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Biomedical subjects

H Miyake

Publications and source records attributed to H Miyake.

At least 505 records · Page 28Linked to original sources
PubMed1986

Surgically treated cerebral arterial ectasia with so-called moyamoya vessels.

The case of a 43-year-old woman with multiple intracranial arterial ectasia was reported. The arterial ectasia was accompanied by stenosis of the middle cerebral artery and so-called moyamoya vessels. After extracranial to intracranial bypass surgery, the size and contour of the arterial ectasia decreased. Because the arterial ectasia decreased in size after the extracranial to intracranial bypass surgery, this operation might be useful for space-occupying lesions due to arterial ectasia.

Adult↗
PubMed1986

[Anti-inflammatory effect of THS-201, a new intra-articular steroid].

The effect of THS-201, a new intra-articular steroid, on inflammations was examined using acute, subacute and chronic experimental models, and the antiinflammatory action of THS-201 was compared with those of reference steroids such as triamcinolone acetonide (TA), methylprednisolone acetate (MPA), hydrocortisone acetate (HA) and halopredone (HP). Reference steroids, which were given s.c. or locally, dose-dependently inhibited carrageenin-induced foot-pad edema, sodium carboxymethyl cellulose-induced leukocyte migration, cotton pellet granuloma and carrageenin granuloma pouch in rats. Although the inhibitory effects of reference steroids on such inflammations were unrelated to their administration routes, the inhibitory potency decreased in the following order: TA greater than MPA greater than HA = HP. THS-201 even at a dose of 100 mg/kg had no inhibitory effects on such inflammations when given s.c. By contrast, THS-201 given locally had anti-inflammatory actions: the inhibitory potency of THS-201 in chronic models was higher than that of TA, but was lower in the acute models than that of HA. In antigen-induced arthritis in rabbits, the inhibition of swelling of inflamed joints by intra-articular injection of THS-201 (2 mg/joint) persisted more than 30 days, suggesting that the elimination of THS-201 from the injected site was very slow. In contrast to the finding of reference steroids, THS-201 showed no systemic adverse reactions in all experiments. The results, which are in agreement with the findings of labeled THS-201 into arthritic joints, indicate that THS-201 can strongly inhibit recurrence of inflammation as compared with reference steroids tested.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Topical↗
PubMed1986

[Pharmacological studies on proglumetacin maleate, a new non-steroidal anti-inflammatory drug. (3) Damaging effects on the gastrointestinal tract].

Damaging effects on the gastrointestinal tract of proglumetacin maleate (PGM), a new indomethacin (IND) derivative, were examined in comparison with those of IND. Gastric and small intestinal lesions were maximum 4 and 24 hr after a single oral administration of PGM, respectively. Ulcerogenic effects of PGM on the gastric mucosa were approximately 1/7 and 1/10 times as potent as those of IND on a molar ratio 4 hr after single oral dosing to fasting and feeding rats, respectively. PGM was also less active on the small intestinal mucosa 24 hr after single oral dosing. After repeated dosing for 7 days, ulcerogenic effects of PGM were about 1/3 and 1/2 times more potent than those of IND on the gastric and the small intestinal mucosa, respectively. The weak ulcerogenicity of PGM appears to be due to the fact that it has little direct action on the gastrointestinal mucosa. On the other hand, protective effects of PGM on diarrhea induced by arachidonic acid in mice were about 1/2 times as potent as those of IND in both 1 and 4 hr pretreatments. So PGM must have less inhibitory effects on prostaglandin biosynthesis in the intestine than IND. PGM is a safer drug than IND because it has less damaging effect on the gastrointestinal mucosa. Therefore, it may be much more useful for the treatment of chronic inflammatory disorders like rheumatoid arthritis.

Administration, Oral↗
PubMed1986

[Pharmacological studies on proglumetacin maleate, a new non-steroidal anti-inflammatory drug. (1). Anti-inflammatory effects].

