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Chemical Compound Review

AGN-PC-00LHFC     13-methyl-17-oxo-3-sulfooxy- 7,8,9,11,12,14...

Synonyms: SureCN12920398, LS-175082, AC1L19TN, C18H22O5S, [6,7-3H] E1S, ...
 
 
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Disease relevance of Premarin

  • A follow-up survey of 908 women who had received 'Premarin' (conjugated equine oestrogen) for menopausal symptoms revealed 8 cases of ovarian cancer [1].
  • These data seem to indicate that in patients with hyperprolactinemia, tonic secretion of gonadotropin is maintained fairly well, while of the positive feedback effect of Premarin on the release of LH is impaired [2].
  • In 10 normal cyclic women at the mid-follicular phase (D7-9) and 10 hypothalamic amenorrhea patients without galactorrhea, LH release was found 48 to 72 h after the iv injection of 20 mg conjugated estrogens (Premarin) [2].
  • However, long-term exposure to estrogens from the Premarin drug increases the risk of breast cancer [3].
  • Estrogen replacement therapies, such as conjugated equine estrogen (CEE, Premarin), reduce the risk of coronary heart disease among postmenopausal women [4].
 

Psychiatry related information on Premarin

  • CONCLUSION: A 1.25-mg/day dose of Premarin administered for 12 consecutive weeks does not produce a meaningful effect on cognitive performance, dementia severity, behavior, mood, and cerebral perfusion in female AD patients [5].
  • Three recent controlled experimental studies using Premarin showed no effects of HRT in preventing further cognitive decline in women who already have Alzheimer's disease [6].
 

High impact information on Premarin

 

Chemical compound and disease context of Premarin

 

Biological context of Premarin

 

Anatomical context of Premarin

 

Associations of Premarin with other chemical compounds

 

Gene context of Premarin

  • The Km value for estrone-3-sulfate uptake by OATP-B (1.56 microM) was close to that for the high-affinity component observed in Caco-2 cells [31].
  • Human organic anion transporter OAT4 is expressed in the kidney and placenta and mediates high-affinity transport of estrone-3-sulfate (E1S) [32].
  • However, in the ER expressing cells the ability of IL-1beta to increase PAI-1 mRNA and protein levels was attenuated by 17beta-estradiol, tamoxifen and twelve estrogen components of Premarin [33].
  • Additionally, comparisons were made of animals treated with PTH alone, 17alpha-ethynyl estradiol alone, equine estrogens (Premarin) alone, raloxifene alone, or combinations of PTH and equine estrogens or raloxifene [34].
  • When initial uptake of estrone-3-sulfate, a typical substrate of OATP, was studied kinetically, we observed an increase in V(max) with decrease of pH from 7.4 to 5.0, whereas the change in K(m) was negligible [35].
 

Analytical, diagnostic and therapeutic context of Premarin

  • After ovariectomy, the moderately atherogenic diet was continued, and they were treated (36 months) with a control diet (soy protein depleted of SPEs), a diet containing SPEs in soy protein isolate, or a diet containing SPE-depleted soy protein with conjugated equine estrogens (CEE; Premarin) added [36].
  • The putative skeletal effects of dietary soy phytoestrogens (SPE) were examined in comparison with those of conjugated equine estrogens (CEE; Premarin) in a 3-yr longitudinal study in ovariectomized female monkeys [37].
  • METHODS: We studied 120 postmenopausal women who underwent hysterectomy and who had AD treated with Premarin for 1 year [38].
  • The effects of intracortical injections of penicillin, bicuculline, and conjugated estrogens (Premarin) were determined on EEG activity and motor performance [39].
  • Quantitative in situ hybridization with an RNA probe for the 68-kDa neurofilament mRNA revealed a significant dose-dependent effect of Premarin on DRG neurofilament gene expression [40].

