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T Nose

Publications and source records attributed to T Nose.

At least 343 records · Page 19Linked to original sources
PubMed1982

Acute toxicity study of KB-944, a new calcium antagonist.

The acute toxicity of diethyl 4-(benzothiazol-2-yl)benzylphosphonate (KB-944) was studied in mice, rats and dogs: In mice and rats, toxic symptoms such as deceleration of spontaneous movement, ataxic gait, disappearance of righting reflex, reduction in body temperature and suppression of breathing appeared following administration of a single dose of KB-944. The symptoms developed in dogs were depression, bradycardia and labored breathing. The LD50 values determined in male and female rats were 1622 and 1555 mg/kg, respectively, for oral administration, 2216 and 2820 mg/kg for subcutaneous injection, and 762 and 479 mg/kg for intraperitoneal injection. The LD50 values determined in male and female mice were 2807 and 3856 mg/kg, respectively, for oral administration, greater than 4000 mg/kg for subcutaneous injection, and 815 and 777 mg/kg for intraperitoneal injection. As shown above, there was no evident difference in LD50 between sexes in either species of animals. Since many of the dogs given an oral dose larger than 1000 mg/kg vomited the drug, oral LD50 value could not be determined.

Animals↗
PubMed1982

1-month subacute oral toxicity study of KB-944, a new calcium antagonist, in rats.

Diethyl 4-(benzothiazol-2-yl)benzylphosphonate (KB-944), a new Ca-antagonist, in the dose range of 25--200 mg/kg/day, was orally administered to Jcl:SD rats for five consecutive weeks and the following results were obtained. Neither death nor inhibition of body weight gain nor any toxic symptoms of the drug were noted in rats but an increase in water intake was found in the rats treated with over 100 mg/kg/day of KB-944. In plasma there was a decrease in alkaline phosphatase activity, creatinine level and cholinesterase activity and an increase in GPT activity and total cholesterol level in rats given a higher dosage of the drug. Weight gain of the liver, kidneys, heart, adrenals and ovaries, and degeneration in the epithelium of the renal proximal tubule were observed. However, none of these changes were serious and the maximum non-toxic dose of KB-944 was 25 mg/kg/day.

Animals↗
PubMed1982

1-month subacute oral toxicity study of KB-944, a new calcium antagonist, in beagles.

Using male and female Beagles, we studied the subacute toxicity of diethyl 4-(benzothiazol-2-yl)benzylphosphonate (KB-944) administered orally and the following results were obtained. No dogs died during the administration period. Both male and female dogs given 200 mg/kg and those given 100 mg/kg underwent body weight decrease and inhibition of body weight increase, respectively. Enlargement of liver cells occurred in male dogs given 200 mg/kg and female dogs given 100 or 200 mg/kg. There were no further findings, even histopathologically, which showed any toxic effect of the drug. The maximum non-toxic dose of this drug was considered to be 30 mg/kg.

Animals↗
PubMed1982

The studies of the mechanism of antiinflammatory action of 2-(5-ethylpyridin-2-yl)benzimidazole (KB-1043).

The mechanism of the antiinflammatory activity of 2-(5-ethylpyridin-2-ly)benzimidazole (KB-1043), a new benzimidazole derivative with antiinflammatory, analgesic and antipyretic activities, is described. KB-1043 inhibits the emigration of leucocytes and the exudation of protein into the site of injury. KB-1043 possesses also a potent membrane stabilizing activity. Although KB-1043, in vitro, did not inhibit the enzyme activity, the increase of enzyme activity at the site of injury was inhibited by the oral administration of KB-1043. The inhibitory effect of KB-1043 on prostaglandin synthesis was slightly weaker than that of acetylsalicylic acid (ASA). The antiinflammatory effect of DB-1043 was observed also in adrenalectomized rats and spinalectomized rats.

Adrenalectomy↗
PubMed1982

Pharmacological studies of a new non-steroidal antiinflammatory drug: 2-(5-ethylpyridin-2-yl)benzimidazole (KB-1043).

2-(5-Ethylpyridin-2-yl)benzimidazole (KB-1043) is a new benzimidazole derivative with marked antiinflammatory, analgesic and antipyretic properties. KB-1043 possesses potent inhibitory activities on the acute inflammatory edema induced by chemical and physical irritants in the hind paw of rats, but almost ineffective (similar to tiaramide) against adjuvant-induced polyarthritis in the rat. The antagonistic effects of KB-1043 on increased vascular permeability are more potent than those of phenylbutazone, and the analgesic effects of KB-1043 on the pain induced by chemical and mechanical stimulations were nearly equal to, or slightly less potent than, those of tiaramide and phenylbutazone. The fevers induced by brewer's yeast and polysaccharide from Pseudomonas fluorescens (T.T.G.) were lowered by KB-1043. THe ulcerogenic activity of KB-1043 was weaker than those of tiaramide and phenylbutazone. The therapeutic index of KB-1043 therefore is superior to those of tiaramide and phenylbutazone.

