Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
Leis, HJ; Zach, D; Huber, E; Ziermann, L; Gleispach, H; Windischhofer, W.
On the inhibition of prostanoid formation by SK&F 96365, a blocker of receptor-operated calcium entry.
Br J Pharmacol. 1995; 114(3):598-601
Doi: 10.1111/j.1476-5381.1995.tb17181.x
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- Führende Autor*innen der Med Uni Graz
- Leis Hans-Joerg
- Co-Autor*innen der Med Uni Graz
- Windischhofer Werner
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- Abstract:
- 1. The proposed blocker of receptor-operated calcium channels, SK&F 96365 was shown to inhibit formation of prostaglandin E2 in two osteoblast-like cell lines, MC3T3-E1 and UMR-106 in a dose-dependent manner at an IC50 of 3-4 microM. Inhibition was observed with various stimuli (arachidonic acid, bradykinin and calcium ionophore A23187). 2. This effect was also observed in human platelets, where SK&F 96365 dose-dependently blocked thromboxane biosynthesis and formation of 12-hydroxy-heptadecatrienoic acid after stimulation with arachidonic acid (IC50 = 4 microM). 3. The compound had no effect on 12-hydroxy-eicosatetraenoic acid production by human platelets. Additionally, linoleic acid oxidation by soybean 15-lipoxidase was not impaired by SK&F 96365. The results thus provide evidence for cyclo-oxygenase inhibition by SK&F 96365 at concentrations used to block receptor-operated calcium influx.
- Find related publications in this database (using NLM MeSH Indexing)
- 12-Hydroxy-5,8,10,14-eicosatetraenoic Acid -
- 3T3 Cells - cytology
- Animals -
- Arachidonic Acid - pharmacology
- Blood Platelets - drug effects
- Bradykinin - pharmacology
- Calcimycin - pharmacology
- Calcium Channel Blockers - pharmacology
- Cell Line -
- Cells, Cultured -
- Cyclooxygenase Inhibitors - pharmacology
- Dinoprostone - antagonists & inhibitors
- Dose-Response Relationship, Drug -
- Humans -
- Hydroxyeicosatetraenoic Acids - antagonists & inhibitors
- Imidazoles - pharmacology
- Linoleic Acid -
- Linoleic Acids - chemistry
- Mice -
- Osteoblasts - cytology
- Oxidation-Reduction -
- Thromboxanes - antagonists & inhibitors