Effects of mepirizole and basic antiinflammatory drugs on HCl-ethanol-induced gastric lesions in rats.
Tanaka H, Nakagawa M, Takeuchi K, Okabe S.SourceDepartment of Applied Pharmacology, Kyoto Pharmaceutical University, Japan.
Digestive diseases and sciences.Dig Dis Sci.1989 Feb;34(2):238-45.
Mepirozole, a basic antiinflammatory drug and duodenal ulcerogen in laboratory animals, macroscopically protected the gastric mucosa of rats from HCl-ethanol-induced damage in a dose-dependent manner. These effects were evident when the agent was given orally, intraperitoneally, or subcutaneously at
Shimada O, Yasuda H.AbstractRadical scavenging action of tinoridine, a non-steroidal anti-inflammatory drug with a potent anti-peroxidative activity, was investigated. Tinoridine reduced a stable free radical, diphenyl-p-picryl-hydrazyl, in the molar ratio of about 1:2, indicating its free radical scavenging ability. Tinoridine inhibited the lipid peroxidation in rat liver microsomes induced by xanthine-xanthine oxidase system in the presence of ADP and Fe2+, in which hydroxyl radical (. OH) is formed. Tinoridine was demonstrated to be oxidized in the course of the lipid peroxidation by following the fluorescence derived from the oxidation product of tinoridine. It was also oxidized by the xanthine-xanthine oxidase system in the presence of Fe2+, but its oxidation was slow in the absence of Fe2+ and almost completely inhibited by catalase. Tinoridine was also oxidized by H2O2-Fe2+ system producing . OH (Fenton reaction), but it did not affect the reduction of cytochrome c caused by superoxide radical. These results indicate that tinoridine is able to scavenge . OH and the main active oxygen species responsible for the lipid peroxidation is . OH. The anti-peroxidative and . OH scavenging ability of tinoridine should contribute to its anti-inflammatory action.
Agents and actions.Agents Actions.1986 Nov;19(3-4):208-14.
Radical scavenging action of tinoridine, a non-steroidal anti-inflammatory drug with a potent anti-peroxidative activity, was investigated. Tinoridine reduced a stable free radical, diphenyl-p-picryl-hydrazyl, in the molar ratio of about 1:2, indicating its free radical scavenging ability. Tinoridin
Protection against hepatic injury by a novel spiropiperidine derivative.
Yasuda H, Izumi N, Shimada O, Maruyama Y, Kobayakawa T.AbstractThe evaluation of a novel hepatoprotective agent, Y-8845 (8(2-dimethylaminoethyl)-3-oxo-4-phenyl-1-thia-4,8-diazaspiro [4,5]decane dihydrochloride monohydrate), against carbon tetrachloride (CCl4)- and endotoxin-induced acute and chronic hepatic injury was carried out in rats. This compound, in a dose-dependent way, markedly reduced the increases in serum transaminase activities, the extent of liver cell necrosis, and the delay in indocyanine green (ICG) disappearance produced by a single toxic dosage of CCl4. This protective effect was observed even at doses of Y-8845 lower than 10 mg/kg po. It was also shown to protect the liver against injury induced by endotoxin. Furthermore, in the chronic liver injury induced by repeated administrations of CCl4 for 12 weeks, significant reductions of the increases in serum enzyme activities, liver fibrosis, and liver enlargement, and improvement in the ICG retention rate, were recognized in the Y-8845-treated groups at 10 mg/kg po or less. These findings indicate that this new agent has a remarkable protective effect, and possibly a therapeutic effect on liver injury.
Toxicology and applied pharmacology.Toxicol Appl Pharmacol.1986 Sep 30;85(3):398-406.
The evaluation of a novel hepatoprotective agent, Y-8845 (8(2-dimethylaminoethyl)-3-oxo-4-phenyl-1-thia-4,8-diazaspiro [4,5]decane dihydrochloride monohydrate), against carbon tetrachloride (CCl4)- and endotoxin-induced acute and chronic hepatic injury was carried out in rats. This compound, in a do
Journal of pharmacobio-dynamics 8(7), 532-538, 1985-07
… This study was carried out to investigate the effect of tinoridine (2-amino-3-ethoxycarbonyl-6-benzyl-4,5,6,7-tetrahydrothieno [2,3-c] pyridine), a non-steroidal antiinflammatory drug, on the lipid peroxidation and renin release in the renin granule fraction. … When the renin granule fraction was incubated with 50 μM tinoridine at 37℃, lipid peroxide formation in this fraction was completely inhibited. …
Journal of Pharmacobio-Dynamics 8(7), 532-538, 1985
… This study was carried out to investigate the effect of tinoridine (2-amino-3-ethoxycarbonyl-6-benzyl-4, 5, 6, 7-tetrahydrothieno [2, 3-c] pyridine), a non-steroidal antiinflammatory drug, on the lipid peroxidation and renin release in the renin granule fraction. … When the renin granule fraction was incubated with 50 μM tinoridine at 37°C, lipid peroxide formation in this fraction was completely inhibited. …
The purpose of this study is to confirm the efficacy of tinoridine hydrochloride ( HCL), three times daily (TID), in the treatment of pain and inflammation in patients with acute tonsillitis and/or acute pharyngitis of nonbacterial origin versus placebo ...