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1.
A sensitive and relatively specific radioimmunoassay for 15 (S) 15 methyl prostaglandin F2α was used to determine the levels of the drug in amniotic fluid after it had been injected intra-amniotically for termination of second trimester pregnancy. The disappearance of the free acid (tham salt) and methyl ester of the prostaglandin analogue were similar. The results of this preliminary study suggest that the drug rapidly equilibrates in the fluid and this is followed by a slow removal from the amniotic sac. A comparison with a similar study with PGF2α, revealed that the analogue had a longer half-life in the amniotic fluid. 相似文献
2.
E.K. Weir M.R.C.P. J.T. Reeves M.D. W. Droegemueller M.D. R.F. Grover M.D. 《Prostaglandins & other lipid mediators》1975,9(3):369-376
Intramuscular injection of the 15-methyl analogue of prostaglandin F2α (15-me-PGF2α) is being used to initiate second trimester abortion. The natural prostaglandin F2α (PGF2α) is a known pulmonary pressor agent but there is little information about the cardiovascular effects of the analogue. Consequently, we compared the hemodynamic responses to the two forms in twenty-three anesthetized dogs. Given I.M. or I.V. 15-me-PGF2α produced a greater and more sustained rise in pulmonary arterial pressure than PG F2α. Intramuscular 15-me-PGF2α also elicited a more prolonged increase in pulmonary vascular resistance than prostaglandin F2α given I.M. or I.V. The methyl analogue (I.M. or I.V.) causes a greater initial fall in systemic arterial oxygen tension and cardiac output, and a greater increase in systemic resistance than I.M. PG F2α Breathlessness seen during abortion induced by prostaglandin F2α or its methyl analogue may be caused by acute pulmonary hypertension in addition to bronchoconstriction. 相似文献
3.
A sensitive and relative specific radioimmunoassay for 15 (S) 15 methyl prostaglandin F2α has been developed to enable the measurements of the concentrations of the drug in biological fluids after its administration for therapeutic abortion. The precision, accuracy and specificity of the assay are described. 相似文献
4.
The present study has been performed to investigate how PGs would participate the hatching process. Effects of indomethacin, an antagonist to PGs biosynthesis, on the hatching of mouse blastocysts were examined in vitro. Furthermore, it was studied that prostaglandin E2 (PGE2), prostaglandin F2α (PGF2α) or 6-keto-prostaglandin F1α (6-keto-PGF1α) were added to the culture media with indomethacin. (1) The hatching was inhibited by indomethacin yet the inhibition was reversible. (2) In the groups with indomethacin and PGE2, no improvement was seen in the inhibition of hatching and the inhibition was irreversible. (3) In the groups with indomethacin and PGF2α, inhibition of hatching was improved in comparison with the group with indomethacin. (4) In the groups with indomethacin and 6-keto-PGF1α, no improvement was seen. The above results indicated that PGF2α possibly had an accelerating effect on hatching and a high concentration of PGE2 would exert cytotoxic effect on blastocysts. 相似文献
5.
Termination of second trimester pregnancy with intra-amniotic administration of 15 (S) 15 methyl prostaglandin F2α (15 me F2α) was attempted in fifty patients. One group (25 patients) was given 1 mg of the analogue and the other group received 2.5 mg. The abortifacient efficacy of 15 me F2α was similar in both groups; over 90% of the patients aborted with a single dose. There was a higher incidence of vomiting, diarrhoea and incomplete abortions in the group treated with 2.5 mg 15 me F2α. Although the mean injection-abortion interval in the 2.5 mg group was shorter, it is concluded that intra-amniotic administration of 1 mg 15 me F2α provides a better regime, giving high efficacy with a single dose, a low incidence of side effects and greater safety in case of inadvertent entry of the intra-amniotic dose into systemic circulation. 相似文献
6.
Michael C. Koss 《Prostaglandins & other lipid mediators》1976,12(6):997-1004
Prostaglandin F2α (5μg/kg, i.v.) causes an increase in pulmonary arterial pressure, decrease in systemic arterial pressure, and reflex bradycardia in the anesthetized cat. The same dose of the 15-methyl analogue of PGF2α produces the same triad of effects but of greater magnitude and duration. Although prostaglandins F1α, F2β and F1β also cause the same cardiovascular effects as F2α, there is a decrease in potency for all parameters measured, with PGF2α>PGF1α>PGF2β>PGF1β. When compared to the actions of PGF2α in producing an increase in pulmonary arterial pressure, PGs F1α, F2β and F1β were less potent by approximately 10, 100, and 1000 fold respectively. 相似文献
7.
