PHARMACOLOGY OF 2 NEW VERY SELECTIVE ANTIPROGESTAGENS - ORG-31710 AND ORG-31806

被引:40
作者
KLOOSTERBOER, HJ [1 ]
DECKERS, GH [1 ]
SCHOONEN, WGEJ [1 ]
机构
[1] ORGANON INT BV,DEPT ENDOCRINOL,OSS,NETHERLANDS
关键词
ANTIPROGESTAGENS; BREAST TUMORS; FERTILITY CONTROL; ORG; 31710; 31806; RU486; ZK98299;
D O I
10.1093/humrep/9.suppl_1.47
中图分类号
R71 [妇产科学];
学科分类号
100211 ;
摘要
Org 31710 and Org 31806 are new antiprogestagens. These compounds were tested for their binding affinity to various steroid receptors and for their bio-activity in various animal models and the results were compared with those of RU38486 and ZK 98299. Both Org compounds are strong antiprogestagens with little antiglucocortocoid activity and are devoid of other hormonal activities except for some weak androgenic and anti-androgenic activity. The two compounds are more potent than RU38486 and ZK 98299 with respect to their anti-progestational activity and are more selective. The Org compounds are effective in inhibiting the development of tumours in the 7,12-dimethylbenz(a)anthracene (DMBA) rat model. Org 31710 and Org 31806 may be applied for both the treatment of breast tumours and the improvement of fertility control.
引用
收藏
页码:47 / 52
页数:6
相关论文
共 20 条
[1]  
ALLAN GF, 1992, J BIOL CHEM, V267, P19513
[2]   TREATMENT OF BREAST-CANCER WITH DIFFERENT ANTIPROGESTINS - PRECLINICAL AND CLINICAL-STUDIES [J].
BAKKER, GH ;
SETYONOHAN, B ;
PORTENGEN, H ;
DEJONG, FH ;
FOEKENS, JA ;
KLIJN, JGM .
JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 1990, 37 (06) :789-794
[3]   THE ANTISTEROID RU486 - ITS CELLULAR AND MOLECULAR-MODE OF ACTION [J].
BAULIEU, EE .
TRENDS IN ENDOCRINOLOGY AND METABOLISM, 1991, 2 (06) :233-239
[4]   SERUM PHARMACOKINETICS OF ORALLY-ADMINISTERED DESOGESTREL AND BINDING OF CONTRACEPTIVE PROGESTOGENS TO SEX-HORMONE BINDING GLOBULIN [J].
BERGINK, W ;
ASSENDORP, R ;
KLOOSTERBOER, L ;
VANLIER, W ;
VOORTMAN, G ;
QVIST, I .
AMERICAN JOURNAL OF OBSTETRICS AND GYNECOLOGY, 1990, 163 (06) :2132-2137
[5]   MIFEPRISTONE - A REVIEW OF ITS PHARMACODYNAMIC AND PHARMACOKINETIC PROPERTIES, AND THERAPEUTIC POTENTIAL [J].
BROGDEN, RN ;
GOA, KL ;
FAULDS, D .
DRUGS, 1993, 45 (03) :384-409
[6]   DETECTION AND COMPARATIVE-EVALUATION OF ALDOSTERONE ANTAGONISTS IN GLUCOCORTICOID-TREATED, ADRENALECTOMIZED RATS [J].
CASALSSTENZEL, J ;
BUSE, M ;
LOSERT, W .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1982, 80 (01) :37-45
[7]   INVIVO EVIDENCE AGAINST THE EXISTENCE OF ANTIPROGESTINS DISRUPTING RECEPTOR-BINDING TO DNA [J].
DELABRE, K ;
GUIOCHONMANTEL, A ;
MILGROM, E .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1993, 90 (10) :4421-4425
[8]   MECHANISMS OF ANTIHORMONE ACTION [J].
GRONEMEYER, H ;
BENHAMOU, B ;
BERRY, M ;
BOCQUEL, MT ;
GOFFLO, D ;
GARCIA, T ;
LEROUGE, T ;
METZGER, D ;
MEYER, ME ;
TORA, L ;
VERGEZAC, A ;
CHAMBON, P .
JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 1992, 41 (3-8) :217-221
[9]  
HERMAN M, 1993, ABSTRACT BOOK ENDOCR, P290
[10]   ESTROGENIC ACTIONS OF RU486 IN HORMONE-RESPONSIVE MCF-7 HUMAN BREAST-CANCER CELLS [J].
JENG, MH ;
LANGANFAHEY, SM ;
JORDAN, VC .
ENDOCRINOLOGY, 1993, 132 (06) :2622-2630