Norgestimate-d6 (Synonyms: Dexnorgestrel acetime-d6)

Norgestimate-d₆ is intended for use as an internal standard for the quantification of norgestimate by GC- or LC-MS. Norgestimate is a progestin and a prodrug form of norelgestromin and levonorgestrel .^1,2 It binds to progestin receptors (mean IC₅₀ = 3.48 nM for rabbit uterine receptors) and is selective for progestin over androgen receptors (mean IC₅₀ = 764 nM for rat prostatic receptors) in radioligand binding assays.³ Norgestimate maintains pregnancy in ovariectomized female rats in a dose-dependent manner.¹ It inhibits ovulation in 100% of female rats when administered at a dose of 0.5 mg/kg. Norgestimate (2 mg/kg) completely inhibits estrone-induced vaginal cornification in ovariectomized female rats, indicating antiestrogenic activity. Formulations containing norgestimate in combination with ethinyl estradiol have been used as oral contraceptives and in the treatment of acne vulgaris.

1.Hahn, D.W., Allen, G.O., and McGuire, J.L.The pharmacological profile of norgestimate, a new orally active progestinContraception16(5)541-553(1977) 2.Stanczyk, F.Z.All progestins are not created equalSteroids68(10-13)879-890(2003) 3.Phillips, A., Demarest, K., Hahn, D.W., et al.Progestational and androgenic receptor binding affinities and in vivo activities of norgestimate and other progestinsContraception41(4)399-410(1990)