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PubMed1989

The glucocorticoid antagonist 17 alpha-methyltestosterone binds to the 10 S glucocorticoid receptor and blocks agonist-mediated dissociation of the 10 S oligomer to the 4 S deoxyribonucleic acid-binding subunit.

The glucocorticoid antagonist 17 alpha-methyltestosterone inhibits binding of the agonist [3H]triamcinolone acetonide ot the glocucorticoid receptor in cytosol prepared from rat pituitary tumor GH1 cells. Competitive binding studies indicate that the dissociation constant for 17 alpha-methyltestosterone is about 1 microM. After incubation of intact GH1 cells with 10 nM [3H]triamcinolone acetonide at 37 C and subsequent cell fractionation at 4 C, three glucocorticoid receptor forms are observed: cytosolic 10 S receptor, cytosolic 4 S receptor, and nuclear receptor. Concurrent incubation with 17 alpha-methyltestosterone reduces the amount of [3H]triamcinolone acetonide bound to each of these receptor forms. Ligand-exchange assays performed at 0 C in intact cells using [3H]triamcinolone acetonide show that the exchangeable antagonist is associated predominantly with cytosolic 10 S receptor. Immunochemical analysis using monoclonal antibody BuGR2 indicates that 17 alpha-methyltestosterone does not cause substantial accumulation of glucocorticoid receptors in GH1 cell nuclei and, when present together with agonist, reduces nuclear accumulation of receptor seen with agonist alone. Results from dense amino acid labeling studies show that unlike [3H]triamcinolone acetonide, 17 alpha-methyltestosterone does not reduce the total amount of cellular glucocorticoid receptor and does not reduce receptor half-life. These results are consistent with a model for glucocorticoid receptor transformation in which binding of agonist promotes the dissociation of an oligomeric 10 S cytosolic receptor protein to its DNA-binding 4 S subunit. The antagonist 17 alpha-methyltestosterone competes with agonist for binding to the 10 S cytosolic receptor but does not appear to promote dissociation of the oligomer, thus inhibiting agonist-mediated nuclear actions of the glucocorticoid receptor.

Animals↗

PubMed1989

Methyltestosterone-induced cholestasis. The importance of disproportionately low serum alkaline phosphatase level.

We describe a 64-year-old man who developed cholestatic jaundice after receiving 20 to 40 mg of methyltestosterone daily for 6 months for impotence but failed to mention it as part of his drug history. He underwent endoscopic retrograde and papillotomy before a positive history for methyltestosterone ingestion could be obtained. Since methyltestosterone is most often used for sexual impotence, the patient may be quite reluctant to mention this hormone as part of his medication. A normal or mildly elevated alkaline phosphatase level, disproportionate to the level of hyperbilirubinemia seen in this patient and in all previous reports, appears to be characteristic of this phenomenon. This pattern of liver function abnormality can be a clue to suspect methyltestosterone as the causative agent and spare the patient unneeded expensive noninvasive and potentially harmful invasive procedures.

Alkaline Phosphatase↗

PubMed1978

Conservative treatment of endometriosis externa: the effects of methyltestosterone therapy.

Twenty-four women with documented endometriosis externa were treated with methyltestosterone. Twenty-one of these patients desired fertility and three conceived (one after methyltestosterone therapy alone, two after conservative operation followed by methyltestosterone treatment). Ten patients later required surgical therapy for recurrence of pain, although all but one patient had initial relief of pain (3 to 6 months after therapy). These results of therapy are contrasted to those of similar studies in the literature in which methyltestosterone and other agents were used.

Adult↗

PubMed1979

Spontaneous rupture of a liver cell adenoma after long term methyltestosterone: report of a case successfully treated by emergency right hepatic lobectomy.

A case of spontaneous rupture of a liver cell adenoma is reported in a female transexual treated with methyltestosterone 150 mg daily for 7 years. Emergency right hepatic lobectomy was performed successfully. Histology showed peliosis hepatis also. Emergency resection of a liver cell adenoma has been reported in a young woman taking oral contraceptives, and an elective resection in another female transexual treated with methyltestosterone. However, to the best of our knowledge this is the first case of emergency resection of a spontaneously ruptured liver cell adenoma in a transexual treated with long term methyltestosterone. Since there are numerous other patients similarly treated, it may be expected that this complication will be seen again.

