Abstract
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 μm. Inhibition was observed with various stimuli (arachidonic acid, bradykinin and calcium ionophore A23187). 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 μm). 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.
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Dates
Type | When |
---|---|
Created | 13 years, 1 month ago (July 19, 2012, 4:08 p.m.) |
Deposited | 1 year, 10 months ago (Oct. 25, 2023, 6:43 p.m.) |
Indexed | 1 year, 3 months ago (May 12, 2024, 1:56 p.m.) |
Issued | 30 years, 7 months ago (Feb. 1, 1995) |
Published | 30 years, 7 months ago (Feb. 1, 1995) |
Published Online | 13 years, 1 month ago (July 19, 2012) |
Published Print | 30 years, 7 months ago (Feb. 1, 1995) |
@article{Leis_1995, title={On the inhibition of prostanoid formation by SK&F 96365, a blocker of receptor‐operated calcium entry}, volume={114}, ISSN={1476-5381}, url={http://dx.doi.org/10.1111/j.1476-5381.1995.tb17181.x}, DOI={10.1111/j.1476-5381.1995.tb17181.x}, number={3}, journal={British Journal of Pharmacology}, publisher={Wiley}, author={Leis, Hans J. and Zach, Doris and Huber, Evelyn and Ziermann, Laszlo and Gleispach, Helmut and Windischhofer, W.}, year={1995}, month=feb, pages={598–601} }