The novel anti-rheumatic drug TA-383 has a macrophage migration enhancing activity.
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.
Ueno
M
M
Lead Generation Research Laboratory, Tanabe Seiyaku Co., Ltd., Osaka, Japan.
Sugita
T
T
Murakami
T
T
Takata
I
I
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology* / Q000627:therapeutic use; D016918:Arthritis, Reactive / Q000139:chemically induced / Q000188:drug therapy; D002465:Cell Movement / Q000187:drug effects; D002630:Chemotactic Factors / Q000494:pharmacology*; D003094:Collagen / Q000009:adverse effects; D003545:Cysteine / Q000031:analogs & derivatives / Q000494:pharmacology; D006968:Hypersensitivity, Delayed / Q000139:chemically induced / Q000188:drug therapy; D007093:Imidazoles / Q000494:pharmacology* / Q000627:therapeutic use; D066298:In Vitro Techniques; D016676:Macrophages, Alveolar / Q000187:drug effects*; D051379:Mice; D008811:Mice, Inbred DBA; D010853:Picryl Chloride / Q000009:adverse effects; D011817:Rabbits; D012460:Sulfasalazine / Q000494:pharmacology; D062367:ortho-Aminobenzoates / Q000494:pharmacology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002630:Chemotactic Factors; D007093:Imidazoles; C053609:macrophage migration enhancement factor; D062367:ortho-Aminobenzoates; C083037:2-(4-chlorophenyl)-4,5-diphenyl-2-imidazoline hydrochloride; D012460:Sulfasalazine; D003094:Collagen; C015735:lobenzarit; D003545:Cysteine; C026535:bucillamine; D010853:Picryl Chloride