References

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  3. Equilenin-derived DNA adducts to cytosine in DNA duplexes: structures and thermodynamics. Ding, S., Shapiro, R., Geacintov, N.E., Broyde, S. Biochemistry (2005) [Pubmed]
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  5. Effects of estrogen on cognition, mood, and cerebral blood flow in AD: a controlled study. Wang, P.N., Liao, S.Q., Liu, R.S., Liu, C.Y., Chao, H.T., Lu, S.R., Yu, H.Y., Wang, S.J., Liu, H.C. Neurology (2000) [Pubmed]
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  14. Differential effect of carbamazepine and valproate monotherapy on plasma levels of oestrone sulphate and dehydroepiandrosterone sulphate in male epileptic patients. Geisler, J., Engelsen, B.A., Berntsen, H., Geisler, S., Lønning, P.E. J. Endocrinol. (1997) [Pubmed]
  15. Effect of experimental infection with Listeria monocytogenes on the development of pregnancy and on concentrations of progesterone, oestrone sulphate and 15-ketodihydro-PGF2 alpha in the goat. Engeland, I.V., Waldeland, H., Ropstad, E., Kindahl, H., Andresen, O. Anim. Reprod. Sci. (1997) [Pubmed]
  16. Perturbations of negative feedback sensitivity in agonadal patients undergoing estrogen replacement therapy. Maruca, J., Kulin, H.E., Santner, S.J. J. Clin. Endocrinol. Metab. (1983) [Pubmed]
  17. In vivo inhibition of oestrone sulphatase and dehydroepiandrosterone sulphatase by oestrone-3-O-sulphamate. Purohit, A., Williams, G.J., Roberts, C.J., Potter, B.V., Reed, M.J. Int. J. Cancer (1995) [Pubmed]
  18. The binding of porphyrins by ligandin. Tipping, E., Ketterer, B., Koskelo, P. Biochem. J. (1978) [Pubmed]
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  20. Double-blind randomized crossover trial of luteal phase estrogens (Premarin) in the premenstrual syndrome (PMS). Dhar, V., Murphy, B.E. Psychoneuroendocrinology (1990) [Pubmed]
  21. In vitro study of the functional expression of organic anion transporting polypeptide 3 at rat choroid plexus epithelial cells and its involvement in the cerebrospinal fluid-to-blood transport of estrone-3-sulfate. Ohtsuki, S., Takizawa, T., Takanaga, H., Terasaki, N., Kitazawa, T., Sasaki, M., Abe, T., Hosoya, K., Terasaki, T. Mol. Pharmacol. (2003) [Pubmed]
  22. Involvement of multispecific organic anion transporter, Oatp14 (Slc21a14), in the transport of thyroxine across the blood-brain barrier. Tohyama, K., Kusuhara, H., Sugiyama, Y. Endocrinology (2004) [Pubmed]
  23. A naturally occurring mutation in MRP1 results in a selective decrease in organic anion transport and in increased doxorubicin resistance. Conrad, S., Kauffmann, H.M., Ito, K., Leslie, E.M., Deeley, R.G., Schrenk, D., Cole, S.P. Pharmacogenetics (2002) [Pubmed]
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  27. The impact of female hormone usage on the lipid profile. The Framingham Offspring Study. Vaziri, S.M., Evans, J.C., Larson, M.G., Wilson, P.W. Arch. Intern. Med. (1993) [Pubmed]
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  31. Predominant contribution of organic anion transporting polypeptide OATP-B (OATP2B1) to apical uptake of estrone-3-sulfate by human intestinal Caco-2 cells. Sai, Y., Kaneko, Y., Ito, S., Mitsuoka, K., Kato, Y., Tamai, I., Artursson, P., Tsuji, A. Drug Metab. Dispos. (2006) [Pubmed]
  32. Human organic anion transporter 4 is a renal apical organic anion/dicarboxylate exchanger in the proximal tubules. Ekaratanawong, S., Anzai, N., Jutabha, P., Miyazaki, H., Noshiro, R., Takeda, M., Kanai, Y., Sophasan, S., Endou, H. J. Pharmacol. Sci. (2004) [Pubmed]
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  34. LY353381 x HCl: an improved benzothiophene analog with bone efficacy complementary to parathyroid hormone-(1-34). Sato, M., Zeng, G.Q., Rowley, E., Turner, C.H. Endocrinology (1998) [Pubmed]
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  36. Inhibition of postmenopausal atherosclerosis progression: a comparison of the effects of conjugated equine estrogens and soy phytoestrogens. Clarkson, T.B., Anthony, M.S., Morgan, T.M. J. Clin. Endocrinol. Metab. (2001) [Pubmed]
  37. Soy phytoestrogens do not prevent bone loss in postmenopausal monkeys. Register, T.C., Jayo, M.J., Anthony, M.S. J. Clin. Endocrinol. Metab. (2003) [Pubmed]
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