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 Lettjournal_title
FEBS lettersauthors
Hardy SP,deFelipe C,Valverde MAdoi
10.1016/s0014-5793(98)00974-0subject
Has Abstractpub_date
1998-09-04 00:00:00pages
236-40issue
3eissn
0014-5793issn
1873-3468pii
S0014-5793(98)00974-0journal_volume
434pub_type
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