[Pharmacological study of 9 alpha-fluoro-11 beta, 17, 21-trihydroxy-16 beta-methylpregna-1, 4-diene-3,20-dione-17-benzoate (betamethasone-17-benzoate, MS-1112), a local anti-inflammatory agent. (1). Its anti-inflammatory and other pharmacological properties].
The anti-inflammatory activity and the other pharmacological properties of MS-1112, a new steroid compound, were examined and compared with other glucocorticoid analogues such as hydrocortisone acetate (Hydr), betamethasone 17-valerate (Val) and dexamethasone (Dexa). Systemically administered MS-1112 and glucocorticoids had a significant effect in inhibiting rat paw edema induced by various phlogistic stimulations and increasing vascular permeabilities and granuloma formation by cotton pellet or granuloma pouch. The order of those inhibiting activity was, in general, Dexa greater than MS-1112 greater than Val greater than Hydr. Concomitantly, Xthymolysis and adrenal weight suppression and reduced rate of body weight gain after multiple systemical administration were also observed. Locally administered MS-1112 caused an inhibiting activity, without systemic side-effects. This activity was approximately 3 to 5 times more potent than that of Dexa in rat carrageenin paw edema and cotton pellet granuloma. MS-1112 was less active than Dexa in glycogen liver deposition activity and in the depression of plasma level of corticosterone but more active than Val and Hydr. In the dose administered, MS-1112 had neither androgenic and anabolic nor estrogenic and anti-estrogenic activity. From this data, it concluded that MS-1112 is a very potent agent applicable regarding permeability and retention of steroids in a local site.
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents; D001565:Benzoates; D001623:Betamethasone / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D001786:Blood Glucose / Q000378:metabolism; D002199:Capillary Permeability / Q000187:drug effects; D003907:Dexamethasone / Q000494:pharmacology; D004487:Edema / Q000188:drug therapy; D004573:Electrolytes / Q000652:urine; D005260:Female; D005837:Genitalia, Male / Q000187:drug effects; D006099:Granuloma / Q000188:drug therapy; D006854:Hydrocortisone / Q000494:pharmacology; D008055:Lipids / Q000097:blood; D008112:Liver Glycogen / Q000378:metabolism; D008297:Male; D051379:Mice; D010913:Pituitary-Adrenal System / Q000187:drug effects; D051381:Rats; D013448:Sulfobromophthalein; D014599:Uterus / Q000187:drug effects; D014945:Wound Healing / Q000187:drug effects
D000893:Anti-Inflammatory Agents; D001565:Benzoates; D001786:Blood Glucose; D004573:Electrolytes; D008055:Lipids; D008112:Liver Glycogen; D013448:Sulfobromophthalein; D003907:Dexamethasone; D001623:Betamethasone; D006854:Hydrocortisone