Pharmacological study in vivo of the new topical anti-inflammatory steroid 21-thiol-9 alpha-fluoro-11 beta,17 alpha-dihydroxy-16 alpha-methyl-3,20-dione-21-acetylamino cysteine.
The pharmacological evaluation, using animal models, of 21-thiol-9 alpha-fluoro-11 beta, 17 alpha-dihydroxy-16 alpha-methyl-3,20-dione- 21-acetylamino cysteine (CMJ), a new steroidal anti-inflammatory compound, is reported. The results obtained show a significant anti-inflammatory activity for CMJ. Comparison with dexamethasone indicates that CMJ is about 9 to 10 times less active in vivo. Of particular interest, however, is the dissociation of local and systemic activities of CMJ, since this compound was shown to be practically devoid of systemic activity (about 970 times less active than dexamethasone) after subcutaneous administration in rats. It is therefore expected that the topical use of CMJ in therapy may not cause the side effects provoked by many of the corticosteroids currently used.
Milioni
C
C
Laboratoire de Pharmacie Chimique, Faculté de Pharmacie, Illkirch, France.
Jung
L
L
Lauressergues
H
H
D000038:Abscess / Q000517:prevention & control; D000287:Administration, Topical; D000305:Adrenal Cortex Hormones / Q000494:pharmacology*; D000311:Adrenal Glands / Q000187:drug effects; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D002351:Carrageenan; D003545:Cysteine / Q000031:analogs & derivatives* / Q000494:pharmacology; D003907:Dexamethasone / Q000494:pharmacology; D003368:Gossypium; D006099:Granuloma / Q000139:chemically induced / Q000517:prevention & control; D008297:Male; D051381:Rats; D013950:Thymus Gland / Q000187:drug effects
D000305:Adrenal Cortex Hormones; D000893:Anti-Inflammatory Agents; D003907:Dexamethasone; D002351:Carrageenan; D003545:Cysteine