[The antigastric ulcer activity of succinic acid mono-3-guaiazulenamide (TPH-3) (author's transl)].

Abstract

Effects of TPH-3 on various experimental gastric ulcers in rats and guinea-pigs were studied and the following results were obtained. In the preventive experiments, such as the Shay's ulcer, pylorus-ligated aspirin ulcer and restraint and water immersion stress ulcer, TPH-3 (200 mg/kg i.d. or p.o.) showed a statistically significant inhibition. TPH-3 markedly inhibited the histamine-induced gastric ulcer in guinea-pigs and a dose-response relationship was obtained for doses of 12.5, 25 and 50 mg/kg p.o. TPH-3 showed the weak inhibition regarding therapy for serosa-seared gastric ulcer and the recovery process of restraint and water immersion stress ulcer in rats. TPH-3, dosing 100 mg/kg intraduodenally, significantly inhibited the gastric secretion in the pylorus-ligated rats. TPH-3 significantly inhibited the histamine, pentagastrin and carbachol-induced acid secretion in the stomach-perfused rats. In particular, TPH-3 showed strong sensitivity to the action of histamine. TPH-3 had no anti-ACh or anti-H1-receptor effects.

• Authors: K Kojima, K Iwano, H Nishimura, A Yoshimura, H Okuda, Y Suzuki
• Journal: Nihon yakurigaku zasshi. Folia pharmacologica Japonica (Nihon Yakurigaku Zasshi) Vol. 79 Issue 1 Pg. 23-32 (Jan 1982) ISSN: 0015-5691 [Print] Japan
• PMID: 7061024 (Publication Type: Journal Article)

Chemical References

• Anti-Ulcer Agents
• Azulenes
• Histamine Antagonists
• Sesquiterpenes
• succinic acid mono-3-guaiazulenamide

Topics

• Animals
• Anti-Ulcer Agents
• Azulenes
• Depression, Chemical
• Gastric Juice (metabolism)
• Gastrointestinal Motility (drug effects)
• Guinea Pigs
• Histamine Antagonists
• In Vitro Techniques
• Intestines (drug effects)
• Ligation
• Male
• Muscle Contraction (drug effects)
• Muscle, Smooth (drug effects)
• Pyloric Antrum
• Rats
• Rats, Inbred Strains
• Sesquiterpenes (pharmacology)
• Stomach Ulcer (prevention & control)