Animals↗
PubMed1982

Effect of trapidil on regional myocardial function during acute coronary occlusion in the dog.

The effects of an antianginal agent, N,N-diethyl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidine-7-amine (trapidil, Rocornal) (5-10 mg/kg), on regional myocardial function were studied in 17 open-chest dogs. The animals were instrumented with a micromanometer for measurement of left ventricular pressure, an electromagnetic flow probe around the left circumflex coronary artery, and 3 pairs of ultrasonic crystals in control, marginal and ischemia-induced segments. In cases of an intact coronary artery, trapidil increased peak dP/dt by 48%, heart rate by 19%, and coronary blood flow by 40%. End-diastolic segment length decreased by 7% with an increase of 17% in shortening. Coronary occlusion increased end-diastolic length of all three segments. In the ischemic segment, active shortening was rapidly replaced by systolic expansion. In the marginal segment, percent shortening decreased by 58%, while in the control segment, shortening was augmented by 11%. Trapidil administered during coronary occlusion significantly improved the shortening of control and marginal segments, as associated with a reduction in end-diastolic length. There was no significant change in function of the ischemic segment. These effects of tripidil during coronary occlusion were not blocked by propranolol (0.5-1.0 mg/kg). These data suggest that trapidil may be an effective treatment for left ventricular failure due to myocardial ischemia by virtue of its potent positive inotropic effects associated with substantial increases in myocardial blood supply sufficient to counteract the increase in oxygen consumption.

Acute Disease↗
PubMed1981

Novel peptidoaminobenzophenones, terminal N-substituted peptidoaminobenzophenones, and N-(acylglycyl)aminobenzophenones as open-ring derivatives of benzodiazepines.

Peptidoaminobenzophenones (1), terminal N-substituted peptidoaminobenzophenones (14), and acylglycylaminobenzophenones (16) were prepared as a novel series of ring-opened derivatives of 1,4-benzodiazepine. Z-Gly- and Z-Ala-N-methylaminobenzophenones (4) were treated with HBr-HOAc to give Gly- and Ala-N-methylaminobenzophenone hydrobromides (8). Reaction of 8 with chloroacetyl chloride in dimethylformamide (DMF) or hexamethylphosphoramide (HMPA) gave chloracetamide (13), which was allowed to react with various amines to afford a number of terminal N-substituted derivatives (14). Reaction of 8 with various acyl halides in HMPA or DMF gave a number of acylglycyl-N-methylaminobenzophenones (16). Peptidoaminobenzophenones (1) were also prepared by several convenient methods. Many of these compounds exhibited high CNS activity in animals when given orally. In antianxiety activity the potency of some compounds is equal to or higher than that of diazepam.

Animals↗
PubMed1981

Incompatibility of citrate utilization plasmids isolated from Escherichia coli.

The 57 conjugative Cit plasmids isolated from 72 citrate-utilizing (Cit+) Escherichia coli strains from various sources were classified into four groups on the basis of their genetic properties. Escherichia coli K13 strains carrying these Cit plasmids could utilize cis-aconitate or tricarballylate, in addition to citrate.

Citrates↗