HEMMUNG DER UTERUSWIRKUNG VON OXYTOCIN DURCH WASSERLÖSLICHE STEROIDE

1965 ◽  
Vol 48 (4) ◽  
pp. 656-663 ◽  
Author(s):  
R. Hempel ◽  
F. Neumann

ABSTRACT Various water-soluble steroids were tested in vitro on the isolated rat uterus for their oxytocin-antagonistic activities. Using progestional agents (19-nor-17α-hydroxyprogesterone-17-hemisulfate-sodium, Δ1,6-17α-hydroxyprogesterone-17-hemisulfate-sodium) oestrogens (oestrone-hemisulfate-sodium), and corticoids (dexamethasone-21-hemisulfate-sodium) it was possible to suppress both the oxytocin-induced single contraction and the spontaneous rhythm intensified by oxytocin. Except for the Δ1,6-17α-hydroxyprogesterone-sulfate-sodium, these compounds were unable to inhibit the single contractions of the uterus induced by serotonin, bradykinin and barium chloride. Following the administration of a mixture of the different watersoluble steroids an additional effect was observed. Based on these results, it can be assumed that the oxytocinantagonistic effect represents an activity per se which is peculiar to certain steroid structures.

Metabolism ◽  
1986 ◽  
Vol 35 (7) ◽  
pp. 608-613 ◽  
Author(s):  
J.P. Riou ◽  
M. Beylot ◽  
M. Laville ◽  
L. De Parscau ◽  
J. Delinger ◽  
...  

1980 ◽  
Vol 87 (1) ◽  
pp. 153-159 ◽  
Author(s):  
D. G. JUDSON ◽  
SARAH PAY ◽  
K. D. BHOOLA

Porcine relaxin produced a rapid, dose-related rise of cyclic AMP values in rat uterine tissue incubated in vitro. In time-course experiments, peak cyclic AMP concentrations were observed in the uterine slices at 5 min; subsequently the values fell, at first rapidly and then more slowly with the tissue concentration remaining significantly raised at 15 min. Levels of cyclic GMP in the same tissue slices were not significantly altered by relaxin. Furthermore, no increase in basal cyclic AMP values was measured in control slices prepared from the rat heart or jejunum. An increase in cyclic AMP concentration comparable to that found in the rat uterus was observed in slices of porcine uterus and cervix but not of vagina when they were stimulated with porcine relaxin. Our results suggest that the hormonal action of relaxin on the uterus and cervix is mediated through receptors linked to the enzyme, adenylate cyclase.


1964 ◽  
Vol 206 (6) ◽  
pp. 1207-1212 ◽  
Author(s):  
Duncan Thomas ◽  
Myron Stein ◽  
Genzo Tanabe ◽  
Vishram Rege ◽  
Stanford Wessler

In 19 dogs, the release of autologous venous thrombi to the lungs resulted in bronchoconstriction, with a rapid rise in the total lung resistance and a fall in the lung compliance. The respiratory rate and arterial-alveolar CO2 tension difference also increased significantly. The administration of either heparin or a 5-HT antagonist completely prevented the bronchoconstriction, without affecting either the respiratory rate or arterial-alveolar CO2 tension difference. Bronchoconstriction resulting from direct 5-HT infusion was not prevented by heparin, nor was the contraction of an isolated rat uterus in response to 5-HT. However, 5-HT was not released from canine platelets by thrombin in vitro, in the presence of heparin. The evidence suggests that bronchoconstriction in the dog due to autologous pulmonary emboli results from thrombin-induced 5-HT release, and that heparin, by its antithrombin action, prevents this release.


