MINERALOCORTICOID ANTAGONIST ACTIVITY OF AN 11-BETA 18-OXIDOPREGNANE

被引：22

作者：

ULICK, S

MARVER, D

ADAM, WR

FUNDER, JW

机构：

[1] UNIV CALIF SAN FRANCISCO, SCH MED, SAN FRANCISCO, CA 94143 USA

[2] REPATRIAT GEN HOSP, HEIDELBERG 3077, AUSTRALIA

[3] PRINCE HENRYS HOSP, MRC, MELBOURNE 3004, VICTORIA, AUSTRALIA

来源：

ENDOCRINOLOGY | 1979年 / 104卷 / 05期

关键词：

D O I：

10.1210/endo-104-5-1352

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

Removal of the 18-hydroxy group of the hemiacetal form of aldosterone transforms its activity from that of pure agonist to predominant antagonist. The 18-deoxy derivative possesses one third of the binding affinity of aldosterone for the cytoplasmic mineralocorticoid receptor of rat kidney and exhibits an approximate 2:1 antagonist to agonist ratio in both toad bladder and adrenalectomized rat bioassay systems. The promising properties of the 11β, l8-oxidopregnane tested included very low androgen receptor affinity and approximately equal effectiveness in vitro and in vivo in displacing aldosterone from mineralocorticoid-binding sites in the rat. © 1979 by The Endocrine Society.

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页码：1352 / 1356

页数：5

相关论文

共 30 条

[1] AMPLIFICATION OF ACTION OF ALDOSTERONE BY 5-ALPHA-DIHYDROCORTISOL [J].

ADAM, WR ;

FUNDER, JW ;

MERCER, J ;

ULICK, S .

ENDOCRINOLOGY, 1978, 103 (02) :465-471

[2] SC25152 - POTENT MINERALOCORTICOID ANTAGONIST WITH REDUCED AFFINITY FOR 5-ALPHA-DIHYDROTESTOSTERONE RECEPTOR OF HUMAN AND RAT PROSTATE [J].

CUTLER, GB ;

PITA, JC ;

RIFKA, SM ;

MENARD, RH ;

SAUER, MA ;

LORIAUX, DL .

JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM, 1978, 47 (01) :171-175

[3]

Duax W L, 1976, Recent Prog Horm Res, V32, P81

[4] BINDING OF 18-HYDROXYDEOXYCORTICOSTERONE AND 18-HYDROXYCORTICOSTERONE TO MINERALOCORTICOID AND GLUCOCORTICOID RECEPTORS IN RAT-KIDNEY [J].

FELDMAN, D ;

FUNDER, JW .

ENDOCRINOLOGY, 1973, 92 (05) :1389-1396

[5] ROLES OF PLASMA BINDING AND RECEPTOR SPECIFICITY IN MINERALOCORTICOID ACTION OF ALDOSTERONE [J].

FUNDER, JW ;

FELDMAN, D ;

EDELMAN, IS .

ENDOCRINOLOGY, 1973, 92 (04) :994-1004

[6] 16 BETA-HYDROXYDEHYDROEPIANDROSTERONE - DICHOTOMY BETWEEN RENAL RECEPTOR-BINDING AND URINARY ELECTROLYTE ACTIVITY [J].

FUNDER, JW ;

ROBINSON, JA ;

FELDMAN, D ;

WYNNE, KN ;

ADAM, WR .

ENDOCRINOLOGY, 1976, 99 (02) :619-628

[7] SC23992 - RADIORECEPTOR ASSAYS FOR THERAPEUTIC AND SIDE-EFFECTS [J].

FUNDER, JW ;

MERCER, J ;

HOOD, J .

CLINICAL SCIENCE AND MOLECULAR MEDICINE, 1976, 51 :S333-S334

[8] SPECIFIC ALDOSTERONE BINDING IN RAT-KIDNEY AND PAROTID [J].

FUNDER, JW ;

FELDMAN, D ;

EDELMAN, IS .

JOURNAL OF STEROID BIOCHEMISTRY, 1972, 3 (02) :209-&

[9] MOLECULAR MODIFICATIONS OF ANTI-ALDOSTERONE COMPOUNDS - EFFECTS ON AFFINITY OF SPIRONOLACTONES FOR RENAL ALDOSTERONE RECEPTORS [J].

FUNDER, JW ;

FELDMAN, D ;

HIGHLAND, E ;

EDELMAN, IS .

BIOCHEMICAL PHARMACOLOGY, 1974, 23 (10) :1493-1501

[10] MICROBIOLOGICAL SYNTHESIS OF ALDOSTERONE FROM CORTICOSTERONE [J].

KONDO, E ;

MITSUGI, T ;

TORI, K .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1965, 87 (20) :4655-&