[Pharmacological study on 9 alpha-fluoro-11 beta, 17,21-trihydroxy-16 beta-methyl pregna-1, 4-diene-3,20-dione-17-benzoate(betamethasone-17-benzoate, MS-1112), a local anti-inflammatory agent. (2). Its action of delayed hypersensitivity dermatitis].
The anti-inflammatory activity of MS-1112, a new steroid compound, after topical application and systemical administration was examined by means of delayed-type hypersensitivity in mice and compared with other glucocorticoid analogues, betamethasone-17-valerate (Val), dexamethasone (Dexa) and betamethasone (Beta). In the case of pretreatment and therapeutic effect, topically applied MS-1112 was most active in inhibiting the delayed-type hypersensitivity induced by picryl chloride. The order of those inhibitory activities of MS-1112 and Val was ointment greater than cream greater than gel. In contrast to MS-1112 and Val, inhibitory action of Dexa was slow in onset after the topical application. It appears that esterification of the 17-hydroxyl group increases the anti-inflammatory activity after topical application. While systemically administered, MS-1112 was more potent than Val, and similarly potent to Beta, but less active than Dexa. From the above results, it may be considered that topically applied MS-1112 is superior to other glucocorticoids in the percutaneous penetration and retention in the skin. MS-1112 is thus considered to be a very potent agent as a dermatocorticoid.
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000627:therapeutic use*; D001565:Benzoates; D001623:Betamethasone / Q000008:administration & dosage / Q000627:therapeutic use*; D003877:Dermatitis, Contact / Q000188:drug therapy*; D003907:Dexamethasone / Q000627:therapeutic use; D005260:Female; D007279:Injections, Subcutaneous; D008297:Male; D051379:Mice; D009824:Ointments; D014631:Valerates
D000893:Anti-Inflammatory Agents; D001565:Benzoates; D009824:Ointments; D014631:Valerates; D003907:Dexamethasone; D001623:Betamethasone