Drospirenone - CAS 67392-87-4
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Not Intended for Therapeutic Use. For research use only.
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Progesterone Receptor
Drospirenone is a synthetic hormone used in birth control pills and postmenopausal hormone replacement therapy pills.
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1.Progestins alter photo-transduction cascade and circadian rhythm network in eyes of zebrafish (Danio rerio).
Zhao Y1, Fent K1,2. Sci Rep. 2016 Feb 22;6:21559. doi: 10.1038/srep21559.
Environmental progestins are implicated in endocrine disruption in vertebrates. Additional targets that may be affected in organisms are poorly known. Here we report that progesterone (P4) and drospirenone (DRS) interfere with the photo-transduction cascade and circadian rhythm network in the eyes of zebrafish. Breeding pairs of adult zebrafish were exposed to P4 and DRS for 21 days with different measured concentrations of 7-742 ng/L and 99-13´650 ng/L, respectively. Of totally 10 key photo-transduction cascade genes analyzed, transcriptional levels of most were significantly up-regulated, or normal down-regulation was attenuated. Similarly, for some circadian rhythm genes, dose-dependent transcriptional alterations were also observed in the totally 33 genes analyzed. Significant alterations occurred even at environmental relevant levels of 7 ng/L P4. Different patterns were observed for these transcriptional alterations, of which, the nfil3 family displayed most significant changes.
2.Effects of different add-back regimens on hypoestrogenic problems by postoperative gonadotropin-releasing hormone agonist treatment in endometriosis.
Lee DY1, Park HG1, Yoon BK1, Choi D1. Obstet Gynecol Sci. 2016 Jan;59(1):32-8. doi: 10.5468/ogs.2016.59.1.32. Epub 2016 Jan 15.
OBJECTIVE: To compare the efficacy of different add-back regimens on hypoestrogenic symptoms during postoperative gonadotropin-releasing hormone (GnRH) agonist treatment in endometriosis patients.
3.Activity of binary mixtures of drospirenone with progesterone and 17α-ethinylestradiol in vitro and in vivo.
Rossier NM1, Chew G2, Zhang K2, Riva F3, Fent K4. Aquat Toxicol. 2016 May;174:109-22. doi: 10.1016/j.aquatox.2016.02.005. Epub 2016 Feb 22.
Despite potential exposure of aquatic organisms to mixtures of steroid hormones, very little is known on their joint activity in fish. Drospirenone (DRS) is a new synthetic progestin used in contraceptive pills in combination with 17α-ethinylestradiol (EE2). Here we systematically analyzed effects of DRS in binary mixtures with progesterone (P4) and EE2. First, we determined the in vitro activity of single compounds in recombinant yeast assays that express the human progesterone, androgen, or estrogen receptor, followed by determination of mixture activities of DRS and P4, DRS and EE2, as well as medroxyprogesterone acetate (MPA) and dydrogesterone (DDG). Mixtures of DRS and P4, as well as of DRS and EE2 showed additive progestogenic and androgenic activities. However, DDG and MPA showed non-additive progestogenic and androgenic activities. We then analyzed the in vivo activity of single compounds and mixtures of DRS and P4, as well as DRS and EE2, by assessing transcriptional changes of up to 14 selected target genes in zebrafish embryos at 48h post fertilization (hpf), and in eleuthero-embryos at 96hpf and 144hpf.
4.Drospirenone intake alters plasmatic steroid levels and cyp17a1 expression in gonads of juvenile sea bass.
Blanco M1, Fernandes D2, Medina P3, Blázquez M4, Porte C5. Environ Pollut. 2016 Mar 17;213:541-548. doi: 10.1016/j.envpol.2016.03.007. [Epub ahead of print]
Drospirenone (DRO) is one of the most widely used progestins in contraceptive treatments and hormone replacement therapies. The pharmacokinetics and potential toxicological effects of DRO were investigated in juvenile sea bass (Dicentrarchus labrax) exposed through the diet (0.01-10 μg DRO/g) for up to 31 days. DRO was detected in the blood (4-27 ng/mL) of fish exposed to the highest concentration, with no significant bioaccumulation over time and no alteration of hepatic metabolizing enzymes, namely, CYP1A and CYP3A-catalysed activities and UDP-glucuronyltransferase (UGT). Pregnenolone (P5), progesterone (P4), 17α-hydroxyprogesterone (17P4), 17α-hydroxypregnenolone (17P5), androstenedione (AD) and testosterone (T) were determined in plasma and gene expression of cyp17a1, cyp19a1a and cyp11β analysed by qRT-PCR in gonads. The significant increase in plasmatic levels of 17P5, 17P4 and AD detected after 31 days exposure to 10 ng DRO/g together with the increased expression of cyp17a1 in females evidence the ability of DRO to alter steroid synthesis at low intake concentrations (7 ng DRO/day).
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CAS 67392-87-4 Drospirenone

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