Effect estradiol

Mong, J. A., et al. (2003b). Reduction of lipocalin-type prostaglandin D synthase in the preoptic area of female mice mimics estradiol effects on arousal and sex behavior. Proc. Natl. Acad. Set USA 100, 15206-11. 

Vargas R, Hewes B, Rego A, Farhat MY, Suarez R, Ramwell PW (1996) Estradiol effect on rate of proliferation of rat carotid segments effect of gender and tamoxifen. J Cardiovasc Pharmacol 27 495-499... 

Creasy GW, Fisher AC, Hall N, Shangold GA. Transdermal contraceptive patch delivering norelgestromin and ethinyl estradiol effects on the lipid profile. J Reprod Med... 

It is useful to compare the activity profile of a SERM with that of estradiol, particularly in relation to effects seen postmenopausally. During chronic administration of estradiol, the risk of endometrial cancer rises co-ad-ministration of a progestin prevents this effect. Breast cancers occur more frequently, likewise thromboembolic diseases. Estradiol effectively alleviates climacteric hot flashes and sweating. After chronic treatment it reduces the incidence of osteoporotic bone fractures by preventing the loss of an estrogen-dependent portion of bone mass. Nonetheless, estrogens can no longer be recommended for this purpose because of the unfavorable benefit-risk constellation (p.330). 

Very Htfle data are available regarding effects of anaboHc steroid implants on the Hpid metaboHsm in growing mminants. Lipogenic enzyme activity and fatty acid synthesis in vitro were elevated in subcutaneous adipose tissue from bulls implanted with estradiol (44), which may account for the increase in fat content of carcasses reported in some studies. TBA implants have no effect on Hpogenesis in intact heifers, and only tend to reduce Hpogenic enzyme activities in ovariectomized heifers (45). 

TABLE 1-5 Effect of Iron on the Birch Reduction of Estradiol 3-Methyl Ether by Lithium, Sodium and Potassium" ... 

A remarkable feature of the Birch reduction of estradiol 3-methyl ether derivatives, as well as of other metal-ammonia reductions, is the extreme rapidity of reaction. Sodium and -butyl alcohol, a metal-alcohol combination having a comparatively slow rate of reduction, effects the reduction of estradiol 3-methyl ether to the extent of 96% in 5 minutes at —33° lithium also effects complete reduction under the same conditions as is to be expected. Shorter reaction times were not studied. At —70°, reduction with sodium occurs to the extent of 56 % in 5 minutes, although reduction with lithium is virtually complete (96%) in the same time. (The slow rates of reduction of compounds of the 5-methoxytetralin type is exemplified by 5-methoxy-tetralin itself with sodium and f-butyl alcohol reduction occurs to the extent of only 50% in 6 hours vs. 99+% with lithium.) The iron catalyzed reaction of sodium with alcohols must be very fast since it competes so well with the rapid Birch reduction. One cannot compensate for the presence of iron in a Birch reduction mixture containing sodium by adding additional metal to extend the reaction time. The iron catalyzed sodium-alcohol reaction is sufficiently rapid that the aromatic steroid still remains largely unreduced. 

The phenotiiiazines may decrease the effectiveness of tiie dopamine receptor agonists. When pramipexole is administered concurrently witii cimetidine, ranitidine, verapamil, and quinidine, there is an increased effect of pramipexole When ropinirole is administered with the estrogens, particularly estradiol, there may be an increased effect of ropinirole... 

The test system was considerably less sensitive to endosulfan when mouse ER, rather than human ER, was used to mediate (3-gal activity (Ramamoorthy et al. 1997). In similar assays, endosulfan at 10 jM had no effect on (3-gal activity in yeast Saccharomyces) transfected with either the human or rainbow trout ER (Andersen et al. 1999). In addition, no effect was observed on transcriptional activation of HeLa cells transfected with plasmids containing an estrogen receptor as a responsive element (Shelby et al. 1996). Endosulfan also did not induce transient reporter gene expression in MCF-7 human breast cancer cells at an incubation concentration of 2.5 pM (Andersen et al. 1999). Maximum endosulfan-induced ER-mediated luciferase reporter gene expression occurred in vitro in a T47D human breast adenocarcinoma cell line at approximately 10 pM, while 50% expression of luciferase occurred at about 5.9 pM the maximum expression was approximately 59% of the effect from exposure to 0.03 nM estradiol (0.00003 pM) (Legler et al. 1999). Luciferase expression from combined treatment with endosulfan and dieldrin was additive over concentrations ranging from 3 to 8 pM. 

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