Inhibition of voltage-gated cationic channels in rat embryonic hypothalamic neurones and C1300 neuroblastoma cells by triphenylethylene antioestrogens.

Abstract:

:The effect of the non-steroidal antioestrogens tamoxifen and toremifene on voltage-gated cationic currents was examined in primary cultures of rat hypothalamic neurones and the C1300 mouse neuroblastoma cell line using the whole-cell patch clamp technique. When applied to the external bathing solution both tamoxifen and toremifene were able to inhibit TTX-sensitive sodium currents with IC50 values of 1-2 microM and delayed rectifier type potassium currents (IC50, 2-3 microM). However, only toremifene showed a significant inhibition of the I(A) current (IC50 3 microM). Inhibition of voltage-gated cationic currents was significantly impaired when tamoxifen was applied in a serum-containing solution. The steroidal antioestrogen ICI 182,780 did not inhibit any of the currents at 10 microM.

journal_name

FEBS Lett

journal_title

FEBS letters

authors

Hardy SP,deFelipe C,Valverde MA

doi

10.1016/s0014-5793(98)00974-0

subject

Has Abstract

pub_date

1998-09-04 00:00:00

pages

236-40

issue

3

eissn

0014-5793

issn

1873-3468

pii

S0014-5793(98)00974-0

journal_volume

434

pub_type

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