Inhibition of voltage-gated cationic channels in rat embryonic hypothalamic neurones and C1300 neuroblastoma cells by triphenylethylene antioestrogens
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 soluti...
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| Veröffentlicht in: | FEBS letters 1998-09, Vol.434 (3), p.236-240 |
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| creator | Hardy, S.P. deFelipe, C. Valverde, M.A. |
| description | 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. |
| doi_str_mv | 10.1016/S0014-5793(98)00974-0 |
| format | Article |
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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.</description><identifier>ISSN: 0014-5793</identifier><identifier>EISSN: 1873-3468</identifier><identifier>DOI: 10.1016/S0014-5793(98)00974-0</identifier><identifier>PMID: 9742930</identifier><language>eng</language><publisher>England: Elsevier B.V</publisher><subject>4-AP, 4-aminopyridine ; Animals ; DR, delayed rectifier ; EGTA, ethylene glycol-bis-(β-aminoethyl ether) N,N,N′,N′-tetraacetic acid ; Estrogen Antagonists - pharmacology ; HEPES, N-[2-hydroxyethyl] piperazine-N′-[2-ethanesulphonic acid] ; Hypothalamus ; Hypothalamus - drug effects ; Hypothalamus - embryology ; Hypothalamus - physiology ; ICI 182,780 ; Ion Channel Gating ; MEM, minimal essential medium ; Mice ; Neuroblastoma - pathology ; Neuroblastoma - physiopathology ; Neurons - cytology ; Neurons - drug effects ; Neurons - physiology ; Potassium Channel Blockers ; Potassium Channels - physiology ; Potassium current ; Rats ; Rats, Sprague-Dawley ; Sodium Channel Blockers ; Sodium Channels - physiology ; Sodium current ; Tamoxifen ; Tamoxifen - pharmacology ; TEA, tetraethylammonium ; Toremifene</subject><ispartof>FEBS letters, 1998-09, Vol.434 (3), p.236-240</ispartof><rights>1998 Federation of European Biochemical Societies</rights><rights>FEBS Letters 434 (1998) 1873-3468 © 2015 Federation of European Biochemical Societies</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c5380-2f013802decf803856478aab2c7740fd11f07c13d812dbd9df37cd322a3236cd3</citedby><cites>FETCH-LOGICAL-c5380-2f013802decf803856478aab2c7740fd11f07c13d812dbd9df37cd322a3236cd3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1016%2FS0014-5793%2898%2900974-0$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0014-5793(98)00974-0$$EHTML$$P50$$Gelsevier$$Hfree_for_read</linktohtml><link.rule.ids>315,782,786,1419,1435,3554,27933,27934,45583,45584,46004,46418,46842</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9742930$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Hardy, S.P.</creatorcontrib><creatorcontrib>deFelipe, C.</creatorcontrib><creatorcontrib>Valverde, M.A.</creatorcontrib><title>Inhibition of voltage-gated cationic channels in rat embryonic hypothalamic neurones and C1300 neuroblastoma cells by triphenylethylene antioestrogens</title><title>FEBS letters</title><addtitle>FEBS Lett</addtitle><description>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.</description><subject>4-AP, 4-aminopyridine</subject><subject>Animals</subject><subject>DR, delayed rectifier</subject><subject>EGTA, ethylene glycol-bis-(β-aminoethyl ether) N,N,N′,N′-tetraacetic acid</subject><subject>Estrogen Antagonists - pharmacology</subject><subject>HEPES, N-[2-hydroxyethyl] piperazine-N′-[2-ethanesulphonic acid]</subject><subject>Hypothalamus</subject><subject>Hypothalamus - drug effects</subject><subject>Hypothalamus - embryology</subject><subject>Hypothalamus - physiology</subject><subject>ICI 182,780</subject><subject>Ion Channel Gating</subject><subject>MEM, minimal essential medium</subject><subject>Mice</subject><subject>Neuroblastoma - pathology</subject><subject>Neuroblastoma - physiopathology</subject><subject>Neurons - cytology</subject><subject>Neurons - drug effects</subject><subject>Neurons - physiology</subject><subject>Potassium Channel Blockers</subject><subject>Potassium Channels - physiology</subject><subject>Potassium current</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Sodium Channel Blockers</subject><subject>Sodium Channels - physiology</subject><subject>Sodium current</subject><subject>Tamoxifen</subject><subject>Tamoxifen - pharmacology</subject><subject>TEA, tetraethylammonium</subject><subject>Toremifene</subject><issn>0014-5793</issn><issn>1873-3468</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1998</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNUcFu1DAQtRCoLIVPqOQTgkPAjrNr-4ToqqWVKnEAzpZjTzZGib3Y3qL8CN-Lk6x6hYvHM-_Nm9E8hK4o-UAJ3X38Rghtqi2X7J0U7wmRvKnIM7ShgrOKNTvxHG2eKC_Rq5R-kpILKi_QRSHXkpEN-nPve9e67ILHocOPYcj6ANVBZ7DY6LnuDDa99h6GhJ3HUWcMYxunBemnY8i9HvRYEg-nGDwkrL3Fe8oIWUvtoFMOo8YGhiLSTjhHd-zBTwPkvjweSkuZBSnHcACfXqMXnR4SvDnHS_Tj9ub7_q56-Prlfv_5oTJbJkhVd4SWWFswnSBMbHcNF1q3teG8IZ2ltCPcUGYFrW1rpe0YN5bVtWY125XfJXq76h5j-HUq49Xo0ryl9hBOSXEmG8maphC3K9HEkFKETh2jG3WcFCVq9kMtfqj52EoKtfihSOm7Og84tSPYp66zAQW_W_HfboDp_0TV7c11vSAzIMVSnqU-rVLFKHh0EFUyDrwB6yKYrGxw_1j2L7gysdg</recordid><startdate>19980904</startdate><enddate>19980904</enddate><creator>Hardy, S.P.