SKF-96365 (130495-35-1) was originally described as a selective blocker of receptor-mediated calcium entry (RMCE), IC50s= 8.5 and 11.7 µM for ADP- and thrombin-stimulated platelets respectively.1 TRPC channels have been shown to mediate RMCE2 and are believed to be the major target of SKF3. In rat vascular smooth muscle Ca entry was reduced by 10 µM SKF which was attributed to TRPC3.4 It has also been shown to inhibit L-type Ca channels.1 More recently it has been demonstrated to be a potent blocker of LVA hCaV3.1 T-type Ca channels, IC50=563 nM (state independent).5 Thus caution should be exercised when using SKF as a sole agent and appropriate controls are recommended.
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