21-Methyl-20,21-diketocorticosteroid類の抗炎症作用(第2報)11β, 17α-Dihydroxy-21-methylpregna-1,4-diene-3,20,21-trione 17-Acetate(TSC-5)の抗炎症作用

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A new steroid, 11β, 17α-dihydroxy-21-methylpregna-1,4-diene-3,20,21-trione 17-acetate (TSC-5) was tested for its inhibitory effect on acute, subacute and chronic inflammation by systemic administration (p.o. and s.c.) or local application, as well as its glucocorticoid effects in experimental animals. TSC-5 showed potent anti-inflammatory activities comparable to those of prednisolone in acute and subacute inflammation models, but its inhibitory effect on chronic inflammation was less than that of prednisolone in rats. Unlike prednisolone, TSC-5 was found to have local anti-inflammatory activity in rats, where TSC-5 was one half as active as prednisolone 21-tert-butylacetate. TSC-5 was 1/12 as active as prednisolone in glycogendeposition activity by s.c. administration. The inhibitory effect of TSC-5 on antibody formation in mice by s.c. and p.o. administrations was less potent than that of prednisolone. TSC-5 was less potent than prednisolone in thymus-involution effect, but the adrenalinvolution effects of both compounds were almost the same in rats. Thus, TSC-5 showed a significant gap between anti-inflammatory and glucocorticoid activities.
社団法人日本薬学会の論文
1979-09-25