Shiro Ohki Katsuhiro Imaki Fumio Hirata Toshio Hanyu Nobuhiko Nakazawa 《Prostaglandins & other lipid mediators》1974,6(2)
Radioimmunoassays for measuring prostaglandin F2α (PGF2α) and 5α, 7α-dihydroxy-11-keto tetranorprosta-1,16-dioic acid, PGF2α-main urinary metabolite (PGF2α-MUM), with 125I-tyrosine methylester amide (TMA) of PGF2α and PGF2α-MUM were developed.Antibody to PGF2α was produced in rabbits immunized with conjugates of PGF2α coupled to bovine serum albumine. Antibody to PGF2α-MUM was also produced in rabbits immunized with conjugates of PGF2α-MUM coupled to bovine serum albumin.PGF2α-125I-TMA had an affinity to antiserum to PGF2α. PGF2α-MUM-125I-TMA also responded to antiserum to PGF2α-MUM. 相似文献
8.
Prostaglandin (PG)F2α, E2, D2 and 6-keto-F1α were determined in human cerebrospinal fluid by a mass spectrometric technique. The samples were obtained from 12 patients with suspected intracranial disease. A 64 fold variation in PG levels was observed. The major PG was 6-keto-F1α (0.12–15 ng/ml). PGF2α and PGE2 were present in lower concentrations PGD2 was below the level of detection (0.05 ng/ml) except in one patient with extremely high total levels of PGs. 相似文献
9.
Hideya Hayashi Seiji Ito Teruo Tanaka Manabu Negishi Hideo Kawabe Yokohama Hiromitsu Kikuko Watanabe Osamu Hayaishi 《Prostaglandins & other lipid mediators》1987,33(4)
In view of the recent finding that prostaglandin D2 is stereospecifically converted to 9α,11β-prostaglandin F2, an isomer of prostaglandin F2α, a highly specific and sensitive radioimmunoassay for 9α,11β-prostaglandin F2 was developed and applied to determine the content of this prostaglandin in various rat tissues. Antisera against 9α-11β-prostaglandin F2 were raised in rabbits immunized with the bovine serum albumin conjugate, and [3H]9α,11β-prostaglandin F2 was enzymatically prepared from [3H]prostaglandin D2. The assay detected 9α,11β-prostaglandin F2 over the range of 20 pg to 1 ng, and the antiserum showed less than 0.04% cross-section with prostaglandin F2α, prostaglandin F2β and 9β,11β-prostaglandin F2. To avoid postmortem changes, tissues were frozen in liquid nitrogen immediately after removal. The basal level of 9α,11β-prostaglandin F2 was hardly detectable in various tissues of the rat examined, including spleen, lung, liver and brain; although it was found to be 0.31 ± 0.06 ng/g wet weight in the small intestine. During convulsion induced by pentylenetetrazole, enormous amounts of prostaglandin D2 (ca. 180 ng/g wet weight) and prostaglandin F2α (ca. 70 ng/g) were produced in the brain; however, 9α,11β-prostaglandin F2 was detected neither there nor in the blood. This result demonstrates that the conversion to 9α,11β-prostaglandin F2 is a minor pathway, if one at all, of prostaglandin D2 metabolism in the rat brain. 相似文献
10.
Plasma levels of prostaglandin F2α (PGF2α) in female red-sided garter snakes (
) were measured at intervals after mating or exposure to males. PGF2α levels increased significantly within 15 minutes of mating and peaked 6–24 hr after mating. Females that did not mate, but received similar amounts of male courtship, had levels of PGF2α significantly lower than those of females that mated. These results extend previous findings that unmated female garter snakes injected with PGF2α exhibit sexual behavior characteristics of females that have mated. Together these data indicate that female garter snakes elaborate PGF2α in response to stimuli associated with mating and that PGF2α has a functional role in inducing post-mating declines in sexual behavior of this species. 相似文献
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11.
In humans eicosapentaenoic acid can be converted to 3-series prostaglandins (PGF3α, PGI3, and PGE3). Whether 3-series prostaglandins can protect the gastric mucosa from injury as effectively as their 2-series analogs is unknown. Therefore, we compared the protective effects of PGF3α and PGF2α against gross and microscopic gastric mucosal injury in rats. Animals received a subcutaneous injection of either PGF3α or PGF2α in doses raning from 0 (vehicle) to 16.8 μmol/kg and 30 min later they received intragastric administration of 1 ml of absolute ethanol. Whether mucosal injury was assessed 60 min or 5 min after ethanol, PGF3α was significantly less protective against ethanol-induced damage than PGF2α. These findings indicate that the presence of a third double bond in the prostaglandin F molecule between carbons 17 and 18 markedly reduces the protective effects of this prostaglandin on the gastric mucosa. 相似文献
12.
