Characterisation of the inhibition of the hepatocyte receptor-activated Ca2+ inflow system by gadolinium and SK&F 96365

Kekulu C. Fernando, Greg J. Barritt

    Research output: Contribution to journalArticle

    33 Citations (Scopus)

    Abstract

    The inhibition of agonist-stimulated divalent cation inflow in hepatocytes by Gd3+ and compound SK&F 96365 (1-{β-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl}-1H-imidazole hydrochloride) was investigated. Gd3+ and SK&F 96365 inhibited Ca2+ and Mn2+ inflow stimulated by vasopressin, angiotensin II or phenylephrine. The concentrations of Gd3+ and SK&F 96365 which gave half-maximal inhibition of vasopressin-stimulated Ca2+ inflow were 2 · 10-7 M and 16 · 10-6 M, respectively. The action of Gd3+ on vasopressin-stimulated Ca2+ inflow was rapid (less than 10 s in onset) and reversible. Gd3+ had no effect on Mn2+ inflow in the absence of an agonist and no effect on the ability of vasopressin to release Ca2+ from intracellular stores. SK&F 96365 inhibited Mn2+ inflow in the absence of agonists and vasopressin-induced release of Ca2+ from intracellular stores, but at approximately a 5-fold higher concentration than that which inhibited vasopressin-stimulated divalent cation inflow. It is concluded that Gd3+ and SK&F 96365 (at concentrations below 20 μM) inhibit, in a selective manner, divalent cation movement through the putative cation channel of the hepatocyte receptor-activated Ca2+ inflow system. Gd3+ appears to be the most potent inhibitor of this Ca2+ inflow system so far described.

    Original languageEnglish
    Pages (from-to)383-389
    Number of pages7
    JournalBBA - Molecular Cell Research
    Volume1222
    Issue number3
    DOIs
    Publication statusPublished - 21 Jul 1994

    Keywords

    • (Rat)
    • Calcium ion inflow
    • Gadolinium
    • Hepatocyte
    • SK&F 96365
    • Vasopressin

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