Adult↗

PubMed1991

Gas chromatographic assay of methyltestosterone in tablets.

A simple gas chromatographic procedure has been developed for the determination of methyltestosterone in bulk powders and in tablets. Two new silyl ether derivatives of methyltestosterone have been prepared using dimethylethylsilylimidazole (DMESI) and dimethylisopropylsilylimidazole (DMiPSI). The method is accurate and selective for methyltestosterone within the concentration range 0.1-1.5 micrograms microliters-1.

Chromatography, Gas↗

PubMed1979

Incorporation of 3H-thymidine in the nephron of Gasterosteus aculeatus L. and its stimulation by methyltestosterone. A high-speed scintillation autoradiographic study.

The rate of 3H-thymidine incorporation into different parts of the renal proximal tubule of female sticklebacks treated with methyltestosterone was investigated using high-speed scintillation autoradiography. The results are compared with those from normal males before or after mucous transformation of the kidney. Labelled cells are observed in all parts of the proximal tubule, with marked variations from one segment to another. They are numerous in part 2 of the proximal tubule, particularly in the distal region. Male sex hormones affect the labelling rate in all parts of the nephron, especially in the distal region of part 2 of the proximal tubule. In that particular area, new tubule formation by budding is observed in some individuals, but this process does not appear to be a general one. Correlation between the frequency of these figures and the time of treatment could not be established. Comparing the action of sex hormones in females with that in males reveals a difference in reactivity in the proximal zone of part 2 of the proximal tubule, where methyltestosterone has a strong action in females; in contrast, in "mature" and "immature" males, only a few labelled cells are present in this region. It is concluded that kidney enlargement during the breeding season does not result only from a swelling of cells belonging to part 2 of the proximal tubule, as was generally believed, but also from a lengthening or even a proliferation of the proximal tubules, induced by an increase in mitotic activity controlled by male sex hormones.

Animals↗

PubMed1976

Methyltestosterone treatment of infertility associated with pelvic endometriosis.

Sixty-four patients who had infertility associated only with endometriosis were treated with methyltestosterone, 5 mg/day, continuously for a period of 6 months. The patients continued to ovulate while receiving medication and 12 patients became pregnant, on an average, 6 months after the initiation of therapy. A computer analysis indicated that approximately 30% of the patients could expect pregnancy within 2 years after the testosterone treatment was begun. The side effects of the low-dose methyltestosterone therapy were acne in 6% of the patients, mild hirsutism in 3%, and an occasional delay in ovulation.

Adult↗

PubMed1977

Hyperplasia and prolapse of hepatocytes into hepatic veins during longterm methyltestosterone therapy: possible relationships of these changes to the developement of peliosis hepatis and liver tumours.

We report the pathological changes in liver biopsies from 10 patients (four female transexuals and six impotent males) after treatment with 150 mg methyltestosterone daily for periods of up to 3 years, and in a hemihepatectomy specimen from a female transexual who developed a liver adenoma after 37 months of this treatment. Hepatocyte hyperplasia and mild focal sinusoidal dilatation was found in most cases. In some cases there were microcysts and dissociation of hepatocytes. In nine patients there was accumulation of hepatocytes between the endothelium and the supporting collagen of hepatic veins which often resulted in either partial occlusion of their lumina or disruption of their walls. These vascular changes do not appear to have been reported before. It is postulated that a single pathological process-hyperplasia, perhaps related to the anabolic effect of methyltestosterone--could be partly responsible both for the formation of cysts through mechanical obstruction of hepatic veins and for the formation of nodules and tumours.

Adult↗

PubMed1975

Comparison of the role of testosterone and methyltestosterone in developing chloroform-induced renal tubular necrosis in mice.

The presence of testosterone is a prerequisite for the development of chloroform-induced renal tubular necrosis in mice. The purpose of this study was to check whether methyltestosterone exerts the same influence. Castrated males and females were treated with one of these compounds: those treated with testosterone developed renal tubular necrosis after chloroform injection, those which received methyltestosterone were free of this lesion.

