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1.
Antibodies against 15 keto PGF2α and 13,14 dihydro 15 keto PGF2α were produced in goats and rabbits using the appropriate prostaglandin protein conjugate. Tritium labeled 15-keto, and 13,14 dihydro 15-keto PGF2α were prepared from 3H-PGF2α. These antibodies and 3H-labeled compounds were used to develop radioimmunoassays for the respective F2α metabolites. The antibodies had relatively little cross-reactivity (≤0.1%) with the parent F2α molecule. Infusion of PGF2α in monkeys increased 15-keto-h2 levels 10–20 fold higher than PGF2α in peripheral plasma. The levels of this metabolite were not altered detectably during clotting, indicating relatively slow rates of PGF2α metabolism in vitro. These assays should be useful to follow release rates of exogenous prostaglandins from various formulations and delivery systems, and in vivo tissue synthesis of PGF2α, where low levels preclude measuring the parent compound. 相似文献
2.
Prostaglandin F2α and E2 contents in human cerebrospinal fluid were determined by the radioisotope dilution method. The mean values of PGF2α and PGE2 of men were 9.8±0.87 ng/ml and 6.5±1.39 ng/ml, respectively. Those of women were 8.3±1.4 ng/ml and 6.9±1.72 ng/ml, respectively. The correlation between age and PG was significantly with PGE2 of men and with PGF2α of women. 相似文献
3.
Pentti A. Järvinen Sirkka Pennanen Pekka Ylöstalo 《Prostaglandins & other lipid mediators》1973,3(4):491-504
Legal abortion was induced by intrauterine administration of prostaglandin F2α in 115 patients during the 11th – 20th week of pregnancy. An intra-amniotic method was used in 61 of the cases, an extra-amniotic one in 54 cases. The average total dose administered was 35.1 mg (range 5 – 65 mg) in the intra-amniotic group, and 6358 μg (range 1500 – 14000 μg) in the extra-amniotic group. Abortion rate was 92 % in the intra-amniotic material and 72 % in the extra-amniotic material, and side-effects, mainly gastrointestinal irritation, were noted in 74 % of the intra-amniotic cases and 54 % of the extra-amniotic ones. If total doses of 4750 μg or more were administered in the extra-amniotic cases, abortion rate went up to 80 %, but the frequency of side-effects simultaneously increased to 64 %. No serious complications occurred. Intrauterine prostaglandin induction is well suited therapeutic abortions in the second trimester, and the intra-amniotic technique is more practicable than the extra-amniotic one. The latter is applicable in cases where the puncture of the amniotic cavity is difficult to achieve, e.g. in cases of fetus mortuus and hydatiform mole. 相似文献
4.
William E Hoffman Marc L Leavitt Ronald F Albrecht David J Miletich 《Prostaglandins & other lipid mediators》1981,21(6):899-904
Prostacyclin (PGI2), prostaglandin E2 (PGE2) and prostaglandin F2∝ (PGF2∝) were tested here in unanesthetized male Sprague-Dawley rats for their effects on the cardiovascular system as mediated by the Central nervous system. Cannulae were chronically implanted into the third cerebral ventricle, femoral arteries and femoral veins of rats. Both PGE2 and PGF2∝ induced increased arterial blood pressure and tachycardia by an action on the central nervous system. The changes seen with PGE2 were larger than those observed with PGF2∝. Only transient depressor effects were seen with PGI2 and these changes appeared to be due to the leakage of the substance into the peripheral vascular system. 相似文献
5.
Shiro Ohki Katsuhiro Imaki Fumio Hirata Toshio Hanyu Nobuhiko Nakazawa 《Prostaglandins & other lipid mediators》1974,6(2):137-148
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
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7.
Antibodies against the main urinary metabolite of PGF2α in the human, 5α,7α-dihydroxy-11-ketotetranorprosta-1,16-dioic acid, were raised in rabbits. The compound was coupled selectively in the ω position to bovine serum albumin prior to injection. The resulting antibodies did not distinguish between tetranor compounds varying only in structure at the ω carbon, and thus the assay could be used also for other metabolites of PGF2α, e.g. the main urinary metabolite in the guinea pig, 5α,7α-dihydroxy-11-ketotetranorprostanoic acid. Labeled ligands for the assays were prepared either by injection of |17,18-3H|-PGF2α into humans after several days' treatment with indomethacin, or by incubation of |17,18-3H|-15-keto-13,14-dihydro-PGF2α with mitochondria from rat liver. The sensitivity of the assay was 10 pg or 4 pg with these two preparations, respectively.The assay was employed for a number of measurements: normal daily excretion in a number of humans; excretion of urinary metabolites during treatment with prostaglandin synthetase inhibitors in human subjects, or after intravenous injection of PGF2α; excretion during human pregnancy; and prostaglandin production in the guinea pig during normal estrous cycles and pregnancies and after estrogen treatment.The results of these studies were in several cases compared to similar measurements earlier performed using mass spectrometric methods, and were found to agree well. Thus, this radioimmunoassay provides a simple and accurate method for estimating prostaglandin production, particularly suitable for long-term studies and for cases where repeated blood sampling must be avoided. 相似文献
8.
