Effect of Local Application of Progesterone on the Rabbit Uterus

McGinty, Daniel A.; Anderson, Laurie; McCullough, Norman B.

doi:10.1210/endo-24-6-829

Cited by 66 publications

(8 citation statements)

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“…Inhibition of progesterone-stimulated endometrial glandular arborization was assessed according to the McPhail scale in E 2 -primed immature female rabbits (five per group) treated with the test compound either by the oral or intrauterine route [8,16,17]. Intrauterine administration (0.25-1.0 g) was employed to examine direct antiprogestational effects of mono-and didemethylated CDB-2914 and monodemethylated CDB-4124 on the uterine endometrium [17].…”

Section: In Vivo Antiprogestational Activitymentioning

confidence: 99%

“…Intrauterine administration (0.25-1.0 g) was employed to examine direct antiprogestational effects of mono-and didemethylated CDB-2914 and monodemethylated CDB-4124 on the uterine endometrium [17]. Oral administration of the putative metabolites (0.4-1.6 mg per rabbit per day for 5 days) to E 2 -primed rabbits was used to evaluate the contribution of further metabolism.…”

Section: In Vivo Antiprogestational Activitymentioning

confidence: 99%

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In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone

Attardi

Burgenson

Hild

et al. 2004

The Journal of Steroid Biochemistry and Molecular Biology

108

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Section: In Vivo Antiprogestational Activitymentioning

confidence: 99%

Section: In Vivo Antiprogestational Activitymentioning

confidence: 99%

In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone

Attardi

Burgenson

Hild

et al. 2004

The Journal of Steroid Biochemistry and Molecular Biology

108

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“…Progesterone, testosterone propionate, estrone, and norethynodrel were all effective in reducing the number of pregnancies occurring during the treatment period. FIGURE 9 shows the number of rats that became pregnant within 30 days after cessation of treatment. With most of these steroids the effects wear off very rapidly; within 1 month after the cessation of treatment these animals were able to conceive, and pregnancy was carried to a successful conclusion.…”

mentioning

confidence: 99%

Some Biological Activities of 17-Ethynyl and 17-Alkyl Derivatives of 17-Hydroxyestrenones

Saunders¹,

Drill²

1958

Ann NY Acad Sci

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The natural hormone, progesterone, has long served as the standard for the production of endometrial changes in the uterus. In 1944 Allen and Ehrenstein' reported that norprogesterone was more active than the natural hormone, a finding that has since been confirmed by Tullner and Hertz2 Recently it has also been demonstrated that the nor derivative of ethynyltestosterone is more potent as a progestational agent than the methylated parent compound, both in animals and man.3, Studies in this laboratory have encompassed a wide variety of steroid structures. Particular attention has been paid to the study of 17-substituted derivatives of 17-hydroxyestrenones with the double bond in either the 5(10) or the 4(5) position. In the series with the double bond in the 5(10) position, the most interesting substance has been norethynodrel, which shows a mixture of both estrogenic and progestational a~tivities.~ With the double bond in the 4(5) position, estrogenic activity is absent and more nearly pure progestational effects are obtained. However, some of this latter group also have androgenic and anabolic activities.6 Inasmuch as the properties in these two series do differ, the endocrine effects of the A6(lU) compound, norethynodrel, will be discussed first, and the progestational activity of the A4(6) steroids second. MethodsProgesteronelike activity, Clauberg assay.7 Immature female rabbits weighing about 1 kg. were treated for 6 days with 5 fig. of estradiol daily. Starting on the following day they received the test compound in oil, subcutaneously, daily for the next 5 days. On the day after the last injection they were sacrificed and the uteri were fixed for later histological study. Sections of the uterus were graded from 1 to 4 on the basis of glandular development.* Further studies were conducted using the technique described by McGinty et aL9 I n this assay the compound in oil was injected into a segment of the uterus in the ovariectomized rabbit, previously primed with estrogen. Uterine sections were examined histologically and graded as above. Estrogenic activity was determined by the uterine weight technique of Rubin et in immature mice and by the vaginal smear technique of Allen and Doisy17 employing castrated rats and scoring according to the method of Biggers and C1aringbold.l' Norethynodrel Norethynodrel has four main properties: (1) It is progestational under certain conditions; (2) it has estrogenic activity; (3) it can inhibit the pro-516 Progesteronelike activity, intrauterine assay. Estrogenic activity. Saunders & Drill: 17-Ethynyl and 17-Alkyl Derivatives 517 CH 111 C FIGURE 1. Structural formula of norethynodrel.duction or release of pituitary gonadotropin; and (4) during treatment it prevents conception.Detailed data illustrating the biological activities of the pure compound, 17a-ethynyl-17hydroxy-5 (lO)-estren-3-one, called norethynodrel, are presented below.The condition of the uterus of an estrogen-primed control rabbit in the Clauberg assay is shown in FIGURE 2. Glandular crypts are lacking. ...

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“…Institute of Animal Physiology, Babraham, Cambridge (Received 27th February 1970) In view of the indication that an ether extract of uterine flushings from the pig contained progestational activity (Challis, Haynes & Lamming, in preparation) as measured by bioassay (McGinty, Anderson & McCullough, 1939), an attempt has been made to isolate progesterone from the reproductive tract flushings of the guinea-pig. In these experiments, radioactive progesterone was infused intravenously until equilibrium had been established between the endogenous circulating progesterone and labelled steroid.…”

mentioning

confidence: 99%

The Identification of Progesterone in Flushings From the Reproductive Tract of Non-Pregnant Guinea-Pigs

Challis¹,

Illingworth²

1970

Reproduction

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Effect of Local Application of Progesterone on the Rabbit Uterus

Cited by 66 publications

References 0 publications

In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone

In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone

Some Biological Activities of 17-Ethynyl and 17-Alkyl Derivatives of 17-Hydroxyestrenones

The Identification of Progesterone in Flushings From the Reproductive Tract of Non-Pregnant Guinea-Pigs

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