RELATIVE BINDING-AFFINITY OF NORGESTIMATE AND OTHER PROGESTINS FOR HUMAN SEX HORMONE-BINDING GLOBULIN

被引：35

作者：

PHILLIPS, A

HAHN, DW

MCGUIRE, JL

机构：

[1] R.W. Johnson Pharmaceutical Research Institute, Ortho Pharmaceutical Corporation, Raritan, NJ

来源：

STEROIDS | 1990年 / 55卷 / 08期

关键词：

STEROIDS; SEX HORMONE-BINDING GLOBULIN; PROGESTINS; NORGESTIMATE; ANDROGENICITY; RECEPTOR AFFINITY;

D O I：

10.1016/0039-128X(90)90062-G

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：

The relative binding affinity of norgestimate for human sex hormone-binding globulin was compared with that of its metabolites and other progestins by measuring their abilities to displace [H-3]testosterone from this carrier protein in vitro. Norgestimate and its 17-deacetylated and 3-keto metabolites did not significantly displace [H-3]testosterone from sex hormone-binding globulin at concentrations up to 10,000 nM, whereas gestodene, levonorgestrel, and 3-keto desogestrel displaced [H-3]testosterone from sex hormone-binding globulin with IC50 concentrations of 23.1, 53.4, and 91.0 nM, respectively. Since it is believed that a progestin may exert androgenic effects by displacing testosterone from sex hormone-binding globulin, thereby increasing circulating levels of free, active testosterone, these data are consistent with the results of preclinical and clinical studies demonstrating the selective progestational activity of norgestimate.

引用

页码：373 / 375

页数：3

共 11 条

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