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Biomedical subjects

T Sawabe

Publications and source records attributed to T Sawabe.

53 records · Page 3Linked to original sources
PubMed1982

Studies on an anti-inflammatory agent. III. Pharmacological investigations of a new non-steroidal anti-inflammatory agent: 2-oxo-3-[4-(1-oxo-2-isoindolinyl)-phenyl]-butanamide (GP 650).

The anti-inflammatory, analgesic, antipyretic and ulcerogenic activities and acute toxicity of 2-oxo-3-[4-(1-oxo-2-isoindolinyl)-phenyl]-butanamide (GP 650) were investigated in laboratory animals and compared with those of phenylbutazone, acetylsalicylic acid (ASA), ibuprofen, tiaramide-HCl and tinoridine-HCl. The anti-inflammatory and analgesic activities of GP 650 were found to be almost equivalent to those of phenylbutazone on the basis of various anti-inflammatory and analgesic tests while its antipyretic activity was less marked, and its ulcerogenic action and acute toxicity were much lower than those of the other agents. It is interesting to note that GP 650 possesses marked anti-inflammatory activity similar to acidic anti-inflammatory agents in chronic inflammatory models along with mild antipyretic and ulcerogenic activities found in basic anti-inflammatory agents. Therefore, GP 650 appears to be a promising anti-inflammatory and analgesic agent.

Analgesics↗
PubMed1982

[Effects of dihydroergotamine mesylate (DEM) on the cardiovascular and nervous systems (author's transl)].

Effects of DEM on the cardiovascular, autonomic, and central nervous systems were studied using dogs, rats and rabbits. DEM showed relatively weak effects on the EEG in curarized rabbits and on ambulatory and drinking activities in rats. DEM suppressed dose-dependently the pressor responses induced by norepinephrine, serotonin and bilateral carotid occlusion, but had no effect on the depressor responses induced by acetylcholine and electrical stimulation to the postganglionic vagus nerve in anesthetized dogs. DEM produced a dose-dependent increase in blood pressure, a dose-dependent decrease in heart rate, a transient decrease in respiration rate, and little change in the ECG of anesthetized dogs. The pressor responses induced by DEM were inhibited by phentolamine, methysergide, and indomethacin in anesthetized dogs. With canine femoral arteries, DEM-induced contractions were blocked 10% by phentolamine, 60% by methysergide, and enhanced 10% by indomethacin. On the other hand, DEM-induced contractions of the femoral veins were blocked 30% by phentolamine, 60% by indomethacin, and 10% by methysergide. DEM provoked a significant increase in the level of prostaglandin E in the bathing fluid of the veins but not in that of the arteries. The results suggest that the arterioconstrictor responses induced by DEM are mediated mainly through the serotonin receptors, and the venoconstrictor responses induced by DEM mainly through the enhanced synthesis of prostaglandin E.

Animals↗
PubMed1981

[Comparative responsiveness of isolated saphenous, femoral and external carotid arteries and veins of dogs to dihydroergotamine mesylate (DEM) (author's transl)].

Changes in tension of spiral strips of saphenous, femoral and external carotid arteries and veins were measured isometrically. DEM stimulated 6 preparations in almost the same concentration ranges (pD2 values were 8.64 to 8.40). However, the dose-response curves for DEM indicted variations in responsiveness among the different arteries and veins. Compared with norepinephrine (NE) (1)( the intrinsic activity of DEM was 0.002 on saphenous arteries, 0.05 on saphenous veins, 0.03 on femoral arteries, 0.18 on femoral veins, 0.13 on external carotid arteries and 0.13 on external carotid jugular veins. Thus DEM contracted more potently the venous strips from the hind limbs. IN femoral and external carotid arteries, antagonism of serotonin by DEM or methysergide was investigated. DEM displaced the dose-contractile response curves for serotonin in a noncompetitive manner, and the antagonistic response of DEM to serotonin was about 8 times more effective in external carotid arteries (pD'2 value=6.96) than in femoral arteries (pD'2 value=6.05). Methysergide, unlike DEM, antagonized the response to serotonin in a competitive manner at low doses but in a noncompetitive manner in high doses, and was fairly equal in antagonizing response to serotonin in external carotid arteries (pA2 value=that the therapeutic value of DEM in the treatment of orthostatic hypotension is due to its selective anti-serotonin activity on the external carotid arteries.