Anti-inflammatory effects of proglumetacin maleate (PGM), a new indomethacin (IND) derivative, were compared with those of IND on an equimolar-dose basis. PGM produced a dose-dependent inhibition of vascular permeability and carrageenin edema. These inhibitory effects of PGM were greater when given 4 hr prior to phlogistic agents than when given 1 hr before. Moreover, these effects of PGM were long-acting. Inhibitory effects of PGM on kaolin edema and UV-erythema were slightly less active than those of IND. PGM markedly reduced the leukocyte migration in carrageenin pleurisy. Subacute anti-exudative and anti-granuloma effects of PGM were nearly equal to those of IND. Also, PGM showed strong prophylactic and therapeutic effects on adjuvant arthritis, the model of chronic (immuno-reactive) inflammation. These effects of PGM were superior or equal to those of IND. These pharmacological properties of PGM suggested its potential usefulness in rheumatic and other inflammatory disorders. It was considered that the mode of action of PGM mainly depended on its active metabolite, IND. However, PGM was also active in the case of local administration into the sites of inflammation on rat hind paw edema. Therefore, it seemed that PGM had a different behavior than a so called "prodrug".

Animals↗
PubMed1986

[Pharmacological studies on proglumetacin maleate, a new non-steroidal anti-inflammatory drug. (2). Analgesic and antipyretic effects].

Analgesic and antipyretic effects of proglumetacin maleate (PGM), a new indomethacin (IND) derivative, were investigated in comparison with those of IND on an equimolar-dose basis. The suppression of phenylquinone-induced writhing in mice by PGM was about 0.8 and 2 times as potent as that by IND when given 1 and 4 hr before the phenylquinone injection, respectively. The analgesic activity of PGM in rat silver nitrate arthritis was about 1.5 times more potent than that of IND. PGM was slightly less active in rat adjuvant arthritic pain than IND. On the other hand, PGM provoked a dose-dependent antipyretic effect on the yeast-induced fever in rats within the dose range without affecting the normal body temperature. Furthermore, PGM showed a significant antipyretic effect on LPS-febrile rabbits. Generally, the antipyretic effect of PGM was moderate as compared with that of IND. These analgesic and antipyretic actions of orally administered PGM may be mainly due to its active metabolite, IND. The above results indicate that PGM may be useful for inflammatory diseases associated with pain and/or fever.

Animals↗
PubMed1986

Cytoprotective effects of NC-1300 and omeprazole on Hcl . ethanol-induced gastric lesions in rats.

NC-1300 (10-100 mg/kg), given p.o. at 0.5, 6, 12 or 24 hr before HCl . ethanol, dose-dependently protected the rat gastric mucosa. This protection was observed even when the gastric contents had been removed before application of HCl . ethanol. NC-1300 (30 mg/kg), given i.p., was without effect on lesion formation in a dose which potently inhibited gastric acid secretion in pylorus-ligated rats. pretreatment with indomethacin (5 mg/kg, s.c.) resulted in no reduction in the protection by NC-1300, excluding the possible participation of endogenous prostaglandins in the protective mechanism. N-ethylmaleimide pretreatment (10 mg/kg, s.c.) slightly reduced the protective activity of NC-1300, suggesting the partial participation of endogenous sulfhydryl compounds in the NC-1300 protection. NC-1300 sulfide and mercaptobenzimidazole (compounds obtained after mixing NC-1300 with acidic solution) also dose-dependently protected against HCl . ethanol-induced lesions when given p.o. at 0.5 hr before HCl . ethanol. The protection was significant but was considerably reduced in contrast to NC-1300 when the compounds were given 12 hr beforehand. NC-1300 sulfone had no effect on lesion formation. Omeprazole (10, 30 mg/kg), given p.o., also dose-dependently inhibited HCl . ethanol-induced lesions. However, the duration of protection was shorter than that seen with NC-1300, i.e., the effect disappeared 12 hr later. Thus, NC-1300 has a potent and long-lasting activity on HCl . ethanol-induced gastric lesions. The mechanism by which this occurs remains unknown.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1986

Pharmacological studies on proglumetacin maleate, a new non-steroidal anti-inflammatory drug (4). Mode of action on anti-inflammatory activity.

