Antiinflammatory properties of E5090, a novel orally active inhibitor of IL-1 generation.
E5090 is a novel orally active inhibitor of IL-1 generation without cyclooxygenase-inhibiting activity. The effects of E5090 on several inflammatory animal models were investigated in rats. In adjuvant arthritis, E5090 suppressed both the paw swelling and the enhancements of ESR and number of peripheral blood leucocytes, like the steroidal antiinflammatory drug prednisolone. However, the thymus was not withered by E5090 though it was by prednisolone. In type II collagen-induced arthritis, E5090 inhibited paw swelling and joint destruction. E5090 was effective in acute inflammatory models such as carrageenin-induced paw edema, and adjuvant-induced local hyperthermia, and also showed analgesic effects against inflammatory pain and antipyretic effects. The results suggest that this orally active inhibitor of IL-1 generation, E5090, may be a therapeutically useful antiinflammatory drug with a novel mechanism of action.
Shirota
H
H
Eisai Tsukuba Research Laboratories, Ibaraki, Japan.
Chiba
K
K
Goto
M
M
Hashida
R
R
Ono
H
H
D000179:Acrylates / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D001169:Arthritis, Experimental / Q000188:drug therapy / Q000473:pathology; D003094:Collagen; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy / Q000473:pathology; D005334:Fever / Q000139:chemically induced / Q000188:drug therapy; D007213:Indomethacin / Q000627:therapeutic use; D007375:Interleukin-1 / Q000096:biosynthesis*; D008297:Male; D009284:Naphthols / Q000494:pharmacology*; D010998:Pleurisy / Q000139:chemically induced / Q000188:drug therapy; D011239:Prednisolone / Q000627:therapeutic use; D051381:Rats; D011916:Rats, Inbred F344; D011919:Rats, Inbred Strains
D000179:Acrylates; D000894:Anti-Inflammatory Agents, Non-Steroidal; D007375:Interleukin-1; D009284:Naphthols; C069676:E 5090; D003094:Collagen; D011239:Prednisolone; D007213:Indomethacin