Acute Kidney Injury↗

PubMed1978

Virilizing effect of methyltestosterone on female descendants in the rat.

Pregnant rats were given daily a subcutaneous injection of methyltestosterone for 4 days from the 17th to the 20th day of gestation, and were allowed to be delivered to their offsprings (F1) which were used for the examination of later reproductive functioning. When observed for 21 weeks after birth, the growth rate of F1 from methyltestosterone-treated groups was higher than that of F1 from the control group. The anogenital distance in 50-microgram-treated F1 females started to become significantly longer on the 14th day and in 5-microgram-treated F1 females on the 28th day after birth than that in F1 from the control. The day on which vaginal opening took place in 50% of females was 34.4 days of age in both the control and the 5 microgram groups, but it delayed until 40.7 days in the 50 microgram group. Furthermore, persistent estrus was observed after about 90 days of age in the 50 microgram group. This persistent estrus disappeared by placing these females with males, resulting no pregnancy. In the 5 microgram group females could be pregnant, but their female fetuses (F2), when examined on the 21st day of gestation, had significantly shortened the length of the urovaginal septum. The observations show that virilization can be induced in the third generation.

Animals↗

PubMed1977

Methyltestosterone therapy in hereditary angioedema.

In a double-blind study of four patients with hereditary angioedema, the efficacy of methyltestosterone (taken daily in 10-mg linguet form) in preventing attacks was shown. There were 19 episodes during 11.8 months of placebo administration, compared with only four attacks during the 46 months of cumulative methyltestosterone treatment (P less than 0.001). The mean serum C4 protein level was twice as high in all patients when they were taking the drug (176 +/- 36 mug/ml) as compared with the placebo (84 +/- 21 mug/ml), and rose to normal range in three of four patients.

Adolescent↗

PubMed1990

[Fibrosing cholangiolitis after administration of methyltestosterone].

A case of intrahepatic cholestasis of great intensity was observed in a patient taking methyltestosterone. In histological examination of liver biopsy specimen evidence was found of fibrosing intralobular cholangiolitis. The histological findings and the clinical course are discussed considering the disease as an atypical liver reaction to methyltestosterone.

Bile Ducts, Intrahepatic↗

PubMed1977

Nature of acid-induced fluorescence of 17alpha-methyltestosterone.

The fluorescence of the 17alpha-methyltestosterone-trichloroacetic acid reaction product, 1,2,10,15,16,17-hexahydro-10,17,17-trimethylcyclopenta[alpha]phenanthren-3-one, in strong acid was investigated. Structural requirements for fluorescence were derived from absorption and fluorescence studies of related phenanthrenones and cinnamylidene compounds possessing a similar chromophore. All compounds showed fluorescence intensity that was structure and pH dependent. Fluorescence is attributed to both enol and protonated species.

Acids↗

PubMed1991

Galanin-like immunoreactivity is increased in the brain of estradiol- and methyltestosterone-treated eels.

A galanin-like peptidergic system was demonstrated in the brain of Anguilla. A group of immunoreactive perikarya was located in the nucleus preopticus periventricularis close to the recessus preopticus. Galaninergic fibers occurred in various brain areas. Galanin identified in mammalian pituitary cells was undetectable in fish adenohypophysial cells. Estradiol increased the immunostaining of the rostral perikarya and brain fibers in both male and female European eels kept in fresh water and in female American eels in sea water. Methyltestosterone, an aromatizable androgen, increased galanin immunoreactivity in rostral perikarya and brain fibers of male European eels and female American eels. The cross-sectional area of these perikarya increased significantly after both treatments whereas cell bodies of the posteroventral hypothalamus were slightly affected. Dihydrotestosterone showed no clear effect. Fibers close to the corticotropes were sometime increased, but galanin synthesis was not induced in pituitary cells. In contrast, estradiol induced galanin synthesis in rat pituitary cells, but had a still controversed effect on hypothalamic galanin. A putative influence of galanin on the pituitary-gonadal axis is discussed as gonadal hormones diversely affect gonadotropes and gonosomatic indices in Anguilla.

Anguilla↗

PubMed1985

The effect of oral medroxyprogesterone acetate and methyltestosterone on sexual functioning in a male contraceptive trial.