W. Schramm L. Bovaird M.E. Glew G. Schramm J.A. McCracken 《Prostaglandins & other lipid mediators》1983,26(3):347-364
In view of the pulsatile nature of PGF2α secretion from the ovine uterus at the time of luteolysis, experiments were designed to examine the effect of pulsed infusions of PGF2α on luteal function and to re-examine the minimal effective levels of PGF2α required to induce luteolysis. To mimic physiological conditions, hour-long infusions of PGF2α in increasing concentrations were given either 4 times in 19 h or 5 times in 25 h into the arterial supply of the autotransplanted ovary in conscious sheep on day 12 of an induced cycle. Blood flow and progesterone secretion rate from the ovary were used to monitor directly the luteolytic effect of administered PGF2α. The concentration of LH in peripheral plasma was measured throughout each infusion experiment and the presence of a preovulatory peak of LH was used as an indicator of the permanence of luteal regression. Four pulses of PGF2α in 19 h caused complete corpus luteum regression in only 1 of 4 animals whereas the addition of a fifth pulse (5 pulses in 25 h) caused permanent regression in 4 out of 4 animals. Infusion of 5 hour-long pulses of saline or PGF2α at a rate of <0.04 μg/h did not induce permanent suppression of progesterone secretion. The average total effective dose of PGF2α required to induced luteal regression when given as 5 pulses was 1/40th of the amount currently regarded as the minimal effective one when given by constant infusion into the ovarian artery. In another series of experiments the luteolytic effect of a single hour-long pulse of 0.1 μg/h PGF2α given daily for either 3 or 4 days was investigated. A significant fall (ANOVA, F0.01) in progesterone secretion rate, which reached a nadir at , was followed by a recovery of progesterone secretion rate. Permanent luteal regression did not occur with this protracted regimen, suggesting that a relatively short pulse frequency of PGF2α over a minimal period of 24 h is a necessary condition for physiological regression of the corpus luteum in sheep. 相似文献
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The inhibition of human platelet aggregation produced by PGF2α is not specific for thromboxane A2 mimetics. Aggregation waves induced by PAF and thrombin are also inhibited by PGF2α (8 μM); ADP is unaffected. These effects are still seen in platelets from aspirin-treated donors and platelets desensitized to thromboxane-like agonists (e.g. 11,9-epoxymethano PGH2). In contrast the thromboxane receptor antagonist EP 045 (up to 20 μM) had no effect on primary aggregation induced by PAF, thrombin and ADP. We have previously shown that EP 045 (IC50 = 0.5 μM), displaces the specific binding of [3H] 9,11-epoxymethano PGH2 to washed human platelets.PGF2α produces small increases in cAMP levels, and both this effect and the anti-aggregation are diminished by the adenyl cyclase inhibitor SQ 22536. The rise in cAMP induced by PGF2α is inhibited to a greater extent by the presence of ADP than by thrombin, PAF or a thromboxane mimetic. The ability of aggregating agents to inhibit this increase correlates inversely with their sensitivity to inhibition by PGF2α.We suggest that the very weak effect of PGF2α on cyclic AMP_ production is sufficient to account for its inhibitory activity, and it is unlikely to be a competitive antagonist at the platelet thromboxane receptor as suggested by others. 相似文献
11.
Janet M. Arce Brian A. Naughton Gail A. Kolks Philip Liu Albert S. Gordon Sam J. Piliero 《Prostaglandins & other lipid mediators》1981,21(3):367-377
Prostaglandins A2, E1, E2, methylated E2s and F2α affected erythropoiesis and/or erythropoietin (Ep) production. This action is indicated in the exhypoxic, polycythemic mouse where radioiron incorporations into RBC increased after administration of these compounds. The kidney and liver have been indicated through previous studies, to actively participate in Ep production. By the removal of one of these active sites in a murine system treated with prostaglandins it is shown that a response is reflected in Ep levels. Interference of the action of prostaglandins (PG) is altered by the removal of one of these target sites of Ep production. The erythropoietic responses elicited by PGA2, E1, and perhaps the methylated PGE2s act through the liver whereas PGE2 may operate through a renal pathway for its response. PGF2α reveals no effect on erythropoietic activity and is no different than that observed for vehicle-treated controls. The prostaglandins tested appear to act primarily through the kidney or liver but the possibility exists that some yet undetermined organ site may also be involved. 相似文献
12.
