Relative binding affinity of norgestimate and other progestins for human sex hormone-binding globulin
1990; Elsevier BV; Volume: 55; Issue: 8 Linguagem: Inglês
10.1016/0039-128x(90)90062-g
ISSN1878-5867
AutoresA. Phillips, D.W. Hahn, J.L. McGuire,
Tópico(s)Hypothalamic control of reproductive hormones
ResumoThe 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 [3H]testosterone from this carrier protein in vitro. Norgestimate and its 17-deacetylated and 3-keto metabolites did not significantly displace [3H]testosterone from sex hormone-binding globulin at concentrations up to 10,000 nM, whereas gestodene, levonorgestrel, and 3-keto desogestrel displaced [3H]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. (Steroids 55:373–375, 1990)
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