Assessment of hypertension control and clinical course of patients excluded from the SYMPLICITY HTN-3 trial.

The screening of patients referred for the Symplicity Renal-Denervation Catheter Therapy on Resistant Hypertension (SYMPLICITY HTN-3) trial was rigorous, with many found not eligible to participate. We investigate patients who were not included in the trial and evaluate their current hypertensive (HTN) therapy, control and clinical status. A retrospective review and telephone interview was performed 8-10 months postscreening on 45 patients and their referring providers who were ultimately not included.

Pharmacokinetics of anabolic steroids.

After an anabolic steroid is administered orally there is a rapid increase in its concentration in the blood in the following few hours. Excretion of the compound and its metabolites takes place via the urine and faeces, usually taking several days to completely pass through the system. Parenteral anabolic preparations, such as microcrystal suspensions, implants and solutions of nandrolone esters in a vegetable oil, are absorbed slowly.

Pharmacological studies with (7 alpha,17 alpha)-17-hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-one (Org OD 14).

A novel steroid, (7 alpha,17 alpha)-17-hydroxy-7-methyl-19-norpregn-5(10)-en-yn-3-one (code name Org OD 14), was found to possess concomitant weak oestrogenic, androgenic and progestational activities. The effects observed in other tests, viz. inhibition of ovulation in rats, prevention of bone loss following ovariectomy in rats and restoration of sex drive in castrated male rats, corresponded to this hormonal profile.

Comparison of the receptor binding properties of nandrolone and testosterone under in vitro and in vivo conditions.

Previous in vitro binding studies with androgen receptors in rat seminal vesicles (Toth M. and Zakar T., J.

Enzymatic microdetermination of free fatty acids in plasma of animals using paraoxon to prevent lipolysis.

A simple, sensitive and rapid enzymatic method, manual as well as automated, is described for the determination of free fatty acids in plasma of animals. Spontaneous hydrolysis of esterified fatty acids present in the plasma samples is prevented by adding a specific lipase-esterase inhibitor.

Implications of basic pharmacology in the therapy with esters of nandrolone.

Experiments in rats have shown that esters of nandrolone injected intramuscularly, are absorbed from the depot according to the kinetics of a first-order reaction. The nature of the fatty acid chain in the ester determines the half-life of the compound in the depot. Once released from the depot, the ester is rapidly hydrolyzed by the esterases in the plasma.

Effects of hyperprolactinemia on the accessory sexual organs of the male rat.

The growth-promoting effect of prolactin on the ventral prostate lobe, the anterior prostate lobe (or coagulating gland), and seminal vesicles has been studied before, during and after puberty in rats up to 5 months of age. Pituitaries from female rats were grafted under the renal capsule of 23-26-day-old male rats. Within 1/2 month substantial (five- to ten-fold) hyperprolactinemia occurred followed by a gradual decline; levels were still high 4 months after grafting.

Oestrogen binding proteins in the female genital tract.

We have estimated the binding characteristics of an oestrogen binding protein in the human vagina and in the human myometrium. The specificities of these binding proteins were analyzed in binding studies using competitors and ligands with different structural features representing the various elements considered to be of importance for binding. The specificity of an oestrogen binding protein in human myometrium was found to be similar to those of oestrogen binding proteins in human breast tumour tissue and in human MCF-7 cells.

Endocrinological studies with (7 alpha, 17 alpha)-17-hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-one (Org OD 14).

A novel steroid, (7 alpha, 17 alpha)-17-hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-one (Org OD 14), is described which has concomitant weak estrogenic, progestational and androgenic activities. This hormonal profile was demonstrated using various endocrinological tests and the results were evaluated in terms of well-known reference compounds. It has been well established that combinations of estrogens, androgens and progestagens exert positive or synergistic effects on certain target organs, e.

Binding of progestagens to receptor proteins in MCF-7 cells.

With the aim of finding an explanation for the biological properties of progestagens currently used for contraceptive purposes, we have assessed their specificity for progesterone, androgen and oestrogen receptors in MCF-7 cells. The specificity of progestagens for the progesterone receptors in the cytosol fraction of MCF-7 cells was similar to that for progesterone receptors in human and rabbit myometrial cytosol but different from that for the progesterone receptor in rat myometrial cytosol. At 37 degrees C the relative affinity of 3-keto-desogestrel, the major metabolite of desogestrel, for the progesterone receptor in intact MCF-7 cells was twice that of levonorgestrel and Org 2058, three times that of medroxy-progesterone acetate (MPA), 4.

Endocrinological studies with desogestrel.

13-Ethyl-11-methylene-18,19-dinor-17 alpha-pregn-4-en-20-yn-17-ol (Org 2969, desogestrel) is a new progestational steroid which has been developed for application in oral contraceptives. In assays for characteristic progestational effects (McPhail test, McGinty test, Deciduoma test and Antifertilization test) and in tests for inhibition of ovulation, desogestrel is highly active after oral administration and more potent than the structurally related reference compounds norethisterone and levonorgestrel. The same holds for its anti-oestrogenic activity.

The pharmacology of oestriol.

The potency ratio of oestriol compared to oestradiol or to ethinyloestradiol depends on the experimental conditions of the test. If a sufficiently high level of oestriol is maintained in a target tissue, either by infusion or by frequent administration, this steroid is capable of eliciting a full oestrogenic effect. At the target tissue, oestriol is a short-acting rather than a weak-acting oestrogen.

A quantitative test for oestrogenic activity using rat endometrium lactate dehydrogenase.

In ovariectomized rats treatment with ethinyloestradiol (EOe) po started 1 week after castration and given for 4 days resulted in an increase of endometrial lactate dehydrogenase per DNA (LDH/DNA). The lambda of the dose-response curve was 0.178.

Comparison of the metabolism of testosterone undecanoate and testosterone in the gastrointestinal wall of the rat in vitro and in vivo.

The metabolism of testosterone undecanoate (TU) and testosterone (T) is studied in the gastrointestinal wall of the rat in vitro. A comparison is made with the in vivo metabolism of these compounds in the rat. The major metabolite first appearing during incubation of TU with the small intestine is T.

Oestrogenic activity of oestradiol-decanoate after oral administration to rodents.

Oestradiol-decanoate, dissolved in arachis oil and orally administered to rodents, produces oestrogenic effects. Compared on a molecular basis the ester has 0.1-1.

Conception, contraception and misconception.

Because of Dr. G. A.

The pharmacology and metabolism of testosterone undecanoate (TU), a new orally active androgen.

Testosterone undecanoate (TU), either dissolved in arachis oil or as micro-crystal suspension, displays androgenic activity on oral administration to rats in the Hershberger test. The solution in arachis oil is more active than the crystal suspension. When [3H]TU is administered orally to rats, most of it is metabolized in the intestinal wall.

Metabolites of lynestrenol acetate in the bile of rats after intravenous administration; a comparison with lynestrenol.

Some aspects of the metabolism of lynestrenol acetate, an orally active contraceptive compound, were studied in female rats. Lynestrenol acetate is stable in gastric and intestinal juice in vitro. After intravenous administration of lynestrenol acetate and lynestrenol with a -14C label in the nucleus approximately 40% of the administered radioactivity was excreted in the bile within 90 min.