M.P.Eddy Moeljono Fuller W. Bazer W.W. Thatcher 《Prostaglandins & other lipid mediators》1976,11(4):737-743
Experiments were conducted to determine if prostaglandin F2α (PGF2α) is luteolytic in swine. In Experiment 1, four bilaterally hysterectomized gilts were injected with PGF2α at 0800 (10mg) and 2000 hours (10mg) and four gilts received .9% saline at the same times on day 17 after onset of estrus. Treatments were reversed in the two groups of gilts 21 days later. All eight PGF2α treated gilts exhibited estrus an average of 88.0 ± 13.5 hours after treatment and average duration of estrus was 66.0 ± 16.4 hours. Saline treated controls did not exhibit estrus. Two additional gilts were hysterectomized bilaterally and the saphenous artery catheterized on day 7 after onset of estrus. PGF2α injected on day 17 resulted in a precipitous decline in plasma progestin concentration and onset of estrus by 110 and 90 hours in gilts 1 and 2, respectively. Another bilaterally hysterectomized gilt, with CL marked with India ink, received PGF2α on day 17. Estrus occurred 92 hours later and, on day 4, regression of marked CL to corpora albicantia and presence of newly formed CL was confirmed at laparotomy.In Experiment 2, 12 bilaterally hysterectomized gilts were treated with PGF2α at 0800 (10mg) and 2000 hours (10mg) on either day 8, 11, 14 or 17 after onset of estrus. None of the gilts treated on days 8 and 11 exhibited estrus. Two of three gilts treated on day 14 and all three gilts treated on day 17 exhibited estrus at an average of 116.0 ± 9.8 hours post-treatment. Average duration of estrus was 49.6 ± 8.8 hours. 相似文献
13.
Levels of prostaglandin F2α (PGF2α) in the amniotic fluid were determined by radioimmunoassay. Concentrations of the prostaglandin were relatively constant between 15 and 35 weeks' gestation, but an increase was observed after 36 weeks. The rise was continued up to 44 weeks. A still greater elevation of PGF2α levels was recorded during labour, when the levels were related to the amount of cervical dilatation.Amniotic fluid PGF2α levels in toxaemia of pregnancy did not significantly differ from those found in normal pregnancy. 相似文献
14.
B. Sjöquist E. Oliw I. Lundén E. ÄnggÅrd 《Journal of chromatography. B, Analytical technologies in the biomedical and life sciences》1979,163(1):1-8
Analysis of prostaglandin F2α (PGF2α) in urine is a useful indicator of renal prostaglandin synthesis. A mass fragmentographic method for PGF2α analysis in human urine was developed using [3,3,4,4-2H4]PGF2α as an internal standard and carrier. PGF2α was extracted from urine (20 ml) with chloroform, purified by preparative thin-layer chromatography and converted to the methyl ester trimethylsilyl ether before analysis by gas chromatograph—mass spectrometry. The specificity of the urine analysis was demonstrated by retention time and the use of two pairs of fragments m/e 494/498 and 513/517 with the same results. The coefficient of variation for duplicate analysis averaged 12.6%, n = 17. Urine from recumbent women contained 4.9 ± 2.6 (S.D.) ng/ml or 4.1 ± 1.0 ng PGF2α per mg creatinine (n = 10) with little diurnal variation. Male urine contained 5.0 ± 2.7 (S.D.) ng/ml or 3.7 ± 2.1 ng/mg creatinine (n = 10). Similar concentrations were found in boys and in girls. These observations indicate that urinary PGF2α originates from the kidneys with little contribution from the male accessory sexual glands. This method can also be applied to analysis of PGF2α in rabbit urine. 相似文献
15.
