Detail of "569-57-3"

Reference

Comparison of quinestrol and Tace for relief of postpartum breast discomfort

Comparison of quinestrol and Tace for relief of postpartum breast discomfort. Grant, Kenneth; Rabello, Yolanda; Freeman, Angelita Galvan; Freeman, Roger K.; Baumgardner, Selina (Dep. Obstet. Gynecol., Univ. Southern California Sch. Med., Los Angeles, Calif., USA). Obstet. Gynecol. (Hagerstown, Md.), 51(5), 636-9 (English) 1978. CODEN: OBGNAS. ISSN: 0029-7844. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) A single 2-mg dose of quinestrol (I) [152-43-2] was safe and effective for controlling postpartum lactation and for alleviating breast discomfort. A double-blind comparison to Tace [569-57-3] 72 mg every 12 h for 2 days, and to placebo, was made in 134 patients. The single oral dose of I showed efficacy equal to the 2-day regimen of Tace. Both were superior to placebo.

Estrogen-stimulated prolactin synthesis in vitro

Estrogen-stimulated prolactin synthesis in vitro. Classification of agonist, partial agonist, and antagonist actions based on structure. Jordan, V. Craig; Lieberman, Mara E. (Dep. Hum. Oncol., Univ. Wisconsin, Madison, WI 53792, USA). Mol. Pharmacol., 26(2), 279-85 (English) 1984. CODEN: MOPMA3. ISSN: 0026-895X. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) An in vitro assay that depends upon the synthesis of prolactin [9002-62-4] by primary cultures of dispersed cells from immature rat pituitary cells was used to study the structural requirement for estrogen action. Two categories of estrogens were identified: full estrogens (agonists) and partial estrogens (partial agonists) with antiestrogenic actions against the effects of 0.1 nM estradiol (E2) [50-28-2]. All of the agonists [DES [56-53-1], dimethylstilbestrol (DMS) [552-80-7], R2858 [34816-55-2], and RU16117 [61665-15-4]] produced dose-related increases in prolactin synthesis equiv. to E2, although potencies were different: E2 = DES = R2858 > RU16117 > DMS. Partial agonists [ICI 3188 [68373-13-7], tri(4-hydroxyphenyl)chloroethylene [66694-25-5], and bisphenol [80-05-7]] each had bis(4-hydroxyphenol) substitutions at the ethylene double bond and stimulated prolactin synthesis only to about 50% of the maximal response obsd. with E2. Trianisylchloroethylene [569-57-3] was weakly active as a partial agonist, but at high concn. (10 mM) decreased prolactin synthesis produced by 0.1 nM E2. Two series of novel compds. were assayed to det. whether their structures would predict biol. activity. LN2299 [22393-63-1], the cis geometric isomer of a triphenylbromomethylene, was a full agonist with activity equiv. to zuclomiphene [15690-55-8], the cis geometric isomer of clomiphene. Cyclofenyl [2624-43-3] was a partial agonist, but deacetylation to the diphenol increased partial agonist activity and potency. However, introduction of a single pyrrolidinoethyl side chain into the deacetylated cyclofenyl increased antiestrogenic potency and completely suppressed the expression of agonist activity. Finally, LN2833 [93449-26-4], with a novel C(OH)CH3 side chain in the position normally occupied by the alkylaminoethoxy side chain of most antiestrogens, produced antiestrogen activity with no estrogen properties. Antiestrogenic potency was increased in LN2839 by a phenol in the triphenylethylene in a position equiv. to the 3-phenolic hydroxyl of E2. In general, the potency and biol. properties could be predicted by ref. to the structure of the mol. Potent estrogens or antiestrogens have a phenolic hydroxyl in a position that would be equiv. to the 3-phenolic hydroxyl of E2. 9002-62-4 which is the cas registry number of one of substances is just one of reagents here. Partial agonist action is predicted by a 4-hydroxyphenol attached to the same carbon as the phenyl ring equiv. to the A-ring of E2. Extending the side chain (acetyl, aminoethoxy) or other substitutions (e.g., Et, 1-ethanol) alters the resulting estrogen-receptor complex in such a ways as to prevent the expression of prolactin synthesis. These results, with a broad range of compds., support the general proposals of Belleau's macromol. perturbation theory. .