The possible mechanism of the anti-inflammatory activity of proglumetacin maleate (PGM), a new indomethacin (IND) derivative interacting with arachidonic acid (AA) metabolism, was investigated to elucidate the contributions of PGM itself and its two major metabolites, desproglumideproglumetacin maleate (DPP) and IND. PGM caused much less inhibition of PGE2 formation by sheep seminal vesicle microsomes (IC50 = 310 microM) and TXB2 formation by a washed rabbit platelet suspension (IC50 = 6.3 microM) than IND. DPP also caused less inhibition of cyclooxygenase than IND. Moreover, PGM had less effect on sodium arachidonate (SAA)-induced rat platelet aggregation ex vivo and AA-induced sudden death in rabbits than IND. These results show that PGM has anti-inflammatory activity after its conversion to the active metabolite IND. However, the inhibitory effects of PGM and DPP were as strong as that of IND on SAA- or collagen-induced rabbit platelet aggregation in vitro. These activities are considered to be associated with platelet membrane interaction. Moreover, unlike IND, PGM (IC50 = 1.5 microM) and DPP (IC50 = 16.3 microM) strongly inhibited 5-HETE formation by the cytosol of guinea pig polymorphonuclear leukocytes. This unique activity of PGM on 5-lipoxygenase may contribute to its anti-inflammatory activity.

Animals↗
PubMed1986

[Effects of toluene vapors on signaled bar press shock avoidance performance in rats].

The effects of single exposure to toluene on signaled lever press shock avoidance behavior in rats were tested during and after exposure. The results obtained were as follows: Rats exposed to 125, 250 and 500 ppm toluene showed a decline in conditioned avoidance responses at 20 min exposure as compared to the pre-exposure baseline, although they recovered to almost the same level of performance as that before exposure. Exposure to 1,000 ppm toluene produced an exposure duration related to the increase in the number of total lever presses and the decrease in the effective response rate. The number of total lever presses increased drastically after 2,000 ppm toluene exposure. Effective avoidance response rate decreased to about 70% compared to the pre-test performance. Beginning at 4,000 ppm toluene exposure, the response rate increased, thereafter it gradually decreased and finally slight ataxia was observed. After 4,000 ppm exposure, all of the rats showed signs of excitation such as marked increase in the response rate. Acceleration of the reaction time was remarkably observed after 1,000 and 2,000 ppm exposure. As a whole, in the case of toluene exposure, concentration-related increases in lever presses and decreases in the effective avoidance response rate beginning at 1,000 ppm were observed. Animals showed excitatory response at 1,000 and 2,000 ppm toluene exposure and at other levels such as 4,000 ppm they showed depressive behavior. The effects were closely dependent on toluene concentration and exposure duration.

Animals↗
PubMed1986

[A case of amylase-producing ovarian tumor].

A 51-year-old woman with ovarian carcinoma with hyperamylasemia is reported. She was admitted to Osaka General (JNR) Hospital in July 1982. A cystic tumor was palpated in the pelvis. Serum amylase, mainly the salivary type, in electrophoresis, had increased to 1583 Smith-Roe units/dL, while the pancreas was normal on ultrasonography and CT. Chemotherapy (MFC) was performed, and laparotomy revealed bilateral ovarian tumors. Histologically, they were serous cystadenocarcinoma. Serum and urinary amylase values dropped to the normal range after chemotherapy and surgery, and varied directly with the clinical course. Immunohistochemically, amylase was demonstrated in the tumor tissue by the PAP method. In conclusion, amylase was a useful marker in the diagnosis and follow-up of the present patient.

Amylases↗