By K. Schrör (auth.), Prof. Dr. med. Curt Diehm, Prof. Dr. med. Helmut Sinzinger, Dr. med. Waltraud Rogatti (eds.)
Although prostaglandin El (PGE ) has been clinically to be had for an extended 1 time, simply in recent times has its effectiveness in peripheral arterial occlusive ailment been proven in managed reports. no longer strangely, the favour capable effects accomplished either in sufferers with severe limb ischaemia and in people with intermittent claudication has inspired examine actions into the medical pharmacology of this prostaglandin. due to those efforts, fascinating new findings have printed that PGE has anti thrombotic , endothelium-stabilizing and leucocyte-stabi 1 lizing homes in addition to results on lipid metabolism, all of which, particularly except its recognized anti-aggregating and vasodilator results, might upload to the scientific efficacy of the substance. New information have additionally been amassed at the metabolism of PGE so much b significantly the detection of 13,14-dihydro-PGE a metabolite which was once b lately remoted in people following the management of PGE . Being 1 biologically energetic, the pharmacodynamic spectrum of 13,14-dihydro-PGE 1 very heavily resembles that of PGE . This discovering can help to provide an explanation for the 1 efficacy of PGE regardless of its quick metabolization whilst given intravenously.
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Additional resources for Prostaglandin E1 : New Aspects on Pharmacology, Metabolism and Clinical Efficacy
Chern. H. Strobach for TXB 2 measurement and S. Kuhlen for skillful technical assistance. Summary The actions of the in vivo metabolites of PGE b 15-keto-PGE 1 and 13,14dihydro-PGE 1 (PGEo), on human platelet and neutrophil polymorphonuclear leukocyte (PMN) function were studied in vitro and were compared to those of PGE 1 . PGEo and PGE 1 were equipotent inhibitors of collagenand ADP-stimulated platelet activation (ICso 10-100 nmoles/l), while 15keto-PGE 1 was nearly ineffective in the same concentration range .
While a dose of 1 Ilg PGE1/kg was not effective, doses above 5 Ilg PGE1/kg, up to 20 Ilg PGE1/kg, resulted in a comparable benefit . Similarly, 13,14-DH-PGE1 was active at the 5 Ilg PGE1/kg dose or above; 1 Ilg PGE1/kg again did not induce significant improvement. 01) effect of 5 Ilg PGE1/kg or 20 Ilg 13,14DH-PGE1/kg on the glycosaminoglycan synthesis. It has been demonstrated that monocyte macrophages entering the arterial wall influence proteoglycan synthesis. Increasing intracellular cyclic AMP in the platelets  and in the vascular wall cells inhibits mitotic activity  and the proliferation  and liberation of the platelet-derived growth factor (PDGF) from platelets [13, 14].
3) and shows no significant dependency on temperature (Fig. 4). PGE j significantly decreased the amount of unlabelled PGE j and 13,14-dihydro-PGE j Increase Low-Density Lipoprotein Receptors 43 Fig. 2. 1 20 oL-__ - L____L -_ _- L____L -_ _ o 10 20 30 40 ~ ____ 50 Minutes ~ 60 __ ~ ____ 70 ~ 80 __ ~ ____ 90 ~ 100 Fig. 3. Time course of specific LDL binding to human liver membranes showing equilibrium after 30 min. M); ~, absence of PGE 1 44 H. Sinzinger et al. % 100 95 90 85 80 75 - PGE1 (10 IJM) ---+- Absence of PGE1 70~--~------~------~-------L------~--------L-- 37°e Temperature 4°e Fig.
Prostaglandin E1 : New Aspects on Pharmacology, Metabolism and Clinical Efficacy by K. Schrör (auth.), Prof. Dr. med. Curt Diehm, Prof. Dr. med. Helmut Sinzinger, Dr. med. Waltraud Rogatti (eds.)