Alfred Boris

Comparative androgenic, myotrophic and antigonadotrophic properties of some anabolic steroids

Abstract Oxymetholone, oxandrolone, methandrostenolone, nandrolone phenpropionate, norbolethone, ethylestrenol, bolasterone, norethandrolone, oxymesterone, methenolone acetate, 4-chlorotestosterone acetate, stanozolol and testosterone were compared for effects upon testes, seminal vesicle, ventral prostate and levator ani weights in immature rats. Testosterone was effective on all four parameters at the lowest tested dose of 40 mcg/day. All of the other compounds showed stimulation of levator ani weight gain at dosages lower than those required to produce increases in the weights of the seminal vesicles and the ventral prostate. All of the preparations except bolasterone, methandrostenolone and testosterone increased the weight of the seminal vesicles at lower dosages than those necessary for prostate weight gain. Nandrolone phenpropionate, norbolethone, bolasterone, norethandrolone, oxymesterone, methenolone acetate and testosterone were antigonadotrophic and myotrophic at the lowest tested dose of 40 mcg/day. The other steroids were antigonadotrophic at dosages equal to or less than those required for myotrophic effects.

Comparison of the effects of six antiandrogens on chick comb stimulation by testosterone.

Summary Six antiandrogens were compared for ability to inhibit the stimulant effect of testosterone on chick comb weight. Relative potencies could not be determined exactly because of nonparallelism of the dose-response curves. Based upon the maximal inhibitions observed, relative potencies were as follows: cyproterone acetate > Ro 5–2537 > methyl, B-nortestosterone > Ro 2–7239 > cyproterone (free OH). A-Norprogesterone was inactive as an antiandrogen at dosages up to 27 × T on a molar basis.

Some studies of the endocrine properties of dydrogesterone.

Abstract Dydrogesterone (9β, 10α-pregna-4, 6-diene-3, 20-dione; Duphaston(R) has been examined in some standard endocrine procedures. The results of these studies indicate that dydrogesterone is uterotrophic, anti-estrogenic, anti-androgenic and antigonadotropic. The data also show that dydrogesterone is not thymolytic and does not cause adrenal atrophy. The compound is not androgenic in either the chick or the castrated rat.

Some endocrine effects of 16-azaestrone-3-methyl ether

Abstract The antigonadotropic and uterotrophic activities of estrone, estrone-3-methyl ether and 16-azaestrone-3-methyl ether were compared in the immature rat. The data obtained indicate that the replacement of carbon with nitrogen in ring D at position 16 reduces, but does not abolish, the antigonadotropic and uterotropic activities.of estrone. This azaesteroid also possesses anti-estrogenic properties.

EFFECTS OF SOME PSYCHOTROPIC DRUGS UPON URINARY WATER OUTPUT.

Summary Chlorpromazine, thioridazine, chlorprothixene, imipramine, amitriptyline, and chlordiazepoxide all manifested antidiuretic activity when a sufficient dose was administered. Diazepam failed to show either diuretic or antidiuretic activity at dosages up to and including 128 mg/kg.

Endocrine Studies of Chlordiazepoxide.

Summary Studies utilizing standard endocrine technics indicate that chlordiazepoxide does not possess gonadal hormone-like activity, anti-gonadal hormone activity, anti-goitrogenic activity, nor does it interfere with normal functioning of the pituitary-gonadal axis.

The effects of some progestational steroids on pubertal ovulation in the rat

15 progestational steroids were tested for their ability to suppress pubertal ovulation in the rat. All of the compounds tested except ethynodiol diacetate inhibited initial ovulation. The steroids tested could be divided into 2 groups based upon their effects on uterine weight. Pregnanes and dimethisterone decreased uterine weight. Nortestosterone derivitives increased the weight of the uterus.

Anti-ovulatory effects of some ahdrogenic-myotrophic steroids in the pubertal rat

The effects of some androgenic-myotrophic steroids on pubertal ovulation in rats were studied. Treatment began at age 32 days. Steroids were given subcutaneously for 14 consecutive days. Autopsy was on the fifteenth day. The control animals showed an ovulation rate of 98% (137/140 rats). All of the steroids tested suppressed ovulation but differed in their potencies. Testosterone (7 rats ovulating/10 in group), dihydrotestosterone (5/10), nortestosterone (4/10), and norethandrolone (6/10) showed inhibitory effects at a dose of 20 micrograms/day. Nortestosterone seemed most effective, reducing ovulation to 10% at a daily dose of 40 micrograms. Androstenedione, methandrostenolone, oxymetholone, oxandrolone, ethylestrenol, and stanozolol required doses of 100 micrograms or more to depress ovulation. With most of the steroids the ovarian weight depression correlated exactly with ovulation suppression in regard to dose. Half of the compounds decreased uterine weight at lower doses but increased it at higher doses within the dosage range (1-4000 micrograms/day). Dihydrotestosterone, oxymetholone, and ethylestrenol caused uterine weight depression, norethandrolone caused uterine weight stimulation, and oxandrolone had no significant effect on this variable. All of the compounds except testosterone, methandrostenolone, and oxymetholone failed to increase body weight. The ovulation suppression, reduced ovarian weight, and reduced uterine weight observed probably are associated with antigonadotropic activity. For purposes of human contraception it is hoped a separation can be achieved by molecular modification between androgenicity and antiovulatory activity.

Utility of pubertal ovulation in the rat for the study of anti-ovulatory compounds

Abstract Immature female rats were autopsied at daily intervals from the ages of 30 to 51 days. Body weights, ovarian weights, uterine weights, and the occurrence of ovulation were recorded. Based upon these data, a starting age (32 days) was selected which would insure lack of prior ovulations, and a duration of treatment (14 days) was chosen which would be sufficient to allow essentially all controls to ovulate. Methallibure, a known, non-steroidal, non-estrogenic, antigonadotropin was then used to test the feasibility of the procedure to detect and evaluate anti-ovulatory compounds. Methallibure showed statistically significant effects on ovulation and ovarian weight at a daily dose of 0.4 mg/rat/day. Uterine weight was depressed significantly at a dose of 1 mg/rat/ day.

A comparison of the androgenic and myotrophic activities of some anabolic steroids in the castrated rat

Abstract Oxymetholone, oxandrolone, methandrostenolone, nandrolone phenpropionate, norbolethone, ethylestrenol, bolasterone, norethandrolone, oxymesterone, methenolone acetate, chlorotes-tosterone acetate, stanozolol and testosterone were compared for effects upon seminal vesicle, ventral prostate and levator ani weights in castrated rats. Linear log dose-response relationships were obtained for all compounds on all three parameters. Variations in slopes indicated non-parallelism of dose-response lines, thus preventing calculations of exact relative potencies. Relative activities are reported based upon “doubling doses” for each target organ.