Wendell H. Rooks

The Relative Expressed Estrogenicity of Oral Contraceptives

Total effective estrogenicity of several human oral contraceptives was investigated through a method determining uterine weight in immature rats. The preparations, normally given to human females in tablet, form were Norinyl-1 (.05 mg mestranol, 1mg norethindrone), Norinyl-2 (.10 mg mestranol, 2 mg norethindrone), Ovulen (.10 mg mestranol, 1mg ethynodiol diacetate), Enovid-E (.10 mg mestranol, 2.5 mg norethynodrel), and Enovid-5 (.075 mg mestranol, 5mg norethynodrel). Each products was administered in total doses of .0025, .005, and .01 of a tablet. Each dose had 3 trials, approximately 10 mice to a trial. Each mouse was given the compound in .2 ml aqueous vehicle orally, daily for a 3-day period so that the sum of the daily doses equaled 1 of the tablet fractions above. Autopsy, on Day 4, discovered the ratio of mg uterus/gm body weight. A .0025 fraction of a tablet of Norinyl-1 produced a mean uterine ratio of 1.79, while control (untreated) mice had a mean ratio of 1.06. Norinyl-2, Ovulen, Enovid-5 and Enovid-E, judging from the corresponding increases in ratios from the control ratio, were found to be 2.1, 2.7, 6, and 8 times, respectively, more estrogenic than Norinyl-1. The relatively high estrogenicity of the Enovids is probably due to the conversion of norethynodrel to estrogenic compounds.

The protective effect of anti-inflammatory steroids on rat-paw necrosis following severance of the common iliac vessels.

Paw necrosis in the adrenalectomized rat was induced by severing the common iliac or ligating the femoral blood vessels. Necrosis did not appear in non-adrenalectomized animals. Administration of either hydrocortisone, 6α, 9α-Difluoro-11β, 16α, 17α, 21-tetrahydroxy-pregna-1, 4-diene-3, 20-dione 16, 17-acetonide or 9α, 11β-dichloro-6α-fluoro-16α, 17α, 21-trihydroxy-pregna-1, 4-diene-3, 20-dione 16, 17-acetonide directly into the paw within two hours after vascular impairment prevented the paw necrosis.

The Nitrogen Retaining Activity in Rats of 19-Nortestosterone 17-(4′-methylbicyclo [2.2.2] oct-2′-ene-1′-carboxylate)

Summary NMB was given in one subcutaneous injection in oil at a dose of 6 mg to female rats on nitrogen and body weight balance. A constant level of food was consumed. A highly significant and prolonged nitrogen retention was obtained. No nitrogen excretion rebound was seen. A significant increase in body weight was produced which was maintained for 19 weeks.