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  • Title: Binding of a contraceptive progestogen ORG 2969 and its metabolites to receptor proteins and human sex hormone binding globulin.
    Author: Bergink EW, Hamburger AD, de Jager E, van der Vies J.
    Journal: J Steroid Biochem; 1981 Feb; 14(2):175-83. PubMed ID: 6451769.
    Abstract:
    Org 2969 is an orally active progestogen which can be used in oral contraceptives because of its strong ovulation-inhibiting activity and acceptability. The present study examines tha binding of Org 2969, its metabolites and reference coupounds to the progesterone and estrogen receptors in human and rabbit myometrium, the rat prostate androgen receptor and human SHBG (sex hormone binding globulin). At 4 degrees Centigrade, the affinite of the major metabolite 3-keto-Org 2969 was similar to that of levonorgestrel and 6 and 2 times higher than that of progesterone and norethisterone, respectively. At 30 degrees, the binding affinity of 3-keto-Org 2969 was twice that of levonorgestrel and 25 times that of progesterone. Other metabolites and derivatives tested displayed low but measurable affinities under equilibrium and non-equilibrium conditions. The binding characteristics of Org 2969 and its metabolites differ from those of other progestogens. The major metabolite 3-keto-Org 2969 binds strongly to the progesterone receptor and relatively weakly to the androgen receptor and human SHBG and shows little or no affinity for the estrogen receptor. Org 2969 is a strong and specific progestogen and its use in oral contraceptives will induce a low incidence of androgenic side effects.
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