Victor A. Drill

Comparative Androgenic and Anabolic Effects of Several Steroids

Summary The androgenic and anabolic effects of testosterone, testosterone propionate, methyl testosterone, methyl androstenediol, androstanolone and 17-ethyl-19-nortestosterone (Nilevar) were compared. The greatest androgenic responses were obtained with testosterone propionate while the most marked anabolic effects were observed with either testosterone propionate or 17-ethyl-19-nortestosterone. Compared to testosterone propionate, methyl androstenediol and androstanolone showed a small increase in the anabolic: androgenic potency ratio but a much more marked increase was observed with 17-ethyl-19-nortestosterone.

SOME BIOLOGICAL ACTIVITIES OF 17‐ETHYNYL AND 17‐ALKYL DERIVATIVES OF 17‐HYDROXYESTRENONES

Some biological activities of 17-ethynyl and 17-alkyl derivatives of 17-hydroxyestrenones were investigated. The most interesting substance in the series with a double bond in the 5(10) position is norethynodrel. Studies have shown that on oral administration norethynodrel produces a progestational response in the estrogen-primed rabbit. This compound has a low but definite inherent estrogenic activity. This estrogenicity prevents the full manifestation of the potential progestational effects of norethynodrel in the rabbit. Norethynodrel causes pituitary gonadotropin inhibition and prevents fertile matings in rats when either the male or the female is treated. However the sterility so induced is temporary as shown both by the rapid recovery in the weights of the gonads and the accessory organs and by the rapid restoration of potency in both females and males after treatment is stopped. Enovid is norethynodrel to which has been added 1.5% of the 3-methyl ether of ethinyl estradiol. This mixture is slightly more estrogenic than norethynodrel but both produce similar progestational responses in the rabbit endometrium. Estrogenicity appears to mask progestational activity in some of the compounds with a double bond in the 5(10) position when they are administered in the uterine lumen. In others of the series as well as in most of those with a double bond in the 4(5) position no estrogenicity was manifest. Many of these compounds produce full progestational effects in the rabbit endometrium and are effective in maintaining pregnancy in the spayed rabbit.

Progesterone-Like Activity of a Series of 19-Nortestosterones

Summary 1. Progestational activity of a series of 17-substituted 19-nortestosterone derivatives was investigated using both intrauterine and systemic assays in rabbits. Several of the substances studied possessed a high order of progestational activity. This activity was not related to either androgenic or anabolic potency of these compounds. Of the compounds studied 17-butenyl appeared to be the most potent, possessing about 10 times and 2 1/2 times the activity of progesterone in intrauterine and systemic assays, respectively. 2. Progesterone-like activity of these 19-nortestosterones was further demonstrated by the ability of some members of the series to maintain pregnancy in ovariectomized rabbits.

PHARMACOLOGICAL PROPERTIES OF PEPSIN INHIBITORS

A review of the literature along with certain experimental studies in our laboratories on the physical, chemical and biological properties of a variety of synthetic sulfated polysaccharides have shown that the pharmacological activities of these substances seem to depend upon a complex interaction of two or more physical or chemical parameters. For example, only fair correlations existed between high antipepsin, antiulcer and anticoagulant activity and high molecular weight or sulfate content. The roles of monosaccharide content, chain shape or the type of glucosidic linkage were difficult to evaluate with the data at hand.

Effects of mescaline in laboratory animals and influence of ataraxics on mescaline-response.

Summary Mescaline, injected intravenously and intraperitoneally into dogs and cats and into the lateral ventricle of the brain of cats, produced acute autonomic effects followed by catatonia. These responses appeared to be altered or prevented by pretreatment with the ataraxic agents chlorpromazine, reserpine, and azacyclonol. We are indebted to Dr. Robert L. Craig and Mr. Robert G. Bianchi for implanting the cranial cannulae and to Dr. Kurt Rorig for synthesizing the azacyclonol.

Ocular Effects of Oral Contraceptives. I. Studies in the Dog

The administration of two oral contraceptives to female dogs for 5 years did not produce ocular lesions. Corneal and lenticular opacities occurred with equal frequency in control and treated groups, and fundic lesions, including papilledema, venous dilatation, and venous or arterial retinal thrombosis, were not produced by doses of Enovid-E or Ovulen 1, 10, and 25 times the human dose.