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Inhibitory effects of calcium channel blockers on thyroid hormone uptake in neonatal rat cardiomyocytes
Departments of 1 Internal Medicine III and 2 Biochemistry, Erasmus University Medical School, 3000 DR Rotterdam; and 3 Department of Veterinary Anatomy and Physiology, Utrecht University, 3508 TD Utrecht, The Netherlands The effects of the Ca 2+ channel blockers verapamil, nifedipine, and diltiaz...
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Published in: | American journal of physiology. Heart and circulatory physiology 2001-11, Vol.281 (5), p.H1985-H1991 |
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container_end_page | H1991 |
container_issue | 5 |
container_start_page | H1985 |
container_title | American journal of physiology. Heart and circulatory physiology |
container_volume | 281 |
creator | Verhoeven, Frank A Moerings, Ellis P. C. M Lamers, Jos M. J Hennemann, Georg Visser, Theo J Everts, Maria E |
description | Departments of 1 Internal Medicine III and
2 Biochemistry, Erasmus University Medical School, 3000 DR
Rotterdam; and 3 Department of Veterinary Anatomy and
Physiology, Utrecht University, 3508 TD Utrecht, The Netherlands
The effects of the
Ca 2+ channel blockers verapamil, nifedipine, and diltiazem
on triiodothyronine (T 3 ) and thyroxine (T 4 )
uptake were tested in cultured cardiomyocytes from 2-day-old rats.
Experiments were performed at 37°C in medium with 0.5% BSA for
[ 125 I]T 3 (100 pM) or 0.1% BSA for
[ 125 I]T 4 (350 pM). The 15-min uptake of
[ 125 I]T 3 was 0.124 ± 0.013 fmol/pM free
T 3 ( n = 6);
[ 125 I]T 4 uptake was 0.032 ± 0.003 fmol/pM free T 4 ( n = 12). Neither T 3 nor T 4 uptake was affected by 1% DMSO
(diluent for nifedipine and verapamil). Uptake of
[ 125 I]T 3 but not of
[ 125 I]T 4 was dose dependently reduced by
incubation with 1-100 µM verapamil (49-87%,
P |
doi_str_mv | 10.1152/ajpheart.2001.281.5.H1985 |
format | article |
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2 Biochemistry, Erasmus University Medical School, 3000 DR
Rotterdam; and 3 Department of Veterinary Anatomy and
Physiology, Utrecht University, 3508 TD Utrecht, The Netherlands
The effects of the
Ca 2+ channel blockers verapamil, nifedipine, and diltiazem
on triiodothyronine (T 3 ) and thyroxine (T 4 )
uptake were tested in cultured cardiomyocytes from 2-day-old rats.
Experiments were performed at 37°C in medium with 0.5% BSA for
[ 125 I]T 3 (100 pM) or 0.1% BSA for
[ 125 I]T 4 (350 pM). The 15-min uptake of
[ 125 I]T 3 was 0.124 ± 0.013 fmol/pM free
T 3 ( n = 6);
[ 125 I]T 4 uptake was 0.032 ± 0.003 fmol/pM free T 4 ( n = 12). Neither T 3 nor T 4 uptake was affected by 1% DMSO
(diluent for nifedipine and verapamil). Uptake of
[ 125 I]T 3 but not of
[ 125 I]T 4 was dose dependently reduced by
incubation with 1-100 µM verapamil (49-87%,
P < 0.05) or nifedipine (53-81%,
P < 0.05). The relative decline in
[ 125 I]T 3 uptake after 4 h of incubation
with 10 µM verapamil or nifedipine was less than after 15 min or
1 h, indicating that the major inhibitory effect of the
Ca 2+ channel blockers occurred at the level of the plasma
membrane. The reduction of nuclear [ 125 I]T 3
binding by 10 µM verapamil or nifedipine was proportional to the
reduction of cellular [ 125 I]T 3 uptake.
