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At least 127 records · Page 7Linked to original sources
PubMed1984

Determination of 17 beta-hydroxy-1 alpha-methyl-17 alpha-propyl-5-alpha-androstan-3-one in plasma by gas chromatography-mass spectrometry with single-ion detection.

The topical anti-androgen 17 beta-hydroxy-1 alpha-methyl-17 alpha-propyl-5 alpha-androstan-3-one is determined in plasma samples by extracting with ether and subsequent mass fragmentography with single-ion detection at m/z 303. 17 beta-Hydroxy-1 alpha-methyl-17 alpha-pentyl-5 alpha-androstan-3-one, added to the samples before extraction, is used as the internal standard. Reproducibility was calculated to be +/- 5.9% at the 5-ng/mL level and 0.4% at the 20-ng/mL level. The limit of detection is approximately 1 ng/mL. Total gas chromatography-mass spectrometry analysis time is approximately 10 min/sample.

Administration, Topical↗
PubMed1984

17 alpha-Propylmesterolone (SH 434): an antiandrogenic sebosuppressive substance not influencing circulating testosterone concentrations. Experimental studies in Syrian hamsters.

17 alpha-Propylmesterolone is a new synthetic 5 alpha-reduced steroid with a propyl group in C-17 position and a methyl group in the A ring. The antiandrogenic action of 17 alpha-propylmesterolone on the sebaceous glands, testes weights and plasma testosterone concentrations were examined in the animal model of the Syrian hamster. The substance was given systemically (3, 5 or 10 mg/kg) and topically (3 or 5 mg/kg). 17 alpha-propylmesterolone reduced both sebaceous gland size and sebogenesis significantly in a dose-dependent manner. The topical administration was more effective than the systemic treatment. There was no influence of 17 alpha-propylmesterolone on testosterone concentration in plasma or testes weights although a diminished capacity or absence of free cytoplasmatic androgen receptor sites was detected in the sebaceous glands of the systematically or topically treated Syrian hamster. 17 alpha-Propylmesterolone exerts a potent topical sebosuppressive effect in the animal model. These findings should give rise to human studies and clinical trials.

Androgen Antagonists↗
PubMed1975

An androgen receptor in rat brain and pituitary.

Dihydrotestosterone (DHT) binding was measured in cytosols from brain regions and pituitary of adult female rats and, with the addition of ventral prostate, in adult male rats. Two types of binding were distinguished: one, saturable at concentration of DHT greater than or equal to 5 X 10(-9) M and an unsaturable component. In intact males saturable (limited capacity) binding was detected only in ventral prostate cytosol; 3 days after orchidectomy the saturable binding sites increase 3-fold in prostate and in pituitary, hypothalamus, amygdala and cortex to detectable levels in approximately the same abundance as in females. There were significant differences in the affinities of the limited capacity binding reactions in cytosols of different tissues though all were in the order of magnitude, 10(-9) M DHT. The affinity in pituitary cytosol was lower than in brain regions with the single exception of female amygdala in which the affinity was significantly lower than in cytosol of the same region from 3-day castrate males. The specificity of the limited capacity binding was investigated by competition between [3h]DHT and unlabelled steroids; the most effective competitors were potent androgen agonists and antagonists.

Amygdala↗
PubMed1991

Topical anti-androgenicity of a new 4-azasteroid in the hamster.

The topical anti-androgenic activity of L-651,580 (methyl 3-oxo-4-methyl-4-aza-5 alpha-androst-1-ene-17 beta-carboxylate) was established in a series of for experiments using castrated male hamsters. During each 21-day experiment, the animals received a daily subcutaneous injection of 40 micrograms testosterone propionate or 20 micrograms dihydrotestosterone propionate. Test compound in 25 microliters of gel was applied daily to the left flank organ. Compounds assayed included L-651,580, WIN 17,665 (17 alpha-propyltestosterone), and SH-434 (17 beta-hydroxy-1 alpha-methyl-17 alpha-propyl-5 alpha-androstan-3-one). Endpoints were flank organ area, sebaceous gland area, and prostate weight. Very similar results were obtained with L-651,580 and WIN 17,665. Daily doses of 0.25 mg or more of either compound usually produced a significant reduction in the areas of treated flank organs and sebaceous glands underlying treated flank organs. Neither compound caused significant changes in the area of the contralateral flank organs and sebaceous glands, which indicated they possess little or no systemic activity at topically effective treatment levels. In direct comparisons, SH-434 was less anti-androgenic than L-651,580 or WIN 17,665, although in one experiment, 0.5 mg/d of SH-434 significantly reduced the area of treated flank organs and sebaceous glands. Neither WIN 17,665 nor SH-434 caused a change in prostate weight; however, in one of four tests, a significant decrease was induced by the 0.5 mg/d level of L-651,580. The results of these experiments show that the topical anti-androgenicity of L-651,580 compares very favorably with that of WIN 17,665 and SH-434. They also indicate that the topical administration of effective dosage levels of L-651,580 causes few, if any, systemic effects.

