Detail of "58691-88-6"

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Interaction of new 19-norprogesterone derivatives with progestagen, mineralocorticoid and glucocorticoid cytosolic receptors

Interaction of new 19-norprogesterone derivatives with progestagen, mineralocorticoid and glucocorticoid cytosolic receptors. Botella, J.; Porthe-Nibelle, J.; Paris, J.In this study， 58652-20-3 and 57-83-0 are also used.; Lahlou, B. (Lab. Physiol. Cell. Comp., Univ. Nice, Nice F 06034, Fr.). J. Pharmacol., 17(4), 699-706 (English) 1986. CODEN: JNPHAG. ISSN: 0021-793X. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) Structure-activity relations were studied in vitro on a no. of natural and artificial steroids in order to assess their progestagen specificity. These substances included TX 066 (nomegestrol acetate) [58652-20-3] [a compd. derived from 19-norprogesterone (I) [472-54-8]] and 2 synthetic intermediates, TX 045 [16895-64-0] and TX 071 [58691-88-6]. The expts. involved binding competition on the cytosolic receptors prepd. from target organs against specific radiolabeled ligands. Relative affinities were detd. in rats against progesterone (P), aldosterone (A), and dexamethasone (DM), by displacement of: (1) [3H]-ORG 2058 from the progestagen receptor of uterus, (2) [3H]-A from Type I (mineralocorticoid) receptor of the kidneys, and (3) [3H]-DM from glucocorticoid receptors of the kidney (Type II) and of the liver. The various modifications introduced in the progesterone mol. led to sequences in competition potency which were either parallel or opposite in the progesterone compared with the 19 norprogesterone series. TX 066, which is intended for use as a progestagen, presents very little mineralo- and glucocorticoid activities at the receptor level; however, its affinity for the progestin receptor is nearly as good as that of progesterone. The 2 derivs. TX 045 and TX 071 displayed very little or no progestagen affinity, and their mineralo- and glucocorticoid potencies were between those of I and TX 066. .