Twenty-three men who participated in a 15-month clinical trial to assess the potential effectiveness of using a combination of varying doses of medroxyprogesterone acetate (MPA) and methyltestosterone (MT) as a male contraceptive agent, completed a "sexual problem checklist" every two weeks. The study was divided into three phases: pre-treatment (3 months), treatment (6 months), post-treatment (6 months). The questionnaire evaluated changes in various aspects of sexual behaviour and sexual perception and explored whether the treatment influenced any of the parameters considered. The results indicated a small, but significant, decrease in subjective assessment of sexual drive. This was not, however, accompanied by a change in sexual behaviour, in that subjects experienced the same number of erections, ejaculations and frequency of intercourse. It is concluded that the combination of MPA and MT in the doses used may produce a slight decrease in subjective assessment of sexual drive, but no change in actual sexual behaviour.

Administration, Oral↗

PubMed1989

Effects of chronic LHRH-a + 17-methyltestosterone or LHRH-a + testosterone therapy on oocyte growth in the striped mullet (Mugil cephalus).

The striped mullet (Mugil cephalus) exhibits a restricted spawning season and matures only once per spawning cycle. In vivo monitoring of ovarian maturation of individual females during the season reveals that timing of full maturity varies. A small percentage of females that mature early can be induced to spawn and will remature. Such females can be spawned a second time within the same season. Chronic administration of luteinizing hormone-releasing analog (LHRH-a) + testosterone results in accelerated egg growth. The majority of females undergoing this therapy mature at least a month before control fish. When these females are induced to spawn, a higher percentage remature and can be spawned again. The double spawnings of both control and LHRH-a + testosterone-treated females occur without any appreciable loss in egg quality. Administration of LHRH-a + 17 alpha-methyltestosterone essentially inhibits egg growth. Steroid profiles from females undergoing this therapy exhibit a significant drop in circulating testosterone and estradiol 17 beta, compared to control and LHRH-a + testosterone-treated females. Hypotheses for the poor performance of this therapy are discussed.

Animals↗

PubMed1979

Selective catalytic reduction of 7-methyl-6-dehydrotestosterone acetate to 7 beta-methyltestosterone acetate by benzyl alcohol.

Using benzyl alcohol as a hydrogen donor in the presence of Pd on charcoal, 7-methyl-6-dehydrotestosterone acetate was selectively reduced to 7 beta-methyltestosterone acetate in 90% yield. The addition of hydrogen atoms to the 6, 7 double bond proceeded from the less hindered alpha-face of the steroid molecule, giving rise to the 7 beta-methyl product. Gas chromatograph analysis indicated small amounts of the 7 alpha-methyl epimer, 7 beta-methyl-5 alpha-dihydrotestosterone acetate and the 5 beta-epimer. The 6,7 double bond was hydrogenated in preference to 4,5 double bond, although both are trisubstituted.

Benzyl Alcohols↗

PubMed1991

The effect of methyltestosterone on the growth hormone response to the dopamine receptor agonist, apomorphine.

1. There is some evidence that androgens affect dopaminergic function in animals and man. We investigated the effect of methyltestosterone (MT) (30 mg po) on the growth hormone (GH) response to the dopamine (DA) receptor agonist, apomorphine (Apo) HC1 (0.5 mg sc), in 9 normal men. MT was given 2 hr before Apo. 2. The peak plasma MT concentration was present 1 hr after administration (19.9 +/- 19.5 ng/ml; X +/- SD); the concentration at 4 hr was 7.2 +/- 4.9 ng/ml. At the time of Apo administration, plasma MT varied from 6.0-24.1 ng/ml. 3. There was no significant effect of MT on Apo-GH secretion (interaction F(7,56) = 1.08; p = NS). The mean individual peak GH concentration after Apo alone was 20.2 +/- 11.9 (X +/- SD) vs 22.2 +/- 9.9 ng/ml when MT preceded Apo (p = NS). 4. These results suggest that exogenous androgens do not affect DA receptor function in males with normal androgenic function. Lack of effect due to an insufficient dose or duration of administration of MT cannot be excluded.

Adolescent↗