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[The modes of anti-inflammatory and analgesic actions of 2-[4-(3-methyl-2-butenyl) phenyl] propionic acid (TA-60) and 2-[4-(2,2-dichlorovinyl) phenyl] propionic acid (TA-668) and effect of TA-60 on the gastrointestinal tract].

Abstract
TA-668 and TA-60, potent anti-inflammatory compounds, showed no inhibition against the dextran-, the serotonin- and the carrageenin + prostaglandin E2 (PGE2)-induced hind paw edemas in rats and neither did typical acidic non-steroidal anti-inflammatory drugs (ANSAIDs) such as indomethacin. On the other hand, salicylic acid, mepirizole and tiaramide X HCl inhibited the hind paw edema induced by carrageenin + PGE2 in rats. TA-668 and TA-60 as well as other ANSAIDs inhibited the arachidonic acid (AA)-induced erythema, but did not inhibit the PGE2-induced erythema. Mepirizole and tiaramide X HCl showed no inhibition against both the AA- and the PGE2-induced erythemas. TA-668 and TA-60 showed analgesic activities in the adjuvant-induced hind paw edematous rats. The analgesic activities of these compounds disappeared when PGE2 was injected into the inflamed paw as well as indomethacin and ibuprofen. It is concluded that anti-inflammatory and analgesic activities of both TA-668 and TA-60 were based on the inhibition of cyclo-oxygenase. TA-60 showed a protective effect against gastric necrosis induced by necrotizing agents such as HCl, NaOH or NaOH + EtOH. TA-60 showed about a 4 times less potent activity than ibuprofen in delay of occurring time of castor oil-induced diarrhea in rats. These results suggest that the slight ulcerating effect of TA-60 on the gastrointestinal tract might be attributed to its gastric protective effect and slight decreasing effect on the gastrointestinal level of PGE2.
AuthorsS Higuchi, Y Shioiri, N Tanaka, S Otomo, H Aihara
JournalNihon yakurigaku zasshi. Folia pharmacologica Japonica (Nihon Yakurigaku Zasshi) Vol. 86 Issue 6 Pg. 417-23 (Dec 1985) ISSN: 0015-5691 [Print] Japan
PMID3879231 (Publication Type: Comparative Study, English Abstract, Journal Article)
Chemical References
  • Anti-Inflammatory Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Benzothiazoles
  • Phenylpropionates
  • Piperazines
  • Epirizole
  • 2-(4-(3-methyl-2-butenyl)phenyl)propionic acid
  • 2-(4-(2,2-dichlorovinyl)phenyl)propionic acid
  • tiaramide
  • Ibuprofen
  • Indomethacin
Topics
  • Animals
  • Anti-Inflammatory Agents (pharmacology)
  • Anti-Inflammatory Agents, Non-Steroidal (pharmacology)
  • Benzothiazoles
  • Diarrhea (prevention & control)
  • Epirizole (pharmacology)
  • Guinea Pigs
  • Ibuprofen (pharmacology)
  • Indomethacin (pharmacology)
  • Intestinal Mucosa (drug effects)
  • Male
  • Necrosis
  • Phenylpropionates (pharmacology)
  • Piperazines (pharmacology)
  • Rats
  • Stomach Diseases (prevention & control)

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