Testosterone steroid profile

Kushnir et al. [44, 45] also measured 17-hydroxyprogesterone within a profile of four adrenal steroids (detailed in Hormonal Steroid Profiles below). They utilized an oxime derivative to improve ESI sensitivity and carried out analyses on an ABI 4000 instrument. Rauh and co-workers [70] published a method for 17-hydroxyprogesterone with ancillary measurement of androstenedione and testosterone. The mass spectrometer was an ABI 4000 instrument with an APCI source, operated in positive-ion mode and with on-line cartridge sample extraction and column switching. The MRM transitions were as used by other workers (Table 5.3.1)... 

Guo and co-workers [24,25] have spearheaded the development of MS/MS serum steroid profiles. Their most recent report describes profiling in 11 min of 12 steroids in 200 pi serum with minimal work-up, comprising acetonitrile protein precipitation. The steroids analyzed were as follows DHEA sulfate, DHEA, aldosterone, cortisol, corticosterone, 11-deoxycortisol, androstenedione, estradiol, testosterone, 17-hy-droxyprogesterone, progesterone, and 25-hydroxyvitamin D3. Stable-isotope-labeled internal standards were incorporated for each steroid. An API-5000 instrument was used with the APPI source in positive-ion mode, with the exception of aldosterone, which had greater sensitivity in negative-ion mode. Separation was carried out on a C8 column, which allowed more rapid separation than the more commonly utilized C18. The MRM transitions utilized are shown in Table 5.3.1. The lower level of sensitivity was between 1.5 and 10 pg/ml, dependent on the steroid. The authors were exhaustive in addressing issues of accuracy, recovery (90-110%) and reproducibility (< 12.2% for same-day and between-day). 

Buiarelli et al. (2004) extended the above analytical approach to many more related steroids when they published a method for the direct analysis of 15 urinary anabolic steroids in a single run, namely T, epitestosterone, dehydroepiandrosterone (DHEA), androsterone, etiocholanolone, their sulfates and their glucuronides (Figure 2,2), They extracted 2 mL of human urine by solid-phase extraction with methanol elution and reconstituted the residue in aqueous methanol in the presence of deuterated internal standards (da-epitestosterone glucuronide, [16,16,17-"H3 testosterone sulfate and [16,16,17-2H3]testosterone), then monitored, for example, mJz. 289-97 and 109 for T and epitestosterone, miz 367-97 for their sulfates, and m/z 463-113 and 287 for their glucuronides. The method does not achieve quantitation, but it allows the estimation of ratios, which makes it possible to monitor the urinary steroid profile, which is useful for monitoring the abuse of anabolic steroids. 

These compounds are specific inhibitors of type II and/or type 15 a-reductase and were removed from the WADA prohibited list in 2010. They are still monitored by our laboratory because they inhibit the conversion of testosterone to 5a-dihydrotestosterone and can alter steroid profiles... 

The phase-I-metabolism of testosterone leads primarily to 5a-androstan-17P-ol-3-one (dihydrotestosterone), 5a-androstan-3a-ol-17-one (androsterone), and 5P-androstan-3a-ol-17-one (etiocholanolone) (Fig. 3.6,2-4, respectively), which represent important parameters of the so-called urinary steroid profile in sports drug testing (see Chapter 6). 

In terms of doping, hCG can be abused to artificially increase plasma testosterone levels. The assumed reasons for this include (a) the stimulation of the testicular testosterone production to counteract the anabolic steroid-induced reduced testis size, and (b) the attempt to mask anabolic steroid misuse being detected by altered urinary steroid profiles or suspicious testosterone /epitestosterone ratios (T/E, see Chapter 6). Consequently, hCG has been prohibited in sports for male athletes since 1987, and the first arbitrary threshold levels of 25 international units (lU) per L of urine were corrected to In 2005, hCG was... 

ADMINISTRATION. The injection or oral intake of testosterone significantly influences the steroid profile, especially the urinary concentration of T and, thus, the T/EpiT and A/T ratios (Table 6.4). Moreover, the increased urinary elimination of metabolites derived from T (including the glucuronide and sulfate of T and the glucuronic acid conjugates of A, E, Adiol, and Bdiol) combined with a reduced excretion of E and 5-androstene-3p,17a-diol was described, which can further substantiate... 