1965 ◽  
Vol 48 (4) ◽  
pp. 645-655 ◽  
Author(s):  
F. Neumann ◽  
R. Hempel

ABSTRACT In vivo Assays: Oil and water-soluble steroids have been investigated for their oxytocin-antagonism in pregnant rabbits treated with oxytocin. The uterine immobilizing effect is more marked after treatment with hydroxyprogesterone-derivatives than following the administration of 19-nor-testosterone-derivatives. In vivo investigations on the latent period show the following: after intramuscular administration of a micro-crystalline suspension, the latent period is 2–3 hours and is at least three hours following the administration of an oily solution. The maximum activity of the oily solution is obtained after 6 hours at the earliest and this occurs even later following the administration of the micro-crystalline suspension. There is no difference in latent period between the intravenous and intramuscular administration of micro-crystalline suspension. The water-soluble progestational agents examined in in vivo tests are 17-hemi-sulphate-esters of various 17α-hydroxyprogesterone-derivatives, Except for one compound* it was possible to prevent the oxytocin induced abortion with all substances in vivo. However, to achieve the inhibitory effect, very high doses of the water-soluble progestational agents were required. The duration of activity of these substances is limited to 2–3 hours. In vitro Assays: In addition, the water-soluble compounds were, with one exception also tested in vitro on the isolated rat uterus. It was possible to suppress the oxytocin-induced single contraction of the rat uterus.


1977 ◽  
Vol 165 (1) ◽  
pp. 43-47 ◽  
Author(s):  
C R Snell ◽  
D G Smyth

[8-Lysine]oxytocin was synthesized on a solid support and possessed an oxytocic activity of 100 +/- 6 units mumol on the isolated rat uterus. The epsilon-carbamoyl, epsilon-3-carboxypropionyl and epsilon-3-carboxybutryl derivatives were prepared and had uterotonic activities of 400, 55 and 50 units/mumol respectively. [8-Lysine]oxytocin was coupled unambiguously through the epsilon-amino group to the carboxyl groups of carboxymethylated dextrans or epsilon-3-carboxypropionly-gelatin. The macromolecular oxytocins were water-soluble and retained signigicant oxytocic activity. [8-Lysine]oxytocin should prove a useful ligand for affinity chromatography of oxytocin-binding proteins.


1964 ◽  
Vol 47 (3_Suppl) ◽  
pp. S37-S52 ◽  
Author(s):  
K. N. Agarwal ◽  
H. Carstensen

ABSTRACT The influence of different factors upon the affinity of human erythrocytes for corticosteroids was studied in vitro in a phosphate buffer. Properties connected with the erythrocytes per se were found to be of importance for the binding of the steroids. Methods were developed for extraction, separation and estimation of water soluble esters of corticosteroids.


2018 ◽  
Vol 27 (2) ◽  
pp. 179-185 ◽  
Author(s):  
Bojana Miladinovic ◽  
Suzana  Brankovic ◽  
Milica Kostic ◽  
Milica Milutinovic ◽  
Nemanja Kitic ◽  
...  

Objective: The purpose of this study was to investigate the relaxative effects of blackcurrant juice on the gastrointestinal smooth muscle in vitro. Materials and Methods: Berries of the blackcurrant cultivar Ometa were used for the preparation of the juice used. The spasmolytic activity of blackcurrant juice was tested on rat ileum isolated from male Wistar rats by monitoring its influence on spontaneous contractions, as well as contractions induced by potassium chloride (KCl), barium chloride (BaCl2), calcium chloride (CaCl2), and acetylcholine (Ach). The results are expressed as the mean ± standard deviation obtained in 6 measurements and statistical significance was determined by the Student t test, with p < 0.05 taken as significant. Results: The blackcurrant cultivar Ometa significantly reduced the frequency and the amplitude of spontaneous contractions (57.94 ± 3.44%) and Ach-induced contractions (42.74 ± 5.36%; p < 0.05) of the isolated rat ileum. Cumulative concentrations (0.01–3 mg/mL) of the Ometa juice also reduced contractions of the isolated rat ileum stimulated by KCl (51.46 ± 6.87%), CaCl2 (57.54 ± 6.47%), and BaCl2 (58.54 ± 10.55%). The inhibitory effects of the juice were proportional to the applied concentration. Conclusion: The antispasmodic effect of Ometa cultivar shows that common gastrointestinal disorders could be treated by the functional food.


1968 ◽  
Vol 20 (03/04) ◽  
pp. 588-595 ◽  
Author(s):  
E. B Goodsell ◽  
R. A Krause ◽  
E. T Kimura

SummaryUbiquin (oligo-3-(N-methylmorpholinium)-l,2-propylene oxide chloride) is a stable, water soluble, active heparin antagonist producing prompt neutralization when administered in a 1:1 ratio to rats and dogs. Initial studies indicate that it is devoid of any effect on coagulation per se; nor are there any obvious side effects manifested during the process of neutralization. The acute toxicity is less than that of other compounds in use: toluidine blue, protamine and hexadimethrine.


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