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Lipoidal estradiol

From Wikipedia, the free encyclopedia
Class of chemical compounds
Estradiol stearate, one of the estradiol esters that represents lipoidal estradiol.

Lipoidal estradiol (LE2) is the variety ofendogenous C17β long-chainfatty acidesters ofestradiol which are formed asmetabolites of estradiol.[1][2] Important examples of these esters includeestradiol arachidonate,estradiol lineolate,estradiol oleate,estradiol palmitate, andestradiol stearate.[1][2] LE2 areestrogens but do not bind to theestrogen receptor, instead acting asprohormones of estradiol.[1][2] Relative to estradiol, they have far longer-lasting durations of effect due to their much slower rates ofmetabolism andclearance.[1][2] It has been hypothesized that LE2 may serve as a store of estrogen for when estradiol levels become low.[1][2] LE2 are highlylipophilic andhydrophobic and are found in highest concentrations inadipose tissue and other estrogen-sensitive tissues and in low but detectable concentrations incirculation, with noneexcreted inurine.[1][2] They have been referred to as the "endogenous counterparts of the synthetic esters of estrogens" likeestradiol valerate andestradiol cypionate.[1][2]

Two of the estradiol esters that compose LE2, estradiol palmitate and estradiol stearate, have been developed and marketed formedical use as long-acting estrogens for use viadepotintramuscular injection.[3][4]

Estradiol is esterified into LE2 bylecithin–cholesterol acyltransferase (LCAT).[5]

See also

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References

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  1. ^abcdefgMichael Oettel; Ekkehard Schillinger (6 December 2012).Estrogens and Antiestrogens I: Physiology and Mechanisms of Action of Estrogens and Antiestrogens. Springer Science & Business Media. pp. 235–237.ISBN 978-3-642-58616-3.
  2. ^abcdefgHochberg RB, Pahuja SL, Larner JM, Zielinski JE (1990). "Estradiol-fatty acid esters. Endogenous long-lived estrogens".Ann. N. Y. Acad. Sci.595 (1):74–92.Bibcode:1990NYASA.595...74H.doi:10.1111/j.1749-6632.1990.tb34284.x.PMID 2197972.S2CID 19866729.
  3. ^J. Elks (14 November 2014).The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. p. 898.ISBN 978-1-4757-2085-3.
  4. ^Index Nominum 2000: International Drug Directory. Taylor & Francis. January 2000. pp. 405–.ISBN 978-3-88763-075-1.
  5. ^Clarkson TB, Appt SE, Wood CE, Cline JM (September 2004). "Lessons to be learned from animal studies on hormones and the breast".Maturitas.49 (1):79–89.doi:10.1016/j.maturitas.2004.06.012.PMID 15351099.
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