Detail of "1852-53-5"

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Studies on the mode of action of androgens in neuroendocrine tissues

Studies on the mode of action of androgens in neuroendocrine tissues. Martini, Luciano; Celotti, Fabio; Massa, Renato; Motta, Marcella (Dep. Endocrinol., Univ. Milan, Milan, Italy). J. Steroid Biochem., 9(5), 411-17 (English) 1978. CODEN: JSTBBK. ISSN: 0022-4731. DOCUMENT TYPE: Journal CA Section: 2 (Hormone Pharmacology) Estradiol benzoate (I) [50-50-0] (50 ng/day for 7 or 14 days) did not have any effect on the testosterone 5a-reductase [9036-43-5] and 3a-hydroxy steroid dehydrogenase [9028-56-2] activities in the anterior pituitary and hypothalamus of castrated rats of either sex. On the other hand, the same dose of I enhanced testosterone (II) [58-22-0] conversion in the hypothalamus of castrated female rats. A higher dose of I (5 mg/rat/day) restored to precastration levels of the 5a-reductase activity of the anterior pituitary of animals of both sexes in the 7-day schedule of administration and further decreased it in the 14-day schedule. The same dose, while ineffective on the activity of the enzymes of the hypothalamus of the female, was highly active in suppressing it in the males. Treatment with prolactin [9002-62-4] (800 mg/rat for 5 days) did not modify the rate of conversion of II in the anterior pituitary and in the hypothalamus of normal male rats and in the gland of castrated males. Suppression of the enzymic activities of the hypothalamus of castrated male rats was obsd. II, dihydrotestosterone (DHT) [521-18-6], 5a-androstane-3a,17b-diol (3a-diol) [1852-53-5] were given, in a dose of 2 mg/day for 6 days, to castrated male and female rats in order to assess their inhibiting effect on LH [9002-67-9] and FSH [9002-68-0] secretion. DHT and 3a-diol were better suppressors of LH than II itself in both sexes. With regard to FSH, no steroid was able to affect FSH release in castrated female and male rats with the exception of DHT which showed some inhibiting effect in males. Thus, I and prolactin, by modifying the rate of conversion of II into DHT and 3a-diol, may modulate the effects of II at anterior pituitary and at hypothalamic levels.

Accumulation of carnitine in rat epididymis after injection of [3H]-butyrobetaine in vivo: quantitative aspects, and the effects of androgens and antiandrogens

Accumulation of carnitine in rat epididymis after injection of [3H]-butyrobetaine in vivo: quantitative aspects, and the effects of androgens and antiandrogens. Boehmer, Thomas (Dep. Med. B, Univ. Oslo, Oslo, Norway). Mol. Cell. Endocrinol., 11(2), 213-23 (English) 1978. CODEN: MCEND6. ISSN: 0303-7207. DOCUMENT TYPE: Journal CA Section: 2 (Hormone Pharmacology) After i.m. injection of Me-3H-labeled butyrobetaine [407-64-7] into intact and castrated rats, the specific activity of plasma carnitine (I) [541-15-1] remained nearly const. over 24-96 h and epididymal uptake of I per unit time was const. for up to 72 h. The uptake ratio of intact to castrated rats was high at 48, 72 and 96 h after injection. Administration of estradiol valerate [979-32-8] over 20 days reduced I uptake in epididymis. This redn. was dose-dependent when estrogen was administered i.m. at 0.33-10 mg/day. A redn. of 90% was obtained with the 10 mg dose. An increase from 33 to 100 mg/day caused no further redn. 19-Norspiroxenone [1235-13-8] (2-10 mg/day) and SKF 7690 [3570-10-3] (1.5 and 7.5 mg/day) were less effective than estradiol valerate (10 mg/day) in suppressing epididymal I uptake. Epididymal I uptake in estradiol valerate treated rats (33 mg/ day for 20 days) increased in a time- and dose-dependent manner with testosterone propionate [57-85-2] treatment (50, 250, 1250 mg/day). I uptake increased to 80% of the nonsuppressed levels when testosterone propionate was administered over a 6-day period at 1250 mg/day. Dihydrotestosterone [521-18-6] increased epididymal I uptake to the same extent as testosterone propionate. D4-Androstene-3,17-dione [63-05-8] and 5a-androstane-3a,17b-diol [1852-53-5] (50 mg/day) were less effective, stimulating uptake to only 15% and 40% resp. of the testosterone propionate (250 mg/day) stimulated levels. Changes in epididymal I uptake evoked by various exptl. procedures were closely paralleled by wt. changes in the ventral prostate. This response resemblance indicates a similarity between the androgen sensitivity of the prostate gland and that of the I uptake system in epididymis. The dose-dependent effect of estrogen on the accumulation of epididymal I, together with the marked responses induced in this system by manipulation of its androgen status, support a possible use for the system as an assay for androgen or antiandrogen potency in vivo.