Premium
Inhibition of voltage‐gated cationic channels in rat embryonic hypothalamic neurones and C1300 neuroblastoma cells by triphenylethylene antioestrogens
Author(s) -
Hardy S.P.,
deFelipe C.,
Valverde M.A.
Publication year - 1998
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/s0014-5793(98)00974-0
Subject(s) - embryonic stem cell , neuroblastoma , chemistry , microbiology and biotechnology , biophysics , biology , biochemistry , cell culture , genetics , gene
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 IC 50 values of 1–2 μM and delayed rectifier type potassium currents (IC 50 , 2–3 μM). However, only toremifene showed a significant inhibition of the I A current (IC 50 3 μM). 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 μM.