Prostaglandins

Oesterling, T.O.; Morozowich, W.; Roseman, Theodore J.

doi:10.1002/jps.2600611202

Cited by 83 publications

(16 citation statements)

References 266 publications

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“…compared to 3 H-PGF 2a after incubation with hamster uterus may not be a reflection of greater metabolism of PGE X during incubation. PGE X is known to be less stable than PGF 2a (15) and may be subject to breakdown in the course of extraction. Also in tissue metabolism, PGEi is first converted to 15-keto PGEj (15), which has a low affinity for PGE X binding sites.…”

Section: Discussionmentioning

confidence: 99%

Prostaglandin Receptors in the Human, Monkey and Hamster Uterus

Wakeling¹,

Wyngarden²

1974

Endocrinology

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An in vitro tissue slice incubation system has been used to measure uptake and binding of 3 H-labeled prostaglandins by uterine tissues from the human, monkey and hamster. Specific binding of prostaglandin Ei (PGEi) and P G F 2 Q was demonstrated in rhesus monkey myometrium, but not endometrium, and in human myometrium. Specific binding of PGE 2 but not PGF, a was present in hamster uterus throughout the estrous cycle. Variations in prostaglandin specific binding during the estrous cycle, and in pregnancy of the hamster, and demonstration of prostaglandin concentrative capacity of the hamster uterus, were indicative of the presence of true prostaglandin receptors in the uterus. Quantitative estimates of PGE, binding in the hamster uterus gave values for the association constant of 5.8 and 16.4 x 10 9 M~! and values for receptor concentration of 3.7 and 4.1 x 10" 12 moles/100 mg tissue for whole uterus and myometrium, respectively. Relative affinities of some prostaglandins for PGE, binding sites in the hamster uterus were 16,16-dimethyl PGE, = PGE, = PGE 2 > 15(S)15-methyl PGE, methyl ester = 13,14-dihydro PGE, = PGA, = PGE, methyl ester $> PGF 2a = 15-keto PGE,. Treatment of ovariectomized hamsters with estradiol decreased PGE, and PGF 2a specific binding in the uterus in a dose-dependent manner. Progesterone increased b'oth PGE, and PGF 2a specific binding. (Endocrinology 95: 55, 1974) R ECENT reports .from this laboratory have demonstrated the presence of prostaglandin receptors in the hamster uterus (1) and in the rabbit oviduct (2). In vitro studies on the nature of prostaglandin Ei (PGEx) receptor in the hamster uterus (3) have shown that the PGE! receptor is located in a membrane fraction of the uterus and is stabilized by association with its ligand. The receptor is at least, in part, a protein and the binding is irreversible in vitro. The relative lability of prostaglandin specific binding in broken-cell preparations (3) has led us to further study of the nature of prostaglandin binding in intact tissue slices of the uterus. In this paper we report studies of prostaglandin uptake by monkey and human uterus, quantitative measurements of the PGEj receptor in the hamster uterus, and changes in prostaglandin specific binding in the hamster uterus in response to changes in physiological state and treatment with ovarian steroids.

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Section: Discussionmentioning

confidence: 99%

Prostaglandin Receptors in the Human, Monkey and Hamster Uterus

Wakeling¹,

Wyngarden²

1974

Endocrinology

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“…PGE 1 is a weak acid with a pKa of 4.85 whose stability in solution may be sensitive to heat and pH. Maximum stability of PGE 1 in normal saline, assessed as a function of pH at room temperature, was observed in pH range of 6–7; considerable activity loss was observed outside this range 16. In newborns, dextrose is the solute of choice for intravenous drug preparations.…”

Section: Discussionmentioning

confidence: 99%

Stability of prostaglandin E₁solutions stored in polypropylene syringes for continuous intravenous administration to newborns

et al. 2017

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ObjectiveWe aimed to monitor the physicochemical stability of prostaglandin E1 (PGE1) 1.5 and 15 µg/mL in 10% dextrose stored in polypropylene syringes.MethodsWe developed a liquid chromatography-high resolution mass spectrometry (LC-HRMS) method to detect and quantify levels of PGE1. Method selectivity was performed with a mixture of PGE1 and its degradation products. Forced degradation tests were performed to determine which degradation products were most likely to form. PGE1 injection solutions in 10% dextrose were stored in unprotected and shielded-from-light polypropylene syringes in a climatic chamber. Samples were taken immediately after preparation (T0) and after 24, 48, 72 and 168 hours for analysis. PGE1 solutions were considered stable if ≥90.0% of the initial concentration was retained.ResultsThe LC-HRMS method was validated in the range of 0.086-0.200µg/mL PGE1 with trueness values between 98.2% and 100.3%, and repeatability and intermediate precision values of <2.2%and <4.7%, respectively. The quantification and detection limits of the method were 0.086 and 0.026µg/mL, respectively. PGE1 and its degradation products were resolved chromatographically. PGE1 injection solutions were≥90.0%stable after 48hours in unprotected from light (UPL) syringes. The solutions remained clear without precipitation, colour or pH modification and subvisible particles within the permitted levels. Prostaglandin A1 was the sole degradation product observed.ConclusionsA LC-HRMS method to evaluate PGE1 stability in a 10% dextrose was developed and validated. PGE1 1.5 and 15µg/mL in 10% dextrose solution are stable for 48hours when stored at 30ºC in UPL polypropylene syringes.

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“…The conversion of prostaglandins to C1-methyl esters has resulted in increased or more rapid intestinal absorption (1,2), as well as in greater potency following intravenous administration (3). Since few prostaglandin C1-aliphatic esters have been reported, various aliphatic esters of dinoprost (I) and dinoprostone (11) were spthesized for evaluation of their utility as prodrugs in continuation of our effort on prostaglandin prodrugs (4).…”

Section: Methodsmentioning

confidence: 99%