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• W2042474871 abstract "Xestospongin‐C isolated from a marine sponge, Xestospongia sp ., has recently been shown to be a membrane‐permeable IP 3 receptor inhibitor. In this study we examined the effects of this compound on smooth muscle from guinea‐pig ileum. In guinea‐pig ileum permeabilized with α‐toxin, xestospongin‐C (3 μ M ) inhibited contractions induced by Ca 2+ mobilized from sarcoplasmic reticulum (SR) with IP 3 or carbachol with GTP, but not with caffeine. In intact smooth muscle tissue, xestospongin‐C (3–10 μ M ) inhibited carbachol‐ and high‐K + ‐induced increases in [Ca 2+ ] i and contractions at sustained phase. It also inhibited voltage‐dependent inward Ba 2+ currents in a concentration‐dependent manner with an IC 50 of 0.63 μ M . Xestospongin‐C (3–10 μ M ) had no effect on carbachol‐induced inward Ca 2+ currents via non‐selective cation channels; but it did reduce voltage‐dependent K + currents in a concentration‐dependent manner with an IC 50 of 0.13 μ M . These results suggest that xestospongin‐C inhibits the IP 3 receptor but not the ryanodine receptor in smooth muscle SR membrane. In intact smooth muscle cells, however, xestospongin‐C appears to inhibit voltage‐dependent Ca 2+ and K + currents at a concentration range similar to that at which it inhibits the IP 3 receptor. Xestospongin‐C is a selective blocker of the IP 3 receptor in permeabilised cells but not in cells with intact plasma membrane. British Journal of Pharmacology (2002) 137 , 1207–1212. doi: 10.1038/sj.bjp.0704988" @default.
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• W2042474871 date "2002-12-01" @default.
• W2042474871 modified "2023-10-17" @default.
• W2042474871 title "Inhibitory mechanism of xestospongin‐C on contraction and ion channels in the intestinal smooth muscle" @default.
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• W2042474871 doi "https://doi.org/10.1038/sj.bjp.0704988" @default.
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