A receptor-independent effect of estrone sulfate on the HERG channel.

Abstract:

:We recently reported that physiological concentrations of 17beta-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 17beta-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.

journal_name

J Pharmacol Sci

authors

Kakusaka S,Asayama M,Kaihara A,Sasano T,Suzuki T,Kurokawa J,Furukawa T

doi

10.1254/jphs.08257sc

subject

Has Abstract

pub_date

2009-01-01 00:00:00

pages

152-6

issue

1

eissn

1347-8613

issn

1347-8648

pii

JST.JSTAGE/jphs/08257SC

journal_volume

109

pub_type

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