Anti-inflammatory and immunomodulating effects of the novel agent gamma-(2-aminoethylamino)-2-butyrothienone. 1st communication: inhibitory effects on mouse paw edema.

A series of 4-hydroxy-(or-amino)-ethyl-amino butyrophenones or butyrothienones were synthesized. For detail studies on antiinflammatory effects, gamma-(2-aminoethylamino)-2-butyrothienone (gamma-ABT) was chosen as representative of these new non-steroidal anti-inflammatories (NSAID). The effect on mouse paw edema induced by various phlogistic agents was first investigated. The inhibitory effect of gamma-ABT on carrageenin-induced edema was remarkable and nearly equal to that of indometacin. Similarly to indometacin, gamma-ABT inhibited the early and late stage of yeast-induced edema in contrast to concanavalin A (Con A) induced edema which was only inhibited by gamma-ABT. Both the above induced edema are supposed to be unrelated to prostaglandins in the rat system. gamma-ABT displayed an inhibitory effect on nystatin-induced edema similar to indometacin suggesting that gamma-ABT has significant membrane stabilizing action and a strong blocking action on synthesis of prostaglandins. gamma-ABT inhibited as well the sustained edema induced by mustard. In conclusion gamma-ABT is an effective agent not only on acute but also on subacute and chronic inflammation and its mode of action appears similar to other NSAID. gamma-ABT posses in addition the advantage of antioxidant activity which is not shared by selective cyclooxygenase inhibitors and thus should be potentially effective in autoimmune diseases.
AuthorsA Gavalas, L Kourounakis, D Litina, P Kourounakis
JournalArzneimittel-Forschung (Arzneimittelforschung) Vol. 41 Issue 4 Pg. 423-6 (Apr 1991) ISSN: 0004-4172 [Print] GERMANY
PMID1859517 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Anti-Inflammatory Agents, Non-Steroidal
  • Plant Lectins
  • Thiophenes
  • Concanavalin A
  • gamma-(2-aminoethylamino)-2-butryothienone
  • Nystatin
  • Carrageenan
  • Indomethacin
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal (pharmacology)
  • Carrageenan
  • Concanavalin A
  • Edema (chemically induced, drug therapy, pathology)
  • Female
  • Foot (pathology)
  • Indomethacin (pharmacology)
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Inbred Strains
  • Mustard Plant
  • Nystatin
  • Plant Lectins
  • Plants, Medicinal
  • Thiophenes (pharmacology)
  • Yeasts

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