A receptor-independent effect of estrone sulfate on the hERG channel

Shoko Kakusaka, Mahoko Asayama, Asami Kaihara, Tetsuo Sasano, Takeshi Suzuki, Junko Kurokawa, Tetsushi Furukawa

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14 Citations (Scopus)

Abstract

We recently reported that physiological concentrations of 17β-estradiol partially down-regulate cardiac rapidly-activating delayed rectifier K+ currents (hERG currents) independently of estrogen-receptor signaling. To determine if other estrogens have the same effect as that of 17β-estradiol, we investigated receptor-independent effects of estrone, estrone 3-sulfate, and estriol on hERG currents in patch-clamped estrogen-negative HEK293 cells. Only estrone 3-sulfate partially suppressed hERG currents in a receptor-independent manner by modifying the gating. The concentration-dependence of estrone 3-sulfate revealed that physiological levels of circulating estrone 3-sulfate can modulate hERG currents to the maximal extent in both women and men at any age.

Original languageEnglish
Pages (from-to)152-156
Number of pages5
JournalJournal of Pharmacological Sciences
Volume109
Issue number1
DOIs
Publication statusPublished - 2009 Jan 29

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Keywords

  • Estrogen
  • Heart
  • K channel (hERG)

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

Cite this

Kakusaka, S., Asayama, M., Kaihara, A., Sasano, T., Suzuki, T., Kurokawa, J., & Furukawa, T. (2009). A receptor-independent effect of estrone sulfate on the hERG channel. Journal of Pharmacological Sciences, 109(1), 152-156. https://doi.org/10.1254/jphs.08257SC