Reference

The conversion of d-norgestrel-3-oxime-17-acetate to d-norgestrel in female rhesus monkeys

The conversion of d-norgestrel-3-oxime-17-acetate to d-norgestrel in female rhesus monkeys. Sisenwine, Samuel F.; Liu, Ann L.; Kimmel, Hazel B.; Ruelius, Hans W. (Res. Div., Wyeth Lab., Inc., Radnor, Pa., USA). Contraception, 15(1), 25-37 (English) 1977. CODEN: CCPTAY. DOCUMENT TYPE: Journal CA Section: 2 (Hormone Pharmacology) At 3 and 6 h after a single intragastric 0.5 mg/kg dose of 14C-labeled d-norgestrel 3-oxime 17-acetate (I) [35189-28-7] was given to female rhesus monkeys, 2 major metabolites, d-norgestrel [797-63-7] and d-norgestrel 3-oxime [53016-31-2], and at least 5 minor metabolites were detected in plasma fractions contg. unconjugated metabolites. D-norgestrel was also in plasma fractions contg. conjugated metabolites although the major biotransformation product was d-3.alpha.,5.beta.-tetrahydronorgestrel glucuronide [62319-59-9]. I was not detected in any plasma sample. I is apparently rapidly deacetylated to d-norgestrel 3-oxime, which is then hydrolyzed to d-norgestrel.

The pharmacological profile of norgestimate, a new orally active progestin

The pharmacological profile of norgestimate, a new orally active progestin. Hahn, D. W.; Allen, G. O.; McGuire, J. L. (Res. Lab., Ortho Pharm. Corp., Raritan, N. J., USA). Contraception, 16(5), 541-53 (English) 1977. CODEN: CCPTAY. DOCUMENT TYPE: Journal CA Section: 2 (Hormone Pharmacology) ORF 10131 (norgestimate)(I) [35189-28-7] was a moderately potent progestin, as judged by the classic Clauberg Assay, with an oral potency of about 1/5 that of D-norgestrel. I bound to progesterone [57-83-0] receptors in vitro and maintained pregnancy in ovariectomized rats. I inhibited ovulation in rats with a potency of at least 800 times that of d-norgestrel. I was slightly less androgenic than d-norgestrel. I was not estrogenic, i.e., it did not induce vaginal cornification, and it did not bind in vitro to estrogen receptors. I possessed marked antiestrogenic activity when compared to d-norgestrel.