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Abstract
Several nonsteroidal estrogens, such as ORF 3858 and F6103, which inhibit pregnancy
in experimental animals when given postcoitally, have been previously described. ORF
8511 (1-diphenylmethylenyl-2-methyl-3-ethyl-4-acetoxycyclohexane) which is structurally
similar to these compounds was studied for its postcoital antifertility activity and
estrogenicity in rats, hamsters, mice and rabbits. Results of these studies suggest
a relationship between these two biological endpoints. ORF 8511 produced uterotropic
stimulation in the rat at microgram doses and totally inhibited implantation at 250
μg/kg/day administered on days 1–6 of pregnancy. However, the other species were considerably
less sensitive to the compound with respect to both parameters. The compound stimulated
tubal transport in rats at its minimum effective dose for antifertility activity as
did diethylstilbestrol, a known estrogen. In the hamster, a species relatively insensitive
to the antifertility effect of ORF 8511, endogenous estrogen titres during early pregnancy
were higher than those in the rat. These data suggest that ORF 8511 and similar nonsteroidal
compounds may owe their postcoital antifertility activity to their estrogenicity and
that estrogens may act as pharmacological agents only in species with low normal endogenous
estrogen titres.
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References
- The Effect of Estrogens and Related Substances on Embryonic Viability.in: Raspe G. Advances in the Biosciences. Pergamon Press, New York1970
- Antifertility Properties of two diphenylethene.Acta Pharmacol. (Kbh.). 1968; 1: 1-97
- Postcoital Contraception.Brit. Med. Bull. 1970; 26: 45
- The Biology of Nonsteroidal Antifertility Agents.in: Lednicer D. Contraception. Marcel Dekker, Inc, New York1969
- Effect of F6103 on Implantation and Early Gestation in Women.Acta Endocrinol. 1970; 64: 705-717
- Species Differences in the Estrogenicity and Postcoital Antifertility Activity of ORF 8511 (1-Diphenylmethylenyl-2-methyl-3-ethyl-4-acetoxy-cyclohexane).in: Fed. Proc.32. 1973: 268
- The Relationship of Endogenous Estrogen Levels to the Efficacy of Estrogenic Postcoital Antifertility Agents.The Pharmacologist. 1973; 15: 256
- Species Differences in Egg Transport in Response to Exogenous Estrogen.Anat. Rec. 1967; 157: 163-172
- Time Course of Serum Estrogen and Luteinizing Hormone (LH) Concentrations During the Menstrual Cycle of the Rhesus Monkey.Endocrinol. 1971; 89: 177-183
- Hormone Levels During Prostaglandin F2α Infusions for Therapeutic Abortion.J. Clin. Endocr. Metab. 1972; 34: 531-536
- Antizygotic Activity of 2-methyl-3-ethyl-4-phenyl-4-cyclohexene carboxylic acid.in: Fed. Proc.26. 1967: 486
- Studies on the Antifertility Effect and Metabolism of a New Postcoital Oral Contraceptive, 2-methyl-3-ethyl-4-phenyl-Δ4-cyclohexene carboxylic acid, sodium salt (ORF 4563).J. Pharmacol. Exp. Thera. 1969; 167: 105
- The Effect of 2-methyl-3-ethyl-4-phenyl-Δ4-cyclohexene-carboxylic Acid (ORF 3858) and its ϱ-hydroxylated Metabolites on Uptake of 3H-estradiol-17β by the uterus.in: Proc. Soc. Exp. Biol. Med.136. 1971: 146-149
- Estrone and Estradiol Levels in the Ovarian Venous Blood from Rats During the Estrous Cycle and Pregnancy.Biol. Reprod. 1971; 5: 297-307
- Estrone, Estradiol, Progesterone and 17α-hydroxyprogesterone in the Ovarian Venous Plasma During the Estrous Cycle of the Hamster.Endocrinol. 1972; 91: 1136-1140
- Ovarian Estrogen Secretion During the Estrous Cycle and Under the Influences of Exogenous Gonadotropins in Rats.Endocrinol. Japon. 1968; 5: 215
- Pregnancy in Women with Secondary Amenorrhea Treated with Human Gonadotropin.Lancet. 1964; 1: 184
Article info
Publication history
Accepted:
February 5,
1974
Identification
Copyright
© 1974 Published by Elsevier Inc.