Testobol 4-OHT Ether 60 tabs
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TESTOBOL ETHER oral tablets contain 100 mg of the chemical described as 4,17beta-dihydroxy-4-androstene-3-one tetrahydropyranyl ether a naturally occurring anabolic / androgenic compound. Chemical Structure Its molecular formula is C24-H36-O4 The active ingredient is a white crystalline powder with a molecular weight of 388.54 Each Tablet contains the following: Inactive ingredients: Magnesium Carbonate, Microcrystalline Cellulose, Pregelatinized Starch, Stearic Acid, Magnesium Stearate, Croscramellose Sodium, and FD&C Red #40. CLINICAL PHARMACOLOGY General The chemical term 4-HydroxyTestosterone THP Ether refers to the isomer: 4,17beta-dihydroxy-4-androstene-3-one tetrahydropyranyl ether. 4-HydroxyTestosterone THP Ether (4-OHT Ether) is the THP Ether derivative of 4-HydroxyTestosterone, which is a metabolite or derivative of the naturally occurring precursor hormone 4-Hydroxy-4-Androstenedione. 1 This compound concerns the isomer form of 4,17beta-dihydroxy-4-androstene-3-one tetrahydropyranyl ether. 4-HydroxyTestosterone THP Ether is an anabolic / androgenic compound that acts similar to real Testosterone. It does this by directly binding to the androgen receptor. 4-HydroxyTestosterone cannot directly convert to estrogen due its chemical configuration. Metabolic Actions Compounds in this class also may cause retention of nitrogen, sodium, potassium, and phosphorous, and decreased urinary excretion of calcium. Androgens have been reported to increase protein anabolism and decrease protein catabolism. Nitrogen balance is improved only when there is sufficient intake of calories and protein. Androgens have been reported to stimulate production of red blood cells by enhancing production of erythropoietic stimulation factor. Pharmacokinetics Animal research performed by Gardi R, Falconi G, Pedrali C, Vitali R, Ercoli A (Steroids) 1972 May 19:5 639-47 demonstrates the androgenic and myogenic activity of orally administered ether modified alkyl androstan-17beta-yl mixed acetyls. 2 The chemical addition of ethers and esters are designed to enhance oral absorption and bioavailability. This lipophilicity allows the compound to be absorbed via the lymphatic system and bypass the first-pass through the liver allowing more of the active compound to enter the bloodstream. More specifically this research demonstrates the androgenic and myogenic activity of an ether modified version of 4-HydroxyTestosterone. Androgen Metabolism The biosynthesis and metabolism of steroid hormones in the ovary, testis and adrenal begin with the formation of cholesterol. Cholesterol is metabolized to Pregnenolone which is further metabolized to 17-HydroxyPregnenolone for the formation of DHEA to Androstenedione(4-AD). 4-AD can then proceed to several different Carbon hydroxylations, estrone, testosterone, and androstanes. For the purpose of this document we are concerned with 4-AD metabolism in regards to C4 hydroxylation for the formation of 4-HydroxyTestosterone (4-OHT). 4-OHT occurs as result of 4-AD metabolism as outlined below (See Figure 1). 4-AD is naturally produced in humans and animals. 4-AD hydroxylation is known to occur at C6B, C11B, C15A, C16A, C16B, and at C19. Although steroid hydroxylation at C4 occurs in nature. Since 4-AD and 4-hydroxy-4-Androstenedione (4-OHA) production occur naturally then metabolites of these compound are naturally occurring. Although the research presented also suggests that since steroid hydroxylation at C4 occurs in nature there should be another direct pathway for this compound. (17beta-hydroxy-4-androstene-3-one to 4,17beta-dihydroxy-4-androstene-3-one). The addition of the THP ether is intended for increasing oral absorption and bioavailability thereby considered modifications to enhance the delivery of the nutrient, and not the equivalent of creating a new synthetic hormone. Efficacy Studies The steroidal aromatase inhibitor, 4-HydroxyAndrost-4-ene-3,17-dione (4-OHA) and its metabolites, 4-HydroxyTestosterone (4-OHT), 3 beta,17-dihydroxy-5 alpha-androstan-4-one (metabolite A) and 3 alpha, 17-dihydroxy-5 beta-androstan-4-one (metabolite B) were evaluated as inhibitors of the human prostatic 5 alpha-reductase enzyme and for binding to the rat prostatic androgen receptor. 4-OHA and 4-OHT were weak inhibitors of 5 alpha-reductase with IC50 values of 15-29 microM. Metabolites A and B had no significant inhibitory activity. 4-OHA and metabolites A and B bound weakly to the androgen receptor. The binding affinities (RBA) relative to mibolerone (RBA = 100) were 0.085, 0.485 and 0.016, respectively. However, 4-OHT (RBA = 75) was a more potent binder than the endogenous androgen 5 alpha- dihydrotestosterone (RBA = 66). The ability of these metabolites, in particular 4-OHT, to bind to the androgen receptor may explain the in vivo androgenic activity of 4-OHA.3 Clinical Studies 4,17beta-Dihydroxy-4-androsten-3-one (1'-methoxy) cyclopentyl ether or 4-HydroxyTestosterone (1'-methoxy) cyclopentyl ether was orally administered in sesame oil to rats. Anabolic index was calculated as the ratio of the increase in levator ani weight (milligram over the control) to the increase in ventral prostrate weight. The data collected for androgenic activity consisted of seminal vesicle and ventral prostrate organ weight. Ether modified 4-HydroxyTestosterone exhibited a potent anabolic activity with the second highest anabolic index of (.78) out of 38 hormones tested.4 (See Figure 2) The control utilized to gage potency was the oral anabolic steroid Methyltestosterone which resulted in an anabolic index of (.37). Seminal vesicle and ventral prostrate organ weight for 4-HydroxyTestosterone did not result in any significant increases. This finding correlates with the previous findings, which demonstrated 4-HydroxyTestosterones ability to alter testosterone metabolism by inhibiting the formation of 5-alpha dihydrotestosterone (DHT).