Analgesics↗
PubMed1981

Computed tomography in von Recklinghausen's disease.

Though we knew it would be difficult to predict whether a child having von Recklinghausen's disease would develop a central nervous system lesion in the future, we tried to find a clue to this question in our study, by comparing computed tomography (CT) findings of 18 children with those of 21 adults. 55% of the children and 85% of the adults showed abnormal findings on CT. The most common finding was mild ventricular dilatation without periventricular hypodensity. Some of them showed ventricular stasis without block on radioisotope cisternography.

Adolescent↗
PubMed1981

Platelet aggregation in patients with Moyamoya disease.

Platelet aggregation was studied by giving ADP or adrenalin to 28 patients with Moyamoya disease. There were 7 males and 21 females, and 27 normal controls, 11 males and 16 females. We found that 2 muM of ADP, and 9.1 and 22.7 muM of adrenalin induced statistically significant increases in nondissociative patterns of platelet aggregation in the patient group. Maximum aggregation was significantly increased in the patient group compared with the controls by the addition of ADP (2 and 4 muM) or adrenalin (9.1 and 22.7 muM). When patients were divided into two groups under and over 20 years of age, there was no discernible difference of platelet aggregation in either group.

Adenosine Diphosphate↗
PubMed1981

[Effects of dehydroepiandrosterone sulfate on serum steroid hormones in pregnant rabbits (author's transl)].

After the administration of dehydroepiandrosterone sulfate (DHAS) (0,10,30,70 mg/kg, i.v.) to rabbits during late pregnancy, serum concentration of DHAS, dehydroepiandrosterone (DHA), testosterone (T), estradiol (E2) and progesterone (Prog) were determined by radioimmunoassay. Serum levels of DHAS increased dose-dependently, and were reduced biphasically to normal levels at 24 hr after the administration. Similarly, the levels of DHA, T and E2 increased, and reached the maximum at 30 min after, though the increase of DHA or T was one-thousandth that of DHAS, and that of E2 was about one-hundred-thousandth. On the other hand, Prog concentration in sera decreased to 50 approximately 60% of that before the injection at 30 min after (p less than 0.05). These results suggest that the changes observed in E2 and Prog levels after the injection of DHAS into pregnant rabbits corresponded to the changes of endogeneous E2 and Prog seen in early parturition in women.

Animals↗
PubMed1981

[Antiulcerogenic action of 7-chloro-1-cyclopropylmethyl-1,3-dihydro-5-(2-fluorophenyl)-2H-1,4-benzodiazepin-2-one (KB-509), a new benzodiazepine derivative].

Effects of KB-509, a new derivative of benzodiazepines and expected to be classified as an antianxiety drug, were studied on the experimental stress ulcers and serum 11-hydroxycorticosterone (11-OHCS) in mice. Firstly, we looked for a stress procedure under which diazepam would show antiulcerogenic effects at a lower dose than those required for a muscle relaxant effect in this species. We found that diazepam possessed a strong antiulcerogenic activity under the stress procedure (26 degrees C, 5 hr restraint and water immersion). KB-509 had a potent protective effect on the erosions induced by the present mild stress method at a considerably low dose (ED50: 0.36 mg/kg, p.o.) and the potency was about 3 and 9 times greater than that of diazepam and atropine sulfate, respectively. KB-509 did not affect indomethacin-induced gastric erosions and thermal ulcers, as did diazepam. KB-509 and diazepam depressed stress-induced increase of serum 11-OHCS in mice, but not at the low doses required for antiulcerogenic effects. In conclusion, the results in this study suggest that the stress method described may be used to evaluate the antianxiety effect of benzodiazepines, especially in mice, and that KB-509 is superior to both diazepam and atropine in antiulcerogenic activity.

11-Hydroxycorticosteroids↗
PubMed1981

[Computed tomography in hypertensive cerebellar hemorrhage (author's transl)].

