Analgesic and anti-inflammatory activity of 6-chloro-alpha-methyl-carbazole-2-acetic acid (C-5720).
The carbazole, C-5720, has the same order of analgesic, antipyretic and anti-inflammatory activity as indomethacin and is more potent than phenylbutazone and acetylsalicylic acid in the yeast inflamed paw, the carrageenin foot edema, the Mycobacterium butyricum-induced pyrexia, and the acute and chronic adjuvant arthritis tests. In chronic adjuvant arthritis in rats, C-5720 lowers the elevated serum mucopolysaccharide and plasma fibrinogen levels, and partially restores the depressed liver N-demethylase activity. C-5720 is 16 times less active than indomethacin in the production of gastric ulcers in rats and is about 70 times less active than indomethacin in blocking arachidonic acid-induced diarrhea in mice. C-5720 has a greater safety margin than indomethacin with respect to the production of gastric ulcers or the blockade of diarrhea and the reduction of inflammation in adjuvant-induced polyarthritis.
D000700:Analgesics / Q000627:therapeutic use; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000627:therapeutic use; D001095:Arachidonic Acids / Q000037:antagonists & inhibitors; D001172:Arthritis, Rheumatoid / Q000188:drug therapy; D001522:Behavior, Animal / Q000187:drug effects; D002227:Carbazoles / Q000494:pharmacology*; D003967:Diarrhea / Q000188:drug therapy; D004487:Edema / Q000188:drug therapy; D005340:Fibrinogen / Q000378:metabolism; D006025:Glycosaminoglycans / Q000097:blood; D008099:Liver / Q000201:enzymology; D008297:Male; D051379:Mice; D010089:Oxidoreductases, N-Demethylating / Q000378:metabolism; D011809:Quinones / Q000037:antagonists & inhibitors; D051381:Rats; D011930:Reaction Time / Q000187:drug effects; D013276:Stomach Ulcer / Q000139:chemically induced
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D001095:Arachidonic Acids; D002227:Carbazoles; D006025:Glycosaminoglycans; D011809:Quinones; D005340:Fibrinogen; D010089:Oxidoreductases, N-Demethylating