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Biomedical subjects

T Ohba

Publications and source records attributed to T Ohba.

At least 127 records · Page 7Linked to original sources
PubMed1987

Effect of 3-[p-(trans-4-aminomethylcyclohexylcarbonyl)phenyl] propionic acid hydrochloride on gastric mucosa directly from the lumen.

The present experiments were designed to determine if the novel anti-ulcer drug 3-[p-(trans-4-aminomethylcyclohexylcarbonyl)phenyl]propionic acid hydrochloride (TEI-5103, TG-51), acts on the gastric mucosa directly from the lumen when given orally. TEI-5103 given orally (50-400 mg/kg) prevented the lesion formation induced by 0.1N HCl + 60% ethanol, but when given intraperitoneally (50-200 mg/kg) or intravenously (40 mg/kg), it did not prevent the formation of lesions. Indomethacin-induced gastric lesions were inhibited by oral administration of TEI-5103, but not by intraduodenal administration. In pylorus-ligated rats, TEI-5103 given intragastrically also inhibited the development of gastric lesions induced by HCl + ethanol. These results suggest that the presence of TEI-5103 in the stomach is necessary to elicit its anti-ulcer effect. In microautoradiographic examination, silver grains corresponding to [14C]-TEI-5103 distributed in the upper part of the mucosa (luminal side) at 0.5 to 4 h after the oral administration. However, when given intraduodenally or intravenously, this high concentration of [14C]-TEI-5103 was not observed in the stomach tissue. When given orally, the content of [14C]-TEI-5103 in rat stomach tissue was about 100 times higher than that in plasma and the time course of distribution was different from that seen in the gastric content. From these results, it seems that TEI-5103 distributes in the gastric mucosa directly from the lumen. In conclusion, TEI-5103, when given orally, distributes in the gastric mucosa as a target issue directly from the lumen; and only the oral and gastric route of administration lead to the anti-ulcer effect.

Administration, Oral↗
PubMed1986

Antitumor activity of alkylesters of 5-fluoro-2'-deoxyuridine 5'-monophosphate (FdUMP) against murine lymphoma L5178Y resistant to 5-fluoro-2'-deoxyuridine.

A series of twenty six 5'-substituted FdUMP (5-fluoro-2'-deoxyuridine 5'-monophosphate) have been evaluated for their inhibitory effects on the proliferation of murine lymphoma L5178Y cells sensitive or resistant to FUdR (5-fluoro-2'-deoxyuridine). 5'-Octylphenylene-FdUMP was the most active among these active derivatives against the parent cell line (L5178Y/P). Several other FdUMP derivatives also proved as potent as FUdR in their antiproliferating activity on the L5178Y/P cell line. Activity of these derivatives was decreased considerably by a substituent with a long aliphatic chain and the introduction of acyl groups on the C-3' position. Eicosyl-FdUMP was found to show no or low cross-resistance on the L5178Y/FUdR subline which was about 19 000-fold resistant to FUdR compared with the parent cell line. This derivative might penetrate cell membrane in an intact form and be converted into FdUMP by a phosphodiesterase inside the cell, because an anabolic enzyme, deoxyuridine kinase, was defective in cells of the L5178Y/FUdR subline. The derivatives were promising as antitumor agents for the treatment of relapsed patients following 5-fluorouracil therapy.

Animals↗
PubMed1986

[Effect of atenolol on MAO activities in SHR].

The effects of atenolol on monoamine oxidase (MAO) activities in the heart, liver, kidney and mesenteric artery in spontaneously hypertensive rats (SHR) were studied. Male SHR (5-weeks-old) were given 20 and 100 mg/kg/day of atenolol by gavage for 10 weeks. The MAO activities were determined once every 2 weeks. Atenolol produced a hypotensive effect and bradycardia in SHR. The heart weight/body weight ratio in SHR was suppressed from 4 weeks of atenolol treatment. Though atenolol induced MAO activities in the 2 weeks treated heart and 4-6 weeks treated liver, it inhibited the increase of MAO activities in all prepared organs after 10 weeks treatment. The MAO activities of the heart were more markedly inhibited than in the other organs by the treatment of atenolol. Atenolol did not lower the Km value, but reduced significantly the Vmax value of the 10 weeks treated heart MAO. Atenolol had no effect on the MAO activities in vitro. These results suggest that the changes of the MAO activities in the organs of SHR by the treatment of atenolol may be relative to the hypotensive and bradycardic effects of the cardioselective beta-adrenoceptor blocking agent.

Animals↗
PubMed1986

The deoxygenations of tosylated adenosine derivatives with Grignard reagents.

The reactions of 2'-O- or 3'-O-tosylated adenosines with Grignard reagents resulted in the formation of various products, which were deoxy or branched-chain deoxy sugar nucleosides, 1',2'-unsaturated nucleosides, 3'-deoxy-2'-keto sugar nucleosides, and so on. The convenient method for the synthesis of the 3'-deoxy-2'-keto adenine nucleoside is described.

Adenosine↗
PubMed1985

[Effect of nicardipine on cholesterol-fed S.H.R].

The effect of nicardipine on experimental hyperlipemia induced by a 1% cholesterol diet in spontaneously hypertensive rats (SHR) was investigated by the change of hemodynamics and the determination of lipid contents of the serum, liver, heart and aorta. Nicardipine increased liver weight and liver weight per body weight ratio, and it decreased heart and kidney weight significantly. Nicardipine inhibited the increase in blood pressure with cholesterol and normal diets. Nicardipine decreased heart rate in SHR fed the normal diet, and it inhibited the increase in heart rate in SHR fed the cholesterol diet. Serum lipid levels significantly increased with the cholesterol diet. Nicardipine significantly increased cholesterol in high density lipoprotein (HDL-C) and phospholipid in HDL (HDL-PL) with cholesterol and normal diets, and it decreased triglyceride and improved the atherogenic index "(total cholesterol-HDL-C)/HDL-C" with the normal diet. Serum GOT and GPT significantly increased with the cholesterol diet. Nicardipine significantly enhanced an increase in GOT and GPT levels with the cholesterol diet. Nicardipine increased phospholipid content in the liver, triglyceride in the heart, and it decreased total cholesterol in the aorta. A morphologic study showed a fatty liver in SHR fed the cholesterol diet, but nicardipine had no effect on the morphological changes in the liver, heart and aorta. These results suggest that nicardipine may prevent atherosclerotic degeneration by the inhibition of hypertension, increase in serum HDL and decrease in total cholesterol in the aorta.

Animals↗
PubMed1984

Computed tomography of renal metastases.

The CT manifestations of renal metastases from nonurinary tract carcinomas were evaluated in five autopsy-proven cases. Three cases resembled renal inflammatory disease or renal cysts. The wide variety of CT manifestations of renal metastases underscores the need to bear renal metastases in mind when renal abnormalities are observed in any case of advanced malignancy.

Adenocarcinoma↗
PubMed1980

Postoperative maxillary cyst.

The postoperative maxillary cyst develops in the maxillary sinus between the ages of 30 and 40 in persons who received sinus surgery 10 to 20 years earlier. Etiology of the cystic lesion appears to be derived from the infected sinus mucosa left after a sinus operation. Chief complaints of postoperative maxillary cysts are swelling or pain in the buccal region, discomfort of the maxilla or maxillary teeth and exophthalmos. Characteristic panoramic radiographic findings of the postoperative maxillary cyst are a monolocular cystic radiolucency with a well-defined margin and surrounding sclerotic bone in the floor of the maxillary sinus.

Adult↗