ANTI-INFLAMMATORY PYRAZOLO-STEROIDS - POTENT GLUCOCORTICOIDS CONTAINING BULKY A-RING SUBSTITUENTS AND NO C3-CARBONYL

被引：56

作者：

SIMONS, SS ^{[1
]}

THOMPSON, EB ^{[1
]}

JOHNSON, DF ^{[1
]}

机构：

[1] NCI,BIOL LAB,BETHESDA,MD 20014

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1979年 / 86卷 / 03期

关键词：

D O I：

10.1016/0006-291X(79)91782-0

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Certain pyrazolo-steroids are extremely potent anti-inflammatory agents but are predicted to be inactive glucocorticoids on the basis of their structure. However, one representative compound is found to possess a high affinity for cytoplasmic glucocorticoid receptors. The biological activity of this steroid is greater than that predicted from its affinity for receptors. This may be due to an exceptionally slow rate of dissociation of the receptorsteroid complex, which would prevent an accurate determination of the equilibrium affinity constant. © 1979.

引用

页码：793 / 800

页数：8

共 23 条

[1]

Bayley H, 1977, Methods Enzymol, V46, P69

[2]

BRAUN VC, 1977, J MED CHEM, V20, P1134

[3]

DAUSSE JP, 1977, MOL PHARMACOL, V13, P948

[4] 16-METHYLATED STEROIDS .4. 6,16ALPHA-DIMETHYL-DELTA6- HYDROCORTISONE AND RELATED COMPOUNDS [J].