Reference

Autoradiographic localization of glucocorticosteroid and progesterone binding sites in the human postmortem brain

Autoradiographic localization of glucocorticosteroid and progesterone binding sites in the human postmortem brain. Sarrieau, Alain; Dussaillant, Monique; Agid, France; Philibert, Daniel; Agid, Yves; Rostene, William (Cent. Rech. Paris Saint-Antoine, Hop. Saint-Antoine, Paris 75571, Fr.). J. Steroid Biochem., 25(5B), 717-21 (English) 1986. CODEN: JSTBBK. ISSN: 0022-4731. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) The presence of glucocorticosteroid- and progesterone [57-83-0]-binding sites in the human brain was investigated by using an in vitro autoradiog. approach with 3H-labeled RU 38486 [84371-65-3]. The hippocampus, entorhinal cortex, subiculum, fimbria, and amygdala showed a different pattern of [3H]RU 38486 labeling with various unlabeled steroids (RU 38486, RU 28362 [74915-64-3], cortisol [50-23-7], RU 27987 [74513-62-5], and dexamethasone [50-02-2]). RU 38486 was the best competitor in all these structures. The hippocampus seems to possess mainly glucocorticosteroid-binding sites, whereas the entorhinal cortex and the subiculum contained both glucocorticosteroid- and progesterone-binding sites. Furthermore, the amygdaloid complex and the fimbria showed a high d. of glucocorticosteroid-binding sites.

Synthesis of trimegestone: the first industrial application of bakers' yeast mediated reduction of a ketone

Synthesis of trimegestone: the first industrial application of bakers' yeast mediated reduction of a ketone. Crocq, Veronique; Masson, Christian; Winter, Jacques; Richard, Christian; Lemaitre, Guy; Lenay, Jacques; Vivat, Michel; Buendia, Jean; Prat, Denis (Direction des Recherches de Procedes Chimiques, Roussel Uclaf, Romainville 93235, Fr.). Organic Process Research & Development, 1(1), 2-13 (English) 1997 American Chemical Society. CODEN: OPRDFK. ISSN: 1083-6160. DOCUMENT TYPE: Journal CA Section: 16 (Fermentation and Bioindustrial Chemistry) Section cross-reference(s): 32 Trimegestone (I) is a new progestomimetic mol. developed by Roussel Uclaf for the treatment of postmenopausal diseases. 154171-23-0 and 74513-62-5 which are cas registry numbers are also used here. It is produced on an industrial scale from a related 3-ketal, 17-keto norsteroid intermediate in a 9-step sequence involving hydrocyanation of the 17-keto group, alkylation of the protected cyanohydrin with EtMgBr to give a 17a-hydroxy 20-ketone, stereospecific 17a-methylation of the corresponding 17,20-enolate, and oxidn. of the 20,21-enolate with air and ketal deprotection to give 3,20,21-triketone. The key step of the synthesis is the chemo-, regio-, and almost stereospecific bioredn. of this triketone to the desired 21(S) alc., trimegestone (de = 99%). This bioredn. is performed with bakers' yeast in water, thus showing the efficiency of this method at an industrial level. .