[Prostaglandins in obstetrics].
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Biomedical subjects
Publications and source records attributed to V V Korkhov.
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Experiments with pregnant and nonpregnant rats have shown that aroxaprostol, a group F2 alpha prostaglandin, injected intravenously and intramuscularly in a dose of 50 micrograms/kg, stimulates the uterine bioelectric activity, increasing both the amplitude and frequency of biopotentials, this evidencing intensification of its contractility. Aroxaprostol has shown an abortive effect, that was related to the luteolytic effect of the drug, manifesting by reduction of progesterone level in the ovaries.
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Experiments on pregnant rats revealed that a combination of low doses of partusisten and clophelin (1.25 mg/kg and 0.15 ml of 0.001% solution, respectively) potentiated a tocolytic effect. A combination of prostenon and oxytocin given in half doses (0.15 mg/kg and 0.25 IU in 0.1 ml, respectively) summarized their stimulant effect on the myometrium. Premedication with partusisten (2.5 micrograms/kg) failed to change the stimulant effect produced by a combination of prostenon and oxytocin given in half doses.
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The synthesis of 2' beta-methyl-16 alpha,17 alpha-cyclohexanoprogesterone and its MM2 conformational analysis have been performed. The acetyl side chain was shown to have an unusual conformation with the torsion angle C13-C17-C20-O20 being -32.1 degrees. This conformation is by 5.4 kJ.mol-1 more stable than the usual one with the torsion angle 130.3 degrees. 2' beta-Methyl-16 alpha,17 alpha-cyclohexanoprogesterone proved to be inactive as a progestogen (pregnancy maintenance and McPhail tests). The lack of the activity may be due to the additional methyl group in D'-ring causing a change of the conformation of the 17 beta-acetyl side chain, thus hindering the formation of the conformation necessary for binding to the progesterone receptor.
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Progestagenic activity of a modified analog of progesteron-6 alpha-methyl-cyclogexan-[1', 2', 16 alpha, 17 alpha]-pregn-4-en-3,20-dion including into mecygepron composition has been studied; its activity is proved to be 5 times as great as that of progesteron at any way of administration. Mecygepron affects processes of ovogenesis and early embryogenetic development in rats. A decreased number of washed out embryos is observed, while the number of lutein bodies specific for intact rats remains the same, decelerated rate of cleavage and increased number of unfertilized ova. In the mechanism of the changes observed an essential role plays a decreased secretion of lutropin resulting in a prolonged estrol cycle and, evidently, in intrafollicular overmaturation of the ova, which loose their ability to be fertilized. Besides, the disturbed hormonal balance under mecygepron influence can affect the character of the oviduct and uterine contents and, thus, prevent the normal development of the fertilized gametes.
In vitro thymidine histoautoradiography was employed to measure labeling index in 18 moderately- and well-differentiated adenocarcinomas of the rectum before and after radiotherapy. After radiation labeling index fell from 13.8 +/- 3.2 to 3.9 +/- 1.4% while mitotic index--from 8 to 1%.
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