[The antigastric ulcer activity of succinic acid mono-3-guaiazulenamide (TPH-3) (author's transl)].
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.
D000818:Animals; D000897:Anti-Ulcer Agents; D052176:Azulenes; D003864:Depression, Chemical; D005750:Gastric Juice / Q000378:metabolism; D005769:Gastrointestinal Motility / Q000187:drug effects; D006168:Guinea Pigs; D006633:Histamine Antagonists; D066298:In Vitro Techniques; D007422:Intestines / Q000187:drug effects; D008026:Ligation; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D011706:Pyloric Antrum; D051381:Rats; D011919:Rats, Inbred Strains; D012717:Sesquiterpenes / Q000494:pharmacology*; D013276:Stomach Ulcer / Q000517:prevention & control*
D000897:Anti-Ulcer Agents; D052176:Azulenes; D006633:Histamine Antagonists; D012717:Sesquiterpenes; C033777:succinic acid mono-3-guaiazulenamide