Disease relevance of Norandrostenolone

• Nortestosterone analogues bearing 11beta-octyl and 11beta-decyl side-chains bind tightly to recombinant AR protein (IC(50) = 6.6 nM and IC(50) = 0.8 nM), block AR dimerization, exhibit activity against LNCaP prostate cancer cells, and comprise partial AR agonists with low antiglucocorticoid activity [1].
• The use of progestogens (nortestosterone or hydroxysteroid derivatives) in order to induce withdrawal periods and to avoid endometrial hyperplasia is recommended [2].

High impact information on Norandrostenolone

• The trans-activation defect of the mutant receptor can be rectified in vitro with the androgenic drug, fluoxymesterone, but not with mesterolone or nortestosterone [3].
• A direct, low-temperature 1-H, 13-C, and 19-F nuclear magnetic resonance study of boron trifluoride complexes with stigmasterol, androstanolone, androsterone, testosterone, nortestosterone, androstenedione, and progesterone-1,2 [4].
• These data indicate that the addition of an electron withdrawing 7alpha-cyano group to 123I-labeled nortestosterone derivatives does not improve their potential to serve as SPECT agents for the imaging of AR densities in the prostate [5].
• In women with normal or elevated sex hormone-binding globulin levels, nortestosterone derivatives increase free T levels only slightly [6].
• Residues of nortestosterone esters at injection sites. Part 2. Behavioural effects [7].

Biological context of Norandrostenolone

• Residues of nortestosterone esters at injection sites. Part 1. Oral bioavailability [8].
• Although there is unequivocal evidence for the endogenous production of nortestosterone in pregnant cows, its function for placenta physiology, pregnancy anabolism and parturition remains unclear [9].
• Comparison of the efficiences of enzymatic and chemical hydrolysis of (nortestosterone and diethylstilboestrol) glucuronides in bovine urine [10].
• Nortestosterone increased heat production [11].

Anatomical context of Norandrostenolone

• In embryonic nortestosterone treated males the appearance of a left 'ovotestis-like' gonad was observed [12].
• A single enzyme in the stallion testis was able to aromatize both testosterone and nortestosterone [13].
• On the other hand, in skeletal muscles that are practically devoid of 5 alpha-reductase activity, the 3-fold higher affinity of nortestosterone to the receptor, expectedly, results in a myotropic activity that is superior to that of testosterone [14].
• Human hepatocyte incubations were used to study the metabolism of precursors of testosterone and nortestosterone and to evaluate qualitatively the correlation between in vitro and published in vivo urinary metabolic profiles [15].

Associations of Norandrostenolone with other chemical compounds

• In contrast, when 19-nortestosterone (NT) is 5 alpha-reduced, its affinity for AR decreases, resulting in a decrease in its androgenic potency [16].
• Young male adult Wistar rats were treated over a 25-day period with either oil (CON, n = 8), nandrolone (nortestosterone decanoate, NAN, n = 8), nandrolone combined with endurance exercise (treadmill running, NAN+EXE, n = 8), or were castrated (CAS, n = 8) [17].
• In all samples the identification of NT and DES was confirmed by high resolution gas chromatography-mass spectrometry (GCMS) [18].
• Groups of female CBA-mice were given 90Sr (14.8 kBq/g-0.4muCi/g--bodyweight) alone or in combination with polyestrodiolphosphate, methylprednisolone or nortestosterone, respectively [19].
• Cell incubations with norandrostenedione and nortestosterone gave rise to large amounts of estrone sulfate in the medium as determined directly by a specific radioimmunoassay (RIA) [20].

Gene context of Norandrostenolone

• The nortestosterone derivatives also showed AR binding, the relative binding affinities ranging from 4.3 to 17.0% as compared with 5alphaDHT [21].
• We conclude that the in vitro binding properties of all four 17alpha-iodovinyl nortestosterone derivatives warrant evaluation of the distribution characteristics of their 123I-labelled analogues to determine their usefulness as PR imaging agents [21].

Analytical, diagnostic and therapeutic context of Norandrostenolone

• Radioimmunoassay of nortestosterone and related steroids [22].
• All subjects tested positive via urinalysis for the presence of nortestosterone at days 3, 5, 7, and 10 [23].
• An immunoassay for nortestosterone with detection by chemiluminescence is described, and applied to the urine and drug administration site of slaughtered cattle [24].
• Metabolic study of 14C-19 Nortestosterone has been carried out in mice by macroscopic autoradiography and in calves by liquid scintillation counting [25].
• A progesterone receptor affinity chromatography reagent: 17 alpha-hexynyl nortestosterone sepharose [26].

References