Abstract | BACKGROUND: DESIGN: RESULTS: We confirmed that NG and its metabolite were progestogen partial agonists (EC50 of 13 and 11.1 nM) and ERα selective agonists (EC50 of 30.4 and 43.4 nM), as well as full antagonists of low affinity for GR (IC50 of 325 and 255 nM) and moderate affinity for MR (IC50 of 81.2 and 83.7). CONCLUSION: We demonstrated that NG and dNG have full progestogen and weak estrogenic (through ERα) properties, which could explain in part the efficacy of NG in association with EE for the treatment of moderate acne in women. Moreover, their antagonist MR activity might have a favorable impact on cardiovascular risk, atherosclerosis and lipid profiles.
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Authors | Françoise Paris, Patrick Balaguer, Frédéric Rimbault, Laura Gaspari, Charles Sultan |
Journal | Gynecological endocrinology : the official journal of the International Society of Gynecological Endocrinology
(Gynecol Endocrinol)
Vol. 31
Issue 6
Pg. 487-90
(Jun 2015)
ISSN: 1473-0766 [Electronic] England |
PMID | 25970022
(Publication Type: Journal Article)
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Chemical References |
- Contraceptives, Oral, Synthetic
- ESR1 protein, human
- Estrogen Receptor alpha
- Mineralocorticoid Receptor Antagonists
- Progestins
- Receptors, Glucocorticoid
- Norgestrel
- norgestimate
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Topics |
- Cell Line
- Contraceptives, Oral, Synthetic
(pharmacology)
- Estrogen Receptor alpha
(agonists)
- Humans
- Mineralocorticoid Receptor Antagonists
(pharmacology)
- Norgestrel
(analogs & derivatives, pharmacology)
- Progestins
(agonists)
- Receptors, Glucocorticoid
(antagonists & inhibitors)
|