Steroid hormones estradiol

See also Steroid Metabolism, Steroid Hormone Synthesis, Steroid Hormones, Estradiol, Androgens, Steroid and Thyroid Hormones - Intracellular Receptors, Tamoxifen... 

In most cases, steroid hormones (estradiol, testosterone) and other hydrophobic small signaling molecules act via endocrine signaling cascade. They are synthesized and secreted into the circulation by specialized endocrine cells, and they bind to their corresponding intracellular receptors following direct diffusion across the... 

What are the similarities and differences between the steroid hormones estradiol and testosterone ... 

FIGURE 25.43 The steroid hormones are synthesized from cholesterol, with intermediate formation of pregnenolone and progesterone. Testosterone, the principal male sex hormone steroid, is a precursor to /3-estradiol. Cortisol, a glucocorticoid, and aldosterone, a mineralocorticoid, are also derived from progesterone. 

The ceUular source of the various ovarian steroids has been difficult to unravel, but a transfer of substrates between two cell types is involved. Theca cells are the source of androstenedione and testosterone. These are converted by the aromatase enzyme in granulosa cells to estrone and estradiol, respectively. Progesterone, a precursor for all steroid hormones, is produced and secreted by the corpus luteum as an end-product hormone because these cells do not contain the enzymes necessary to convert progesterone ro other steroid hormones (Figure 42-8). 

The influence of gonadal hormones on prepubertal animals suggests some steroidal sensitivity in adults with regard to F. elicitation. Young male sheep are induced to perform F. in response to exogenous T and to 17-p-estradiol F. in female red deer is also sensitive to T injections (Parrott, 1978 Fletcher, 1978). Sex differences can interact with the hormonal state where social conditions vary. Female cats (intact) display F. to urine marks only in the absence of males testosterone propionate induced F. in spayed females towards estrous females (Verbeme, 1976 Hart and Leedy, 1987), whereas an ovarian hormone (estradiol) failed to elicit F. to males (intact, and sexually inactive), presumably indicative of social inhibition overriding steroid facilitation. 

The intracellular distribution of steroid hormone receptors has long been the object of controversy. The first theoretical formulation on the intracellular location of the ERs was elaborated by Jensen in 1968 and is known as the two-step theory. Its execution was based entirely on biochemical observations obtained by means of tritium-marked estradiol. The ERs, in cells not exposed to hormones, are found abundantly in the soluble cell fraction, or cytosol (Fig. 1.1). Treatment with hormones confines the receptors to the particulated or nuclear fraction and causes their disappearance from the cytosol. The two-step theory established that the receptor is found in the cytoplasm naturally and upon the arrival of a hormone it is transformed into a complex hormone-receptor (first step) capable of translocating itself to the nucleus and of modifying gene expression (second step). 

Brain delivery of steroid hormones is also of interest to medicinal chemists. Again, most data available on CDSs of steroids pertain to rates of oxidation of the dihydropyridine carrier, to blood and brain concentrations, and to pharmacological activities. The latter can then be taken as proof of efficient cerebral hydrolysis of the pyridinium metabolite. Thus, the dihydrotrigonelline carrier allowed good brain delivery of estradiol and some other estrogens [181][182],... 

Steroid hormones form a group of pollutants that includes natural hormones such as estradiol, testosterone, and their metabolites as well as several synthetic analogues. Steroid hormones used as growth promoters have already been found in water and sediments (Lai et al. 2000 Thorpe et al. 2003), and their adsorption properties on earth materials have been considered. Lee et al. (2003) report batch experiments where simultaneous sorption of three hormones (17- 3-estradiol, 17-a-ethyl estradiol, and testosterone) on four midwestem U.S. soils and a freshwater sediment were performed. Apparent sorption equilibria were reached within a few hours. Sorption isotherms generally were linear for the chemicals studied on one of these soils (Drummer soil), ranged from 23.4 to 83.2 L kg and log ranged... 