FIGURE 7 In vitro release profiles of steroids with different physicochemical properties from P-CDC6 nanocapsules (HCR HL, hydrocortisone high loaded, HCR CL, hydrocortisone conventionally loaded TST HL, testosterone high loaded TST CL, testosterone conventionally loaded PRO HL,progesterone high loaded PRO CL,progesterone conventionally loaded). 

Figure 9.81 HPLC chromatograms of steroids. The elution profiles of five standard A4-3-oxosteroids are illustrated as the broken line. Peaks = A, progesterone B, 17 a-hydroxyprogesterone C, androstenedione D, testosterone E 11-deoxycortisol. The solid line is a chromatogram of a defatted extract obtained by incubation of pregnenolone with ovarian homogenates. (From Suzuki et al., 1980.)...

Ketoconazole is well absorbed from the gut (poorly where there is gastric hypoacidity, see below) it is widely distributed in tissues but concentrations in CSF and urine are low its action is terminated by metabolism by cytochrome P450 3A (CYP 3A) (t) 8 h). Ketoconazole is effective by mouth for systemic mycoses (see Table 14.2) but has been superseded by fluconazole and itraconazole for many indications largely on groimds of improved pharmacokinetics, imwanted effect profile and efficacy. Impairment of steroid synthesis by ketoconazole has been put to other uses, e.g. inhibition of testosterone synthesis lessens bone pain in patients with advanced androgen-dependent prostatic cancer. 

These improved pharmacokinetic and side-effect profiles for SARMs versus steroidal androgens are associated with potent, tissue-selective effects in therapeutic target tissues. Hyperanabolic effects in skeletal muscle have been seen for SARMs in rat for numerous molecules [90, 151, 176, 184] with myoanabolic effects in castrated rats in the range of 100-150% compared to testosterone. These effects have also been seen in human trials as manifested by increases in LBM and improvements in physical performance tests (stair climb time [96]). Osteoanabolic effects have also been demonstrated in rats [95, 128, 151] and monkeys [130] for numerous molecules however, only limited clinical trials data have been released in human [128],... 

The temperature-responsive colunans used for the separation of steroids were produced by grafting pNIPAM to the adsorbent (Kanazawa et al, 1996). At temperatures above the transition point the pNIPAM-modified surface becomes hydrophobic. This provides better separation of the steroid molecules according to their log P values, where P is the partition coefficient of the substance in an octanol/water system. The separation of steroid molecules depends on the hydrophobicity of the stationary phase, which could be regulated by the temperature change. The temperature rise increases hydrophobicity of the modified stationary phase resulting in longer retention times and better separation of steroids according to their hydrophobicity. This is illustrated in Fig. 13.1, which presents elution profiles of five steroids hydrocortisone, prednisolone, dexamethasone, hydrocortisone acetate and testosterone at different temperatures. 

Wei, J.Q. Wei, J.L. LucareUi, C. Zhou, X.T. Wang, D.Q. Dai, W.J. Li, S. Li, S.M. Liu, R.T. Serum steroid hormonal profiles by reversed-phase liquid chromatography in patients with 17-hydroxylase deficiency and in an affected family, Clin.Chem., 1992, 38, 76-82. [cortisone hydrocortisone deoxy-cortisol androstenedione testosterone progesterone hydroxyprogesterone desoxycorticosterone]... 

Figure 8 Selected ion monitoring of seven steroid hormones profiled in the plasma sample (0.1 ml of plasma analyzed) of a female neonate (a) testosterone (T, m/z 680.2) not detected, [IG.lG.lf- Hjltestosterone (dj-T, m/z 683.2), 4-androstenedione (4A, m/z...

Dehennin, L., and Matsumoto, A.M. (1993) Long-term administration of testosterone enanthate to normal men Alterations of the urinary profile of androgen metabolites potentially useful for detection of testosterone misuse in sport. Journal of Steroid Biochemistry and Molecular Biology, 44,179-189. 

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