Antioestrogenic Action of Chlormadinone Acetate

Rosner, Jorge M.; Macome, J. C.; Denari, J. H.; Carli, D. N. De

doi:10.1530/acta.0.0690403

Cited by 8 publications

(5 citation statements)

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“…In contrast to the data presented here and by Eisenfeld 8c Axelrod (1967), Rosner et al (1972) reported a reduction of oestradiol uptake in the uterus and pituitary of the rat after the administration of chlormadinone acetate. It was also observed that the decrease in uterine radioactivity 1 h after the oestradiol injection was restricted entirely to the nuclear cell fraction.…”

Section: Discussioncontrasting

confidence: 99%

Interaction of Contraceptive Progestins and Related Compounds With the Oestrogen Receptor

Jm¹,

Mm²,

Jm³

1975

Acta Endocrinologica

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The distribution pattern of oestradiol in ovariectomized rats as a function of time has been studied following intravenous administration of the tritiated hormone. Oestrogen specific binding with limited capacity was observed in the uterus, vagina, anterior pituitary, adrenals, preoptic area, hypothalamus, amygdala, septum and tractus diagonalis. Maximal uptake of oestradiol in the pituitary occurred within 5 min, in the uterus 60 min after injection, and remained almost unchanged at this level for more than two hours. The binding capacity per mg tissue decreased in the order pituitary, uterus, vagina, preoptic area, adrenals, hypothalamus, amygdala, septum and tractus diagonalis. The hormone concentration in these tissues one hour after [3H]oestradiol injection was lowered by previous administration of ethinodiol, norethinodrel, lynestrenol and norethindrone, whereas medroxyprogesterone, chlormadinone, megestrol and methyllynestrenol had no effect. The same results were obtained, when instead of the steroid alcohols the corre-

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Section: Discussioncontrasting

confidence: 99%

Interaction of Contraceptive Progestins and Related Compounds With the Oestrogen Receptor

Jm¹,

Mm²,

Jm³

1975

Acta Endocrinologica

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“…Chlormadinon acetate, a progestagen which has been investigated as a contra¬ ceptive, is known as a potent anti-oestrogenic and anti-androgenic compound (Maqueo et al 1963;Rudel et al 1964;MacDonald et al 1968;Zañartu et al 1968;Geller et al 1969;Rosner et al 1972).…”

mentioning

confidence: 99%

The Ultrastructure of the Accessory Sex Organs of the Male Rat

Dahl¹,

Hars²

1975

Acta Endocrinologica

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The present paper describes the fine structure of the accessory sex organs of the male rat as seen after administration of the anti-androgenic compound chlormadinon acetate for 20 days. There was a general involution of the organs with macroscopic atrophy and reduced amount of secretory material. Ultrastructurally the cells contained less organelles as compared with the controls, loss of cytoplasm and reduction both of cell height and width. The major changes also included reduction of the Golgi areas and the rough endoplasmic reticulum. Within the dorsal lobe prominent nuclear changes were found. The alterations observed in the present study are similar to the changes which were found in rats treated with another anti-androgenic compound, Cyp A. It is concluded that these two anti \x=req-\ androgenic compounds exert their effects through similar mechanisms with a specific influence on the prostate and the seminal vesicles.

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“…Further, these progestins also inhibited oestradiol binding to oestrogenic receptor, but only to the extent of 8-12%. The decrease in the uptake of [3H]oestradiol in the presence of norethynodrel (Laumas et al, 1972), chlormadinone acetate (Rosner et al, 1972) and norethindrone/norethindrone acetate (Van Kordelaar et al, 1975) has been well demonstrated. In the present study, this progestin-oestradiol interaction was investigated at the receptor level, giving adequate attention to the specific and nonspecific binding.…”

Section: Discussionmentioning

confidence: 89%

Interaction of progestins with steroid receptors in human uterus

Kasid

Buckshee

Hingorani

et al. 1978

Biochemical Journal

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Norethindrone (17beta-hydroxy-19-nor-17alpha-pregn-4-en-20-yn-3-one) and norethindrone acetate (17beta-acetoxy-19-nor-17alpha-pregn-4-en-20-yn-3-one) interfered to a varying degree, by competitive inhibition, with the binding of progesterone and oestradiol to respective cytoplasmic receptors in the human uterus. Progesterone binding to 4S macromolecule was saturable and co-specific for progestins. Competitors like norgestrel (17beta-hydroxy-18-methyl-19-nor-17alpha-pregn-4-en-20-yn-3-one), 19-norprogesterone, medroxyprogesterone acetate (17alpha-acetoxy-6alpha-methylpregn-4-ene-3,20-dione) and compound R(5020) (17,21-dimethyl-19-norpregna-4,9-diene-3,20-dione) possessed higher binding affinities for the progestin receptor. The dissociation constant (K(d)) for the progesterone-receptor interaction was 0.6-1.6nm and the receptor concentration ranged between 6600 and 8200 sites/cell. Norethindrone and norethindrone acetate competed for the progesterone receptor with inhibition constants (K(i)) of 6.8 and 72nm respectively. Gradient displacement and competitive-receptor assays indicated that norethindrone acetate-binding affinity for progestin receptor was approximately one-tenth that of norethindrone and progesterone. The progestins also inhibited oestradiol binding to 4.6S oestrogenic receptor by 8-12%, involving interaction at the oestradiol-binding site with a calculated K(i) value of 0.5-0.8mum. The competitive interaction of progestins with steroid receptors may be of putative importance in explaining the progestin action at the target site.

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Antioestrogenic Action of Chlormadinone Acetate

Cited by 8 publications

References 0 publications

Interaction of Contraceptive Progestins and Related Compounds With the Oestrogen Receptor

Interaction of Contraceptive Progestins and Related Compounds With the Oestrogen Receptor

The Ultrastructure of the Accessory Sex Organs of the Male Rat

Interaction of progestins with steroid receptors in human uterus

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