Many steroid hormones are regulated by this type of axis—e.g., thyroxin, cortisol, estradiol, progesterone, and testosterone. In the case of the glucocorticoids, the hypothalamus releases corticotropin-releasing hormone (CRH or corticoliberin, a peptide consisting of 41 amino acids), which in turn releases corticotropin (ACTFl, 39 AAs) in the pituitary gland. Corticotropin stimulates synthesis and release of the glandular steroid hormone cortisol in the adrenal cortex. 

Examples are shown in Fig. 23.9. Stereochemistry is indicated by dotted lines (a-bonds, behind the plane) and solid lines (P-bonds, in front of the plane) of any substituents on the rings. The sex hormones are the molecules mainly responsible for differentiating the sexes. The difference between testosterone and progesterone is a hydroxy versus an acetyl group. The natural sex hormones are used to treat prostate cancer, to alleviate menopausal distress, and to correct menstrual disorders. Other common natural steroids are estradiol, cholesterol, and cortisone. Infamous... 

Of the numerous hormones that regulate body function, two steroid hormones are extremely important estradiol, a female sex hormone and testosterone, a male sex hormone. Present in the body in insignificant amounts, they regulate sexual differentiation and reproduction as well as affect the performance of many other physiological systems. Despite the great similarity in chemical structure, they are very different in terms of physiological action. 

Sulfotransferases (SULTs) are important for the metabolism of a number of drugs, neurotransmitters, and hormones, especially the steroid hormones. The cosubstrate for these reactions is 3 -phosphoadenosine 5 -phosphosulfate (PAPS) (Fig. 4.1). Like the aforementioned enzymes, sulfate conjugation typically renders the compound inactive and more water soluble. However, this process can also result in the activation of certain compounds, such as the antihypertensive minoxidil and several of the steroid hormones. Seven SULT isoforms identified in humans, including SULTs lAl to 1A3, possess activity toward phenolic substrates such as dopamine, estradiol, and acetaminophen. SULTIBI possesses activity toward such endogenous substrates as dopamine and triiodothyronine. SULTIEI has substantial activity toward steroid hormones, especially estradiol and dehydroepiandrosterone, and toward the anti-... 

Synthetic steroid hormones retain the common steroid nucleus, but they may contain novel substituents that affect their pharmacological activity. The two most widely used synthetic steroid estrogens are ethinyl estradiol (Estinyl) and mestranol, found in oral contraceptives. Synthetic steroids containing an ethinyl substitution are metabolized more slowly. Thus, these synthetic steroid hormones have better oral absorption properties and extended biological half-lives than the natural estrogens. 

Approximately 50% of a dose of mestranol is de-methylated to form ethinyl estradiol. Ethinyl estradiol also can be deethinylated. Subsequently, the metabolism of these two synthetic estrogens proceeds by means of the same pathways as the natural steroid hormones. The principal metabolites of mestranol and ethinyl estradiol are hydroxylated derivatives that are conjugated with either glucuronic acid or sulfate. The synthetic steroid estrogens, in contrast to the natural estrogens, are excreted primarily in the feces. 

Sexual receptivity. The effects of THC on sexual behavior in female rats and its influence on steroid hormone receptors and neurotransmitters in the facilitation of sexual receptivity was examined. Results revealed that the facilitatory effect of THC was inhibited by antagonists to both progesterone and dopamine D(l) receptors. To test further the idea that progesterone receptors (PR) and/or dopamine receptors (D[1]R) in the hypothalamus were required for THC-facilitated sexual behavior in rodents, antisense, and sense oligonucleotides to PR and D(1)R were administered intra-cerebroventricularly into the third cerebral ventricle of ovariectomized, estradiol benzoate-primed rats. Progesterone- and THC-facilitated sexual behavior was inhibited in animals treated with antisense oligonucleotides to PR or to D(1)R. Antagonists to... 

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