C. N. Hensby 《Prostaglandins & other lipid mediators》1974,8(5):369-375
Prostaglandins E2 and D2 were both converted to prostaglandin F2α (9α, 11α) by an enzyme present in sheep blood. Neither the 9β, 11α epimer nor the 9α, 11β epimer was produced from PGE2 or PGD2 respectively. The rate of reduction was measured using isotope dilution (D4 PGF2α) and multiple-ion detection gas chromatography-mass spectrometry. 相似文献
13.
T.G. Kennedy 《Prostaglandins & other lipid mediators》1976,12(6):1061-1071
Experiments were performed to determine if prostaglandins were able to reduce cervical tone in the rat. Cervical tone was assessed indirectly by measuring uterine luminal fluid accumulation in ovariectomized rats implanted subcutaneously with Silastic capsules containing crystalline estradiol-17β. When given subcutaneously in separate experiments, 16,16-dimethyl-prostaglandin E2, methyl ester, and 15(S)-15-methyl-prostaglandin F2α, analogous of prostaglandins E2 and F2α, respectively, caused the loss of uterine luminal fluid. Fluid accumulation in uterine horns ligated at the cervical end did not differ in control and treated rats, whereas in non-ligated horns the prostaglandin analogues reduced fluid accumulation, suggesting the cervix as their site of action. For both prostaglandin analogues, the effects on uterine luminal fluid accumulation were seen within 45 min of administration and were related to the dose administered. The effects of submaximal doses of the analogues were additive. These results suggest that prostaglandins are able to reduce cervical tone in the estrogen-treated rat. 相似文献
14.
John W. Wilks 《Prostaglandins & other lipid mediators》1977,13(1):161-170
The naturally-occurring metabolite of prostaglandin F2α, 15-keto prostaglandin F2α (15-keto PGF2α), elicited rapid and sustained declines in serum progesterone concentrations when administered to rhesus monkeys beginning on day 22 of normal menstrual cycles. Evidence for luteolysis of a more convincing nature was obtained in studies where a single dose of 15-keto PGF2α was given on day 20 of ovulatory menstrual cycles in which intramuscular injections of hCG were also given on days 18–20; serum progesterone concentrations fell precipitously in monkeys within 24 hours following intramuscular administration of 15-keto PGF2α. However, corpus luteum function was impaired in only 4 of 11 early pregnant monkeys when 15-keto PGF2α was administered on days 30 and 31 from the last menses, a time when the ovary is essential for the maintenance of pregnancy. Gestation failed in 2 additional monkeys 32 and 60 days after treatment with 15-keto PGF2α, but progressed in an apparently normal manner in the remaining 5 animals. Two pregnant monkeys treated with 15-keto PGF2α on day 42 from the last menstrual period, a time when the ovary is no longer required for gestation, continued their pregnancies uneventfully. Corpus luteum function was not impaired in 9 control monkeys which received injections of vehicle or hCG at appropriate times during the menstrual cycle or pregnancy. 相似文献
15.
Earlier work had shown that the lactogen, LTH and HPL, foster testosterone binding by the prostate. This study was undertaken to see if prostaglandin F2α would oppose the effect of the lactogen on the prostate as it does the luteotrophic action of the hormone on the corpus luteum. When it was found instead that the PGF increases steroid binding and that its interaction with lactogen was neither antagonistic nor additive, attention was directed to further characterization of the prostaglandin's effect. A dosage/response study of F2α alone showed that concentrations of 4 ng/ml and 40 ng/ml increased binding but that 400 ng/ml did not. Glands with stromal hyperplasia and/or inflammation were more responsive than those with epithelial hyperplasia. Assays of water extracts of the tissue revealed concentrations of about 340 ng of F2α per gram fresh weight and that the concentration varied inversely as the β-glucuronidase activity. If the enzyme level is considered an index of the epithelial cell density within the specimen, the inverse relationship suggests a non-epithelial (stromal) site of prostaglandin concentration. 相似文献
16.