Animals↗
PubMed1980

Influence of adjuvant arthritis on main urinary metabolites of prostaglandin F and E in rats.

The influence of adjuvant arthritis in rats on main urinary metabolites (MUM) of prostaglandin (PG) F and E type was studied. 1) In our model rats, urinary excretion of PGE-MUM increased on day 11 prior to the appearance of secondary lesions, but that of PGF-MUM did not change significantly during the observed period (21 days). The excretion of PGE-MUM was not proportional to the increase in both hind paws volume. 2) Indomethacin, which diminished primary lesions but did not suppress secondary lesions, reduced the increase in urinary excretion of PGE-MUM. 3) Prednisolone and azathiopurine, which suppressed both primary and secondary lesions, increased the excretion of PGE-MUM over adjuvant control values on days 4 and 8. The facts described above suggest that the increase of endogenous PGE during days 4 to 8 may be important in the suppression of secondary lesions in adjuvant arthritis in rats.

Animals↗
PubMed1978

[The study of developmental pharmacology (I). Effect of pentazocine HCl on the physiology of rats given the drug during perinatal and postnatal periods (author's transl)].

The effects of drug administration on the dams (F0) and their offspring (F1), particularly on the central nervous and reproductive functions of F1, were studied by oral administration of pentazocine HCl to rats during the perinatal and postnatal periods. No significant differences were observed between administered and control rats regarding body weight changes and food intake during perinatal and postnatal periods in F0 at all dosages, but temporary salivation was observed in the 200 and 100 mg/kg groups, and decline of spontaneous activity and respiratory rate, disappearance of righting reflex, clonic convulsion were observed in some of the 200 mg/kg group. No significant differences were observed regarding litter size, birth rate, state and timing of differentiation as postnatal development, sex maturity, reproductive function in F1, although some groups were slightly inferior in body weight at birth and during the nursing period. Furthermore, no differences were observed in respect to the nervous functions of balance, exercise and psychotic related activity in the open-field test.

Administration, Oral↗
PubMed1978

[The study of developmental pharmacology (II). Histological observations of central nervous tissue in rats of dams given pentazocine HCl during perinatal and postnatal periods (author's transl)].

In previous literature, we reported that the rats whose dams had been administerd pentazocine HCl 200 mg/kg/day during the perinatal and postnatal periods, showed no differences between control rats in the physiological function and psychotic activity tests. Brain tissues of the rats were observed histologically herein to confirm the result of previous tests. Abnormal findings such as deficits, undevelopment and metamorphosis, in the shape, size and configuration of nerve cells, myelin sheaths and vessels in consecutive transverse sections stained by Nissl and Klüver-Barrera method were not evident on examination under light microscope, and in cell bodies, dendrites, axons, myelin sheaths, synaptic complexes of nerve cell, neuroglia and vessels in the cerebral cortex, under electron microscope. The lack of abnormal findings in the histological observation of brain tissues supports the result of previously conducted physiological function and psychotic activity tests in which no significant differences were found between treated and control rats. Pentazocine HCl had no effect on the brain tissues of rat offspring from dams administered the drug during perinatal and postnatal periods.

Animals↗
PubMed1978

Studies on combination dosing (III). Aspirin and ethenzamide.

In our studies with drug combinations, we search for mixtures which would enhance the effectiveness of the related active substances. Ethenzamide was found to possess a specific suppressive effect on the gastric damage induced by aspirin. Such effect could not be demonstrated in analgesic agents such as salicylamide, bucetin, acetaminophen and phenacetin. The combination of aspirin with ethenzamide had a potentiating effect on analgesic activity and reduced motor incoordination and loss of righting reflex. We calculated the safety margins of various ratios of combinations and concluded that the best was aspirin and ethenzamide at a ratio of 2:3.

Analgesics↗