</creator><creator>deFelipe, C.</creator><creator>Valverde, M.A.</creator><general>Elsevier B.V</general><scope>6I.</scope><scope>AAFTH</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19980904</creationdate><title>Inhibition of voltage-gated cationic channels in rat embryonic hypothalamic neurones and C1300 neuroblastoma cells by triphenylethylene antioestrogens</title><author>Hardy, S.P. ; deFelipe, C. ; Valverde, M.A.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c5380-2f013802decf803856478aab2c7740fd11f07c13d812dbd9df37cd322a3236cd3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1998</creationdate><topic>4-AP, 4-aminopyridine</topic><topic>Animals</topic><topic>DR, delayed rectifier</topic><topic>EGTA, ethylene glycol-bis-(β-aminoethyl ether) N,N,N′,N′-tetraacetic acid</topic><topic>Estrogen Antagonists - pharmacology</topic><topic>HEPES, N-[2-hydroxyethyl] piperazine-N′-[2-ethanesulphonic acid]</topic><topic>Hypothalamus</topic><topic>Hypothalamus - drug effects</topic><topic>Hypothalamus - embryology</topic><topic>Hypothalamus - physiology</topic><topic>ICI 182,780</topic><topic>Ion Channel Gating</topic><topic>MEM, minimal essential medium</topic><topic>Mice</topic><topic>Neuroblastoma - pathology</topic><topic>Neuroblastoma - physiopathology</topic><topic>Neurons - cytology</topic><topic>Neurons - drug effects</topic><topic>Neurons - physiology</topic><topic>Potassium Channel Blockers</topic><topic>Potassium Channels - physiology</topic><topic>Potassium current</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Sodium Channel Blockers</topic><topic>Sodium Channels - physiology</topic><topic>Sodium current</topic><topic>Tamoxifen</topic><topic>Tamoxifen - pharmacology</topic><topic>TEA, tetraethylammonium</topic><topic>Toremifene</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Hardy, S.P.</creatorcontrib><creatorcontrib>deFelipe, C.</creatorcontrib><creatorcontrib>Valverde, M.A.</creatorcontrib><collection>ScienceDirect Open Access Titles</collection><collection>Elsevier:ScienceDirect:Open Access</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>FEBS letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Hardy, S.P.</au><au>deFelipe, C.</au><au>Valverde, M.A.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Inhibition of voltage-gated cationic channels in rat embryonic hypothalamic neurones and C1300 neuroblastoma cells by triphenylethylene antioestrogens</atitle><jtitle>FEBS letters</jtitle><addtitle>FEBS Lett</addtitle><date>1998-09-04</date><risdate>1998</risdate><volume>434</volume><issue>3</issue><spage>236</spage><epage>240</epage><pages>236-240</pages><issn>0014-5793</issn><eissn>1873-3468</eissn><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 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.</abstract><cop>England</cop><pub>Elsevier B.V</pub><pmid>9742930</pmid><doi>10.1016/S0014-5793(98)00974-0</doi><tpages>5</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | FEBS letters, 1998-09, Vol.434 (3), p.236-240 |
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| source | MEDLINE; Access via Wiley Online Library; Access via ScienceDirect (Elsevier); EZB-FREE-00999 freely available EZB journals; Wiley Online Library (Open Access Collection); Alma/SFX Local Collection |
| subjects | 4-AP, 4-aminopyridine Animals DR, delayed rectifier EGTA, ethylene glycol-bis-(β-aminoethyl ether) N,N,N′,N′-tetraacetic acid Estrogen Antagonists - pharmacology HEPES, N-[2-hydroxyethyl] piperazine-N′-[2-ethanesulphonic acid] Hypothalamus Hypothalamus - drug effects Hypothalamus - embryology Hypothalamus - physiology ICI 182,780 Ion Channel Gating MEM, minimal essential medium Mice Neuroblastoma - pathology Neuroblastoma - physiopathology Neurons - cytology Neurons - drug effects Neurons - physiology Potassium Channel Blockers Potassium Channels - physiology Potassium current Rats Rats, Sprague-Dawley Sodium Channel Blockers Sodium Channels - physiology Sodium current Tamoxifen Tamoxifen - pharmacology TEA, tetraethylammonium Toremifene |
| title | Inhibition of voltage-gated cationic channels in rat embryonic hypothalamic neurones and C1300 neuroblastoma cells by triphenylethylene antioestrogens |
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