M.D. Nelson Burton Shirley Carlile M.D. William Jubiz 《Prostaglandins & other lipid mediators》1975,10(6):667-674
Plasma prolactin and F-prostaglandins (PGF) were measured in anesthetized male Sprague-Dawley rats before and at 15, 30, 45 and 60 minutes following i.v. injection of either PGF2α (4 mg/kg), chlorpromazine, 1 mg/kg or chlorpromazine (1 mg/kg) after pretreatment with i.p. indomethacin (2 mg/kg). Following PGF2α administration, plasma prolactin levels increased significantly only at 15 and 30 minutes in spite of extremely high PGF levels throughout 60 minutes. Besides the expected rise in plasma prolactin, chlorpromazine caused a transient but statistically significant increase in PGF. Indomethacin blocked the chlorpromazine-induced PGF rise but not prolactin increase. Animals stressed with ether anesthesia showed elevation of plasma prolactin, which was not blocked by indomethacin although PGF concentration fell. These results indicate that PGF2α can stimulate prolactin release. This effect does not appear to be physiologic since very high PGF levels are required. Furthermore, blockade of prostaglandin synthesis by indomethacin does not prevent the release of prolactin in response to chlorpromazine or stress. Our findings do not support a possible role of PGFs as intermediaries in prolactin release. However, it is possible that PGFs may work through other mechanisms not investigated in our study. 相似文献
17.
C. Patrono G. Ciabattoni D. Grossi-Belloni 《Prostaglandins & other lipid mediators》1975,9(4):557-568
The release of PGF1α and PGF2α from superfused blood platelets was studied by the combined use of two radioimmunoassay systems with different specificities. PGF1α only accounted for approximately 30% of the total immunoreactivity. A substantially similar pattern of release was obtained with platelets of rat and human origin, although the latter released considerably lower amounts of both compounds. Indomethacin, Fenoprofen, Ditazole and Aspirin all inhibited PGF2α release from rat platelets in descending order of potency. Hydrocortisone was practically inactive. The release of PGF1α and PGF2α was inhibited to the same extent by both Indomethacin and Fenoprofen. Moreover, a quite similar inhibitory effect by the same drug on rat and human platelets was found in preliminary experiments. In agreement with a previous similar finding, Aspirin displayed a higher inhibitory activity than that reported in other tissues. The use of superfused platelets seems to provide a simple and reproducible model for studying pharmacologic influences upon PG formation. 相似文献
18.
Martin A. Wasserman 《Prostaglandins & other lipid mediators》1975,9(6):959-973
The airway and lung dynamics of prostaglandin F2α (PGF2α) and three of its metabolites were examined in the spontaneously-ventilated, pentobarbital anesthetized dog. Changes in expiratory flow rate, tidal volume, respiration rate, lung resistance and dynamic lung compliance were evaluated and compared quantitatively. In a dose range of 0.3–3.0 μg/kg i.v., PGF2α and its 13,14-dihydro metabolite were found to be exceptionally potent agents. This metabolite was approximately twice as potent as PGF2α on most parameters studied. Two other metabolites, 15-keto-PGF2α and 15-keto-13,14-dihydro-PGF2α, were only slightly effective, even in a dose range of 1.0–30.0 μg/kg i.v. These latter two metabolites produced dose-response curves with significantly shallower slopes than PGF2α and were shown to be at least thirty-five times less potent than the parent compound. Therefore, oxidation of PGF2α at the carbon-15 position by 15-hydroxy prostaglandin dehydrogenase appears to produce compounds with minimal
bronchopulmonary activity. 相似文献
19.
A viroimmunoassay of PG F2α is presented here. By a modification of the technique used by Dray et al. (3), it allowed us to measure as low as one picogram of PG F2α. It seems that such a sensitive assay might be usefull for many purposes in the prostaglandin field. 相似文献
20.
The cerebral cortical action of prostaglandin F2α (PGF2α) has been determined by recording the effects of intracarotid injections of PGF2α on cerebral evoked potentials. PGF2α differentially reduced cortical evoked potentials. The cortical action of PGF2α appeared to be qualitatively identical with that of norepinephrine (NE) but weaker. A protection of the cortex from the inhibitory action of NE by a preceding dose of PGF2α was demonstrated. The actions of both PGF2α and NE appear to be on the same or related postsynaptic receptors. The actions described were at doses that did not reduce oxygen availability. PGF2α may act as a modulator of adrenergic transmission in the cortex. The intracellular recording in the companion paper supplies the further critical evidence that PGF2α has a synaptic inhibitory action. 相似文献