Administration, Topical↗
PubMed1975

Fetal testicular homografting for bilateral congenital anorchism.

Fetal testicular homografting, performed on a 27-year-old man with histologically proven congenital anorchism, is reported. The clinical and laboratory findings 4 and 12 months after the operation suggested that the grafted testicles were viable. No similar case has been encountered in a review of the literature.

Adult↗
PubMed1980

Infertility: a review of 291 infertile couples over eight years.

Two hundred and ninety-one infertile couples were studied over an 8-year period. Anovulation was the most common cause of infertility, being the causative factor in half of the patients. Ovulation induction with clomiphene or cyclic hormone therapy readily achieved pregnancy in the majority of these patients. The distribution of other etiologic factors was fairly uniform, but treatment was much less successful. Thorough evaluation of both partners is advised both for treatment purposes and as a more accurate guide to the prognosis for conception. Furthermore, even in the presence of oligospermia, ovulation induction may be successful in achieving a pregnancy.

Anovulation↗
PubMed1985

Fertility of men with and without a varicocele.

The fertility of 742 men visiting our male infertility clinic was studied. A comparison was made between patients operated on for varicocele and patients treated in other ways. Of the men with a varicocele, 37.8% impregnated their partners; of the men without a varicocele, 21.5%. By subdivision of the total group of patients into those with sperm counts above and those with sperm counts below 20 X 10(6)/ml, it appeared that only men with low sperm counts operated on for varicocele showed a significantly higher fertility, as compared with patients not having a varicocele. It is suggested that patients not having oligozoospermia perhaps have spermatozoal defects other than too low a number as the principal cause of their infertility which do not significantly improve after varicocele operation.

Female↗
PubMed1976

Psychotropic effects of androgens: a review of clinical observations and new human experimental findings.

In a review article, clinical literature concerned with the psychotropic effects of androgens is presented, and the results of experimental clinical work from biochemistry, electrophysiology and psychoexperimental tests are reported. The conclusion that androgens do have psychotropic properties similar to those of well known psychotropic substances is based on evidence from a number of sources: Clinical observations of patients with androgen deficiency or excess, observations of the effect of androgen therapy, and lastly experimental work with methods developed especially for testing psychotropic substances.

Adult↗
PubMedDate not supplied

Hepatitis following cimetidine administration.

There have been only two reports of cimetidine-induced hepatitis. Such a low incidence suggests a hypersensitivity type of reaction. The case of an adult who developed both hepatic dysfunction and an impaired macrophage migration after exposure to cimetidine is discussed.

Aged↗
PubMed1993

Sex hormones and antiandrogens influence in vitro growth of dermal papilla cells and outer root sheath keratinocytes of human hair follicles.

Anagen hair bulb papillae, interfollicular dermal fibroblasts, and interfollicular keratinocytes isolated from fronto-parietal scalp biopsies as well as outer root sheath keratinocytes from plucked anagen hairs were separately grown in subculture for 14 d. The effect of different concentrations (2.4 nM-17.3 microM) of testosterone, dihydrotestosterone, and the antiandrogens cyproterone acetate or 17 alpha-propylmesterolone on growth behavior of the mesenchymal and epithelial cell types of the hair follicle were comparatively studied by means of growth curves, cell doubling times, and 3H-thymidine incorporation. For control, all cell lines were subcultured in hormone-free medium. Testosterone and dihydrotestosterone (345 nM) significantly reduced proliferation of papilla cells compared with dermal fibroblasts (p < 0.01) and outer root sheath keratinocytes compared with interfollicular keratinocytes (p < 0.01), as well as compared with cells cultured in control medium. Low concentrations of 17 beta-estradiol were ineffective, whereas doses of 180 nM 17 beta-estradiol increased the growth velocities of all cell types, especially of papilla cells, compared with dermal fibroblasts. Low doses of either cyproterone acetate (24 nM) or 17 alpha-propylmesterolone (29 nM) induced a growth enhancement, especially of papilla cells and outer root sheath keratinocytes, whereas high doses of cyproterone (1.20 microM) and 17 alpha-propylmesterolone (1.45 microM) had opposite effects. These changes were significant between papilla cells and dermal fibroblasts as well as between outer root sheath keratinocytes and interfollicular keratinocytes. Applying increasing doses of androgens to cyproterone acetate (24 nM)- or 17 alpha-propylmesterolone (29 nM)-containing media neutralized the growth-stimulating effect of antiandrogens, particularly in papilla cells and outer root sheath keratinocytes. However, minor differences between testosterone and dihydrotestosterone effects on cell growth were found. The data clearly demonstrate that the changes of in vitro growth of hair follicle cells depend on the concentrations of androgens and antiandrogens, as higher doses of both antiandrogens tested retarded the cell proliferation similar to testosterone or dihydrotestosterone. The papilla cells and outer root sheath keratinocytes reacted more sensitively to the hormones tested, thereby confirming the concept of a distinct androgen sensitivity of these specialized hair follicle cells.

