We have investigated the effect of a novel anti-rheumatic drug, cis-2-(4-chlorophenyl)-4,5-diphenyl-2-imidazoline hydrochloride (TA-383), on macrophages. TA-383 (> or = 10(-9) M) significantly stimulated rabbit alveolar macrophage (AM) migration, and its migration-stimulatory activity was more potent than those of L-fucose (5 x 10(-3) M), lobenzarit disodium, bucillamine (SA-96) and salazosulfapyridine. In addition, TA-383 enhanced the production and/or release of macrophage migration enhancement factor by rabbit spleen cells. In vivo, TA-383 (0.4 mg/kg, p.o.) has suppressive effects on picryl chloride-induced delayed type hypersensitivity and type II collagen-induced arthritis in mice. These results suggest that the anti-rheumatic activity of TA-383 may be exerted through the dispersion of macrophages from inflammatory sites.

1995-07-01·International Journal of Immunopharmacology

Effect of a novel anti-rheumatic drug, TA-383, on type II collagen-induced arthritis

Article

作者: Masakazu Takeshita ; Kazunori Imaizumi ; Takahisa Sugita ; Isao Takata ; Makoto Ueno

The effects of Ta-383 (0.016, 0.08, 0.4, 2 and 10 mg/kg) and anti-rheumatic drugs (lobenzarit 10 and 50 mg/kg, dexamethasone 0.25 mg/kg) were evaluated on type II collagen-induced arthritis in DBA/1J mice. The arthritis score was markedly suppressed in the groups treated with dexamethasone and TA-383. Serum anti-type II collagen IgG was significantly suppressed in the groups treated with dexamethasone and 0.4 mg/kg TA-383. Histopathological evaluation of the knee joints revealed suppression of the inflammatory changes in the groups treated with dexamethasone and TA-383. These findings suggest that the histopathological examination of the joints of the animal model is useful for the evaluation of anti-rheumatic drugs, and that TA-383 has suppressive effects on type II collagen-induced arthritis, an animal model for human rheumatoid arthritis.

1993-05-01·International Journal of Immunopharmacology

Effect of a novel anti-rheumatic drug, TA-383, on type II collagen-induced arthritis — Suppressive effect of TA-383 on interleukin 6 production

Article

作者: Takanori Murakami ; Makoto Ueno ; Tetsuya Tosa ; Isao Takata ; Osamu Furukawa ; Takahisa Sugita

We have evaluated the effect of a novel anti-rheumatic drug, cis-2-(4-chlorophenyl)-4,5-diphenyl-2-imidazoline hydrochloride (TA-383), on type II collagen (CII)-induced arthritis in DBA/1J mice. Treatment with TA-383 (0.4 mg/kg/day) from the day of immunization with CII strongly suppressed the arthritic responses. Increased serum interleukin 6 (IL-6) level was lowered in parallel with the effect. Effect of TA-383 on IL-6 production was examined in vitro. TA-383 inhibited the production of IL-6 by murine synovial fibroblasts stimulated with recombinant interleukin 1 (IL-1) beta in a dose-dependent manner (0.1-10 microM). Neither the general protein synthesis nor the expression of type I IL-1 receptor was affected by TA-383. The results show that TA-383 possesses an inhibitory activity on IL-6 generation and suggest that the effect may partly contribute to the anti-arthritic effect of TA-383.

100 项与 TA-383 相关的药物交易

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