This paper is only available as a PDF. To read, Please Download here.
Abstract
The effect of compound CDRI-85/287, a pure, nonsteroidal antiestrogen, on implantation-associated
changes in rat uterus were studied. Results provide a clear correlation between the
antideciduogenic action of 85/287 (0.05 mg/kg in days 1–5 post-coitum or 2.5 mg/kg
on day 1 post-coitum) and the time of its administration in relation to the secretion
of prenidatory luteal phase estrogen. The antiestrogenic nature of the compound is
further highlighted by inhibition of estradiol-induced increase in vascular permeability.
In the present study, differences in the pattern of biochemical maturation of the
pregnant, pseudopregnant and 85/287-treated rat uterus have also been illustrated.
As compared to the pregnant rat uterus, absence of (the blastocyst and) decidualizing
tissue in the pseudopregnant rat uterus accounts for the low uterine weight, protein,
RNA, phospholipids and alkaline phosphatase at the time of implantation. Post-coital
treatment with 85/287 (2.5 mg/kg, oral) inhibited increase in these parameters at
the time of implantation. Glycogen levels which were lowered in the pregnant rat uterus
on days 5 and 6, remain unaltered in the pseudopregnant and 85/287-treated rat uteri,
suggesting nonutilization of this energy substrate. These findings provide sufficient
evidence that the antiimplantation activity of 85/287 is due to its antiestrogenic
property.
Keywords
To read this article in full you will need to make a payment
Purchase one-time access:
Academic & Personal: 24 hour online accessCorporate R&D Professionals: 24 hour online accessOne-time access price info
- For academic or personal research use, select 'Academic and Personal'
- For corporate R&D use, select 'Corporate R&D Professionals'
Subscribe:
Subscribe to ContraceptionAlready a print subscriber? Claim online access
Already an online subscriber? Sign in
Register: Create an account
Institutional Access: Sign in to ScienceDirect
References
- Foetal resorption in rats treated with an antiestrogen in relation to luteal phase nidatory estrogen secretion.Acta Endocrinol Copenh. 1992; 126: 444-450
- Cellular Biology of the Uterus.in: North Holland, Amsterdam1967: 191
- Implantation and decidua formation after administration of antiestrogenic compounds.Biol Reprod. 1970; 3: 61-66
- Early developmental studies with clomiphene citrate: Their subsequent validation and extension.Indian J Exp Biol. 1992; 30: 931-946
- Biochemical aspects of implantation.J Reprod Fert (Suppl). 1976; 25: 29-52
- The production of deciduomata and the relation between the ovaries and the formation of the decidua.J Am Med Ass. 1908; 50: 1897-1901
- Biological profile of 2-[4-(2-N-piperidi-noethoxyphenyl)]-3-phenyl (2H) benzo(b) pyran, a potent antiimplantation agent in rat.Contraception. 1991; 44: 461-472
- DRI-85/287, a novel antiestrogen and antiimplantation agent: Biological profile and interaction with the estrogen receptors in immature rat uterus.Contraception. 1991; 45: 81-92
- Effect of centchroman on tubal transport and preimplantation embryonic development in rats.J Reprod Fert. 1986; 76: 317-324
- Delayed nidation in the rat induced by progesterone.in: Proc Soc Exp Biol Med. 96. 1957: 155-159
- Protein measurement with Folin reagent.J Biol Chem. 1951; 193: 265-275
Burton K. A study of the conditions and mechanism of the diphenylamine reaction for the colorimetric estimation of DNA. Biochem J, 956;62:315–323.
- Metabolism of U-(14C)glucose in the rat uterus in the presence of an intrauterine device.J Reprod Fert. 1969; 20: 389-400
- Differentiation between ribose-3-phosphate and ribose-5-phosphate by means of the orsinol pentose reaction.J Biol Chem. 1947; 167: 369-376
- Practical Physiological Chemistry.in: McGraw Hill, New York1957: 1060
- Determination of plasma phosphatase by determination of hydrolysed phenol with aminoantipyrine.J Clin Path. 1954; 7: 322-326
- Determination of glycogen.Arch Biochem & Biophys. 1957; 67: 378-386
- Proteins and Steroids in Early Pregnancy.in: Springer-Verlag, Berlin1982: 245
- Mechanism of antifertility action of CDRI-85/287: a coumarin derivative.in: Proceedings of the First Annual Conference of the Indian Society for the Study of Reproduction and Fertility, Bombay, IndiaNov. 3–6 1988: 79
- A new derivative of triphenyl-ethylene: effect on implantation and mode of action in rats.J Reprod Fert. 1967; 13: 101-119
- Uptake of (3H)-leucine into proteins of rat uterus during early pregnancy.Biochim Biophys Acta. 1970; 204: 278-279
- Protein metabolism of the rat uterus during the oestrous cycle, pregnancy and pseudo-pregnancy, and as affected by an antiimplantation compound ICI 46474.J Reprod Fert. 1971; 27: 72-82
- Effect of Centchroman (67/20) and 78/224 on nucleic acid and protein biosynthesis during implantation in rats.J Biosci. 1985; 9: 185-190
- The uptake of (3H)-uridine into nucleic acids of the rat uterus during early pregnancy.Biochem J. 1970; 117: 65-71
- Carbohydrate metabolism in the rat uterus during early pregnancy.Steroids and Lipids Research. 1973; 4: 48-64
- Incorporation of (3H)-uridine into ribonucleic acid of rat uterus during pseudopregnancy and in the presence of ICI 46474 (trans-1-(p-dimethyl aminoethoxyphenyl-1,2-diphenyl but-1-ene).Biochem J. 1970; 119: 609-613
- Uterine lipid metabolism — a review of the literature.Comp Biochem Physiol. 1972; 42B: 175-195
- Uterine nucleic acid and phospholipid metabolism in the early stages of rat pregnancy.J Endocr. 1976; 68: 33-34
- Ultrastructural features of blastocyst attachment and trophoblastic invasion in the rat.J Reprod Fert. 1970; 21: 37-56
- Reaction of the mouse uterus during implantation and deciduoma formation as demonstrated by changes in the distribution of alkaline phosphatase.J Reprod Fert. 1964; 8: 331-338
- Uterine enzymes during early pregnancy.J Endor. 1966; 35: 385-391
- Changes in the uterine sialic acid and glycogen during early pregnancy in the rat.Biol Reprod. 1972; 6: 204-209
- Uterine glycogen metabolism of the rat in early pregnancy.Biol Reprod. 1972; 7: 297-304
- Oestrogen-antiestrogen interaction: effect of U 11100A, MRL-41 (clomiphene) and U 11555A on oestrogen-induced uterine glycogen and protein synthesis in the rat during delayed implantation.Acta Endor. 1969; 62: 489-497
- Duration of antiestrogenicity of compoundInd J Exp Biol. 1992; 30: 968-971
![Math Eq]()
: A new orally active nonsteroidal antiimplantation agent.
: A new orally active nonsteroidal antiimplantation agent.Article info
Identification
Copyright
© 1993 Published by Elsevier Inc.