Adult↗
PubMed1989

Effects of topically applied antiandrogenic compounds on sebaceous glands of hamster ears and flank organs.

Growth of sebaceous glands in the ears and flank organs of castrated male hamsters is dependent on androgen substitution. Taking this for granted, a study was done to compare the effects of topical antiandrogenic treatment in vivo on the morphology and size of sebaceous glands with the concomitant changes in in vitro metabolism of 3H-testosterone. The role of dihydrotestosterone in sebaceous gland stimulation was thereby investigated. Topical treatment was carried out with the androgen antagonist 17 alpha-propylmesterolone (PM), with 4-androsten-3-one-17 beta-carboxylic acid (17 beta-C), and 17 beta-N,N-diethylcarbamoyl-4-methyl-4-aza-5 alpha-androstan-3-one (4-MA), both described as specific 4-steroid-5 alpha-reductase inhibitors, and with progesterone (PRO), which is an androgen receptor antagonist with 5 alpha-reductase inhibiting properties. Regrowth of sebaceous glands after castration and substitution with testosterone propionate or dihydrotestosterone could be inhibited by topical PM and PRO. This occurred irrespective of the influence on testosterone metabolism and irrespective of the mode of substitution. 4-MA, on the other hand, while exhibiting strong 5 alpha-reductase inhibition in vitro, was ineffective in reducing sebaceous gland sizes in vivo. The compound 17 beta-C was ineffective in every respect. In no case were systemic antiandrogenic effects on prostates and seminal vesicles observed. Our results support the view that the DHT formation rate has no regulatory function for growth of sebaceous glands in hamsters and that PM and PRO counteract the androgenic stimulus by their competitive antagonistic binding to the androgen receptor, but not by their influence on testosterone metabolism.

Administration, Topical↗
PubMed1975

Sterility of three brothers in connection with a disturbed carbohydrate metabolism in semen.

Sterile semen of three brothers was investigated biochemically. Most strikingly was the strong similarity of both the amino acid and the carbohydrate composition of the semen. Inside the spermatozoa much more fructose and glucose was present than normally is found. It could be shown that in the seminal plasma peptides and proteins were present all containing more or less beta-alanine and all able to bind glucose and fructose. After incubation with labelled glucose it was evident that inside the spermatozoa enzymes requried for formation of lactic acid were lacking or inactive. Moreover labelled tyrosine and serine was found. Treatment with proviron did not improve carbohydrate metabolism but the amounts of present glucose and fructose inside the spermatozoa had strongly decreased. It is supposed that the sterility of the men is due to a disturbance in spermatogenesis.

Adult↗
PubMed1988

Turner syndrome: effect of hormone therapies on height velocity and adult height.

76 patients with Turner syndrome received estrogen alone, androgen and estrogen started simultaneously or, after preceding androgen therapy, estrogen with or without androgen. Six patients had spontaneous pubertal development and received no estrogen. Two patients received human growth hormone with androgen during greater than 2.0 years. Height velocity increased during all therapies to mean SD scores of 7.6 during androgen-estrogen started simultaneously, 4.6 during androgen alone, 4.2 during androgen-estrogen after preceding androgen, 2.7 during estrogen alone, and 0.6 during estrogen after preceding androgen. Adult height was measured in all cases, it was 145.5 +/- 5.7 (mean +/- SD) for the whole series without significant differences between the groups. It correlated strongly with midparent height, and was greater for patients with the 45,X karyotype than for the others combined.

Adolescent↗