Fourteen cases of cerebellar hemorrhage were analysed from the point of CT-scan, and the following results were obtained. 1. The number of cases of cerebellar hemorrhage forms 4.4% of that of total intracranial hemorrhage. 2. Most of the cerebellar hematomas extend upward. Downward extension is rare. 3. In acute dead cases hematomas are 5 cm or more in diameter and lie over bilateral hemistpheres with the extension to third or fourth ventricles in CT-scans. 4. Slowly progressive cases are deteriorated by the secondary hydrocephalus. 5. In mild cases hematomas are 3cm or less in diameter on CT-scans and the hematoma evacuation is not indicated for these cases. 6. The shunt operation alone is sufficient for the life saving of the slowly progressive cases, but the hematoma evacuation is indicated in these cases if the functional prognosis is taken into consideration. 7. Immediate hematoma evacuation together with the ventricular drainage is considered to be effective for the life saving of the acute fulminant cases.

Aged↗
PubMed1980

Different antihypertensive effects of nifedipine in conscious experimental hypertensive and normotensive rats.

Antihypertensive effects of nifedipine and hydralazine were investigated in normotensive rats, spontaneously hypertensive rats (SHR), DOCA-NaCl hypertensive rats and renal hypertensive rats all in a conscious state. The blood pressure fall after nifedipine 5 mg/kg p.o. was 22% of the initial value in normotensive rats, 49% in SHR, 53% in DOCA-NaCl hypertensive rats and 44% in renal hypertensive rats. Hydralazine in the same dose decreased the blood pressure by 40% in normotensive rats, 52% in SHR, 33% in DOCA-NaCl hypertensive rats and 54% in renal hypertensive rats. The selective action of nifedipine in hypertensive rats in contrast to normotensive rats seemed to be attributable to the different affinity for calcium ion of vascular smooth muscle of hypertensive rats as compared with that of normotensive rats. Also, the heart rate of hypertensive rats or normotensive rats was increased with nifedipine but less than with hydralazine.

Animals↗
PubMed1980

[Effects of dehydroepiandrosterone sulfate on serum steroid hormones and endocrine organs in adrenalectomized immature female rats (author's transl)].

SD female rats were bilaterally adrenalectomized or sham-operated at the age of 20 days and were given dehydroepiandrosterone sulfate (DHAS; 50 or 100 mg/kg body wt. p.o.) for 7 days. Twenty-four hours after the last administration the animals were sacrificed and levels of serum estrone, estradiol, estriol, testosterone (T), progesterone(P), aldosterone, 11-OH-corticosteroid (11-OH-CS), dehydroepiandrosterone (DHA) and DHAS were determined. Uterus, ovary, pituitary gland, thyroid, thymus, liver and kidney were weighed and examined histologically. Adrenalectomy significantly reduced serum levels of T, P, aldosterone, 11-OH-CS, DHA and DHAS organ weights of liver and kidney, and increased the weight of the thymus. In sham-operated rats, DHAS increased weight of the uterus and serum DHAS level while the other hormones and organs were not affected. In the adrenalectomized rats, DHAS increased the serum levels of DHAS and T, weight of the uterus and inhibited increase in the weight of the thymus. These findings suggest that DHAS-induced increases in the weight of uterus are not affected by endogenous hormones secreted from the adrenal gland.

Adrenalectomy↗
PubMed1980

[Psycopharmacological and general pharmacological studies of 7-chloro-1-cyclopropylmethyl-1, 3-dihydro-5-(2-fluorophenyl)-2H-1, 4-benzodiazepin-2-one (KB-509) (author's transl)].

KB-509, a new derivative of benzodiazepines, increased locomotor activities of mice in doses of 8-32 mg/kg (p.o.) and a decrease occurred with higher doses. This drug was 3-6 and 1-2 times more potent than diazepam (DZP) and nitrazepam (NZP), respectively, in anticonvulsant (anti-pentylenetetrazol, bemegride, strychnine) activities, antiaggressive activity and potentiation of chlorprothixene-induced hypnosis in mice. On the other hand, KB-509 possessed similar potency to DZP and NZP in muscle relaxant activity in mice and inhibition of flexor in cats, and was markedly weaker than DZP and NZP in causing a loss of righting reflex in mice. In the spontaneous EEG activity, KB-509 induced a drowsy pattern and slightly inhibited arousal response to EEG in rabbits, as did DZP. In particular, KB-509 was more potent than DZP in suppressing the amygdala afterdischarge and had a longer duration of action. KB-509 and DZP slightly depressed body temperature, the cardio-respiratory system and the gastrointestinal tract in high doses. Potentiation of spontaneous motility of the uterus and increase of urine excretion were also observed with high doses. In conclusion, KB-509 is superior to both DZP and NZP in the ratio of anticonvulsant and/or taming activities and muscle relaxant activity, and has a weak central depressant activity.

Animals↗