Prostaglandins (PG) of both the E and F series may serve as modulators of norepinephrine (NE) release from peripheral sympathetic neurons. We have studied the effects of PGE2 and PGF2α on the accumulation and release of 3H-NE in the CNS using synaptosomes isolated from rat hypothalami.The release of 3H-NE from synaptosomes superfused with Krebs-Ringer bicarbonate buffer was multiphasic with an initial fast release phase followed by a slower release. Raising KC1 concentration of the superfusion medium to 56mM during the slow release phase is known to stimulate 3H-NE release. PGE2 (1 × 10?6M) attenuated 3H-NE release during the fast phase and reduced the amount of 3H-NE released due to KC1 stimulation. At lower concentrations of PGE2 there was no change in the release profile. PGF2α was without effect on 3H-NE release at all concentrations tested.The accumulation of 3H-NE was significantly diminished by PGE2 at a concentration of 1 × 10?6M, while a lower concentration (1 × 10?7M) was ineffective. PGF2α had no effect on 3H-NE accumulation at all concentrations investigated. 相似文献
16.
Michael C. Koss Jiro Nakano Joseph A. Rieger 《Prostaglandins & other lipid mediators》1976,11(4):691-698
Intravenous injection of prostaglandin F2α (4–15 μg/kg, i.v.) produces an increase in pulmonary arterial pressure in conjunction with reflex bradycardia and hypotension in the anesthetized cat. Meclofenamic acid (30 mg/kg, i.v.) inhibited the bradycardia and the reflex contribution to the systemic hypotension. Neither the PGF2α-induced pulmonary vasoconstriction nor the direct systemic vasodilator actions of PGF2α were blocked by meclofenamate. In addition, the reflex responses caused by i.v. veratrine and 5-HT were not inhibited by meclofenamate. These results suggest that meclofenamic acid selectively blocks the afferent mechanism by which PGF2α induces reflex bradycardia and hypotension in the cat. 相似文献
17.
The objectives were to test the hypothesis that exogenous prostaglandin F2α (PGF2α) temporarily restores sexual behavior of castrated boars, and to evaluate effects of PGF2α on serum hormone concentrations. At 35 d after castration, nine lean-type adult boars were randomly assigned to three treatments in a 3 × 3 latin square (with three replicates). Treatments were three doses of PGF2α doses (0, 10, and 20 mg) and three periods of treatment, with 5 d between each period. Serum testosterone (T) concentrations were non-detectable at the start of the experiment. Serum concentrations of estradiol (E2), LH, prolactin (PRL), and cortisol were unaffected (P > 0.05) by PGF2α treatment. The interval from treatment to ejaculation in boars treated with 10 mg (758 s) or 20 mg (660 s) PGF2α did not differ, but were different (P < 0.05) from control boars (>1 800 s). Ejaculation duration and false mounts differed (P < 0.05) between control boars and boars treated with 10 or 20 mg PGF2α. In conclusion, PGF2α treatment did not change serum concentrations of T, E2, LH, PRL, or cortisol, but restored sexual behavior. This restoration may have been due to an effect of PGF2α directly in specific areas of the brain, or indirectly via release of other hormones that stimulated areas in the brain that affected sexual behavior. 相似文献
18.
Robert C. Corlett M.D. Boonlaw SribyattaDaniel R. Mishell Jr. M.D. Charles BallardRobert M. Nakamura Ph.D. Ian H. Thorneycroft 《Prostaglandins & other lipid mediators》1972
The abortifacient activity of prostaglandin F2α was investigated by placing one or two 50 mg tablets of prostaglandin F2α in THAM salt into the vagina of nine women less than 4 weeks pregnant at intervals of 2 to 4 hours for a 24 hour period. Serum levels of HCG, estradiol (E2), progesterone and 17α-hydroxyprogesterone were measured by radioimmunoassay prior to starting therapy and at frequent intervals thereafter for 48 hours. All but two patients had significant side-effects, mainly diarrhea and vomiting, indicating that systemic absorption took place. Although bleeding was induced in 8 of 9 women, only 3 had complete abortions. A D&C was performed on all patients 48 hours after starting therapy. A significant fall in HCG levels was noted only in the patients who aborted. Only 3 of the 9 women had significant changes in steroid levels. A fall in progesterone and 17α-hydroxyprogesterone occurred in the 3 women who aborted and took place following the fall in HCG. Estradiol levels remained in the same range in all subjects. These findings indicate that prostaglandin F2α when administered in this vehicle and this dosage is relatively ineffective as an abortifacient. When effective, its action would appear to be due to contractions of uterine muscle and not secondarily to luteolysis. 相似文献
19.
Delivery was induced by an intravenous infusion of prostaglandin F2α (PGF2α) in gradually increasing doses in 30 consecutive cases of fetal death in utero after the 28th week of gestation. Twenty patients delivered during the first day of prostaglandin administration, 9 on the second day, and 1 patient not until the third day of infusion. It is concluded, that intravenous PGF2α appears to be superior to oxytocin in termination of pregnancy under these conditions. 相似文献