Vasoconstrictor activities of some novel synthetic steroids in alcoholic solution.
Ethanolic solutions of 8 new, topically active, anti-inflammatory steroids and 1 standard (betamethasone 17-valerate) were assessed with a modified vascoconstrictor assay. Pallor was graded at 17 reading times for determination of complete blanching curves. The compounds were ranked by three methods: (1) summed % total possible score, (2) area under the blanching profile, and (3) square root transformation of sum of scores divided by number of volunteers, for statistical differentiation of the solutions. Conclusions on structure-vasoconstrictor activity relationships were that substitution or removal of 21 hydroxy provided compounds with a wide range of activity. Poor activity correlated with a hemisuccinate salt grouping at position 21, or the absence of 11beta-hydroxy.
D000287:Administration, Topical; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000494:pharmacology*; D001623:Betamethasone / Q000031:analogs & derivatives / Q000494:pharmacology; D002855:Chromatography, Thin Layer; D003201:Computers; D004305:Dose-Response Relationship, Drug; D000431:Ethanol; D005938:Glucocorticoids; D006801:Humans; D007249:Inflammation / Q000188:drug therapy; D012867:Skin / Q000098:blood supply; D012996:Solutions; D013056:Spectrophotometry, Ultraviolet; D013259:Steroids, Fluorinated / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014662:Vasoconstrictor Agents
D000893:Anti-Inflammatory Agents; D005938:Glucocorticoids; D012996:Solutions; D013259:Steroids, Fluorinated; D014662:Vasoconstrictor Agents; D000431:Ethanol; D001623:Betamethasone