[Effect of the prostaglandin Nalador on progesterone and estrogen receptors in the pregnant uterus of guinea pigs].
Explore the source record for details and available documents.
Biomedical subjects
Publications and source records attributed to W Elger.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
A number of 11-substituted 19-norsteroids with inverse configuration at C-13 were synthesized. 11 beta-Aryl compounds in this series were found to possess antiprogestational and antiglucocorticoid activities.
The title compound was synthesized and tested for its biological activities. It showed neither antiprogesterone nor antiglucocorticoid properties.
The preparation of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid is described. This acid has good anti-inflammatory and analgesic activities without producing irritation in the gastrointestinal tract up to the highest tested dose.
Using the immunoperoxidase technique and specific goat anti-serum to uteroglobin, selective immunochemical staining products are localized in the epididymal epithelium of the caput and proximal corpus region, at the adluminal border of the cauda epididymidis and, as well known, in epithelial cells of the endometrium of pregnant and progesterone-treated rabbits. Specific staining is also seen on spermatozoa. A uteroglobin-like antigen has been similarly localized in alveolar and bronchial epithelial cells of the lung. Testis, prostate, seminal vesicle and ductus deferens do not seem to contain in their tissues immunoreactive uteroglobin-like antigens. Similarly, the uterus and ductus epididymidis of immature rabbits are devoid of immunoreactivity. The presence of uteroglobin-like antigens in tissues other than the endometrium, particularly the ductus epididymidis, stimulates new discussions on the function of this protein in reproductive physiology and fertility research.
Potent, albeit nonselective, smooth-muscle stimulant activity has been previously reported for 16-phenoxy- and 17-phenylprostaglandins, a finding that led to the design and development of the tissue-selective uterine stimulant sulprostone. As an extension of this work, analogues incorporating the 16-phenoxy and 17-phenyl substituents into the rigid indanyl, tetrahydronaphthyl, dihydrobenzofuryl, and dihydrobenzopyranyl ring systems were prepared and evaluated for uterine stimulant activity in vitro and diarrheal effects in vivo. Since these cyclic groups, with the exception of the indanyl, contain a chiral center, both optical antipodes were prepared. These studies demonstrate that ring size, heteroatom, and absolute configuration at C-16 are important determinants for potency and selectivity.
Prostaglandin E2 (Sulproston, S) can induce parturition and luteolysis during late pregnancy in the pig. We now tested whether Sulproston is able to interfere with the duration of the pig's estrous cycle. Sulproston was given i.m. in two injections (0.008 mg/kg each) at 12-hour-intervals to ten gilts day 10, to five gilts day 14 and to five gilts day 16 of the estrous cycle. Blood was collected shortly before and up to 48 hrs after the onset of treatment; further daily blood samples were taken from day 0 (1st day of standing heat) to the end of the cycle. Sulproston-administration did not shorten or lengthen the duration of the estrous cycle, nor were plasma-progesterone levels altered when compared to controls. In a second study five gilts received the tenfold amount of S on day 10 of the cycle. A significant decrease in plasma-progesterone (8.52 +/- 2.8 SEM ng, treatment vs. 32.95 +/- 1.86 SEM ng/ml, control) occurred on day 11, which had returned by day 16 to the level of controls (19.22 +/- 6.28 ng/ml vs. 26.75 +/- 2.10 SEM ng/ml, respectively). No alteration in cycle length occurred. Therefore the PGE2-analogue Sulproston - though luteolytic in late pregnancy - is neither luteolytic nor luteotrophic during the estrous cycle of the pig.
In male rats, fed for 10 weeks on a Torula yeast-based, low selenium and low vitamin E diet, the selenium level and the glutathione peroxidase activity in the blood and in several tissues decreased by 50 to 98% compared with animals that received the same basal diet supplemented with 0.25 mg Se/kg sodium selenite. In the testes, however, the selenium content did not differ from that of the control animals. Despite the low selenium levels in the extragonadal tissues and their increased requirement of this element due to the low vitamin E status, the selenium from an intravenously injected dose of sodium selenite was retained above all in the testes. After the removal of the pituitary gland, because of the decrease in the testicular mass and in the selenium content in the remaining testicular tissue, the amount of selenium in the testes was greatly reduced. After administration of pregnant mare's serum gonadotropin (PMS), due to the regeneration of the tissue and the simultaneous restoration of the selenium content, a relatively large amount of this element was shifted to the testes even though the selenium status in the other tissues was low. The results of these studies show that the selenium level in the male gonads is maintained by regulation mechanisms and that the supply of sufficient amounts of selenium to the testes has priority over the supply to other tissues.
Explore the source record for details and available documents.
At the 43rd day of pregnancy 6 Experimental guinea-pigs were treated orally with the PGE1-analogue, CP 48,630 (Pfizer), while 6 animals served as vehicle Controls. An average dose of 1.5 mg CP 48,630 compromized the conceptus and provoked abortion in 6.6 +/- 1.4 hours in all 6 Experimental guinea-pigs. The vehicle Controls, with all pregnancies continuing intact, had high P-levels in peripheral and uterine vein plasma, ovaries, placenta and uterine tissue and low PGF-levels in the uterine vein plasma. In contrast, in the Experimental animals the P-levels were significantly reduced and the PGF-levels elevated. Thus, the "PG-Impact" rapidly tipped the regulatory balance of pregnancy, compromized the conceptus (all fetuses were dead and the placentae discolored), and provoked the evolution of uterine activity culminating in abortion.
In an effort to develop tissue-selective prostaglandin analogues resistant to the metabolic inactivating pathways of the natural materials, hybrid compounds modified both at C-1 with a sulfonimide moiety and in the n-amylcarbinol side chain with substituted phenoxy groups were synthesized and evaluated in a variety of in vitro models. Several of these analogues exhibited potent, tissue-selective, uterine stimulant activity, a finding subsequently confirmed in clinical studies with one member of this series, N-(methanesulfonyl)-16-phenoxy-omega-tetranor-PGE2-carboxamide (CP-34089/ZK-57671, sulprostone).
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Sulprostone, a new synthetic prostaglandin E2-derivate has been tested for artificial abortion in 628 women with intact or disturbed pregnancies in all stages of gestation. Compared with other prostaglandins used for this purpose systemic side-effects were low and success-rate was high. Systemic routes of application (constant intravenous drop infusion, intramuscular injection) were evaluted to be more successful and conventient than the local ones (extra- and intraamniotic). Suppositories showed no clinical success. Based on our expereince recommendations for the treatment with sulprostone are given: Intramuscular injections for inducing early abortion or menstrual regulation (less than 6th week of pregnancy) without necessity of curettage and for cervical rpiening (less than 12th week of pregnancy) prior to curettage, constant intravenous drop infusion for induction of abortion in second and third trimester pregnancy.