Diltiazem (1-100 µM) had no dose-dependent effect on
[ 125 I]T 3 uptake but reduced
[ 125 I]T 4 uptake by 45% ( P < 0.05) at each concentration tested. Neither the presence of 20 mM
K + nor the presence of low Ca 2+ in the medium
affected [ 125 I]T 3 uptake. In conclusion, the
inhibitory effects of Ca 2+ channel blockers on
T 3 uptake in cardiomyocytes are not secondary to their
effects on Ca 2+ influx but, rather, reflect interference
with the putative T 3 carrier in the plasma membrane.
heart; culture; ATP; free hormone fraction</description><identifier>ISSN: 0363-6135</identifier><identifier>EISSN: 1522-1539</identifier><identifier>DOI: 10.1152/ajpheart.2001.281.5.H1985</identifier><identifier>PMID: 11668059</identifier><language>eng</language><publisher>United States</publisher><subject>Adenosine Triphosphate - metabolism ; Animals ; Animals, Newborn ; Biological Transport - drug effects ; Calcium - pharmacology ; Calcium Channel Blockers - pharmacology ; Cell Membrane - metabolism ; Cells, Cultured ; Diltiazem - pharmacology ; Iodine Radioisotopes ; Muscle Fibers, Skeletal - cytology ; Muscle Fibers, Skeletal - drug effects ; Muscle Fibers, Skeletal - metabolism ; Myocardium - cytology ; Nifedipine - pharmacology ; Potassium - pharmacology ; Rats ; Rats, Wistar ; Thyroxine - pharmacokinetics ; Triiodothyronine - pharmacokinetics ; Verapamil - pharmacology</subject><ispartof>American journal of physiology. Heart and circulatory physiology, 2001-11, Vol.281 (5), p.H1985-H1991</ispartof><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c456t-edba2a02f77dbdbd42157ab730353d1ffa0f452fc310560d3fd54991be7561873</citedby><cites>FETCH-LOGICAL-c456t-edba2a02f77dbdbd42157ab730353d1ffa0f452fc310560d3fd54991be7561873</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11668059$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Verhoeven, Frank A</creatorcontrib><creatorcontrib>Moerings, Ellis P. C. M</creatorcontrib><creatorcontrib>Lamers, Jos M. J</creatorcontrib><creatorcontrib>Hennemann, Georg</creatorcontrib><creatorcontrib>Visser, Theo J</creatorcontrib><creatorcontrib>Everts, Maria E</creatorcontrib><title>Inhibitory effects of calcium channel blockers on thyroid hormone uptake in neonatal rat cardiomyocytes</title><title>American journal of physiology. Heart and circulatory physiology</title><addtitle>Am J Physiol Heart Circ Physiol</addtitle><description>Departments of 1 Internal Medicine III and
2 Biochemistry, Erasmus University Medical School, 3000 DR
Rotterdam; and 3 Department of Veterinary Anatomy and
Physiology, Utrecht University, 3508 TD Utrecht, The Netherlands
The effects of the
Ca 2+ channel blockers verapamil, nifedipine, and diltiazem
on triiodothyronine (T 3 ) and thyroxine (T 4 )
uptake were tested in cultured cardiomyocytes from 2-day-old rats.
Experiments were performed at 37°C in medium with 0.5% BSA for
[ 125 I]T 3 (100 pM) or 0.1% BSA for
[ 125 I]T 4 (350 pM). The 15-min uptake of
[ 125 I]T 3 was 0.124 ± 0.013 fmol/pM free
T 3 ( n = 6);
[ 125 I]T 4 uptake was 0.032 ± 0.003 fmol/pM free T 4 ( n = 12). Neither T 3 nor T 4 uptake was affected by 1% DMSO
(diluent for nifedipine and verapamil). Uptake of
[ 125 I]T 3 but not of
[ 125 I]T 4 was dose dependently reduced by
incubation with 1-100 µM verapamil (49-87%,
P < 0.05) or nifedipine (53-81%,
P < 0.05). The relative decline in
[ 125 I]T 3 uptake after 4 h of incubation
with 10 µM verapamil or nifedipine was less than after 15 min or
1 h, indicating that the major inhibitory effect of the
Ca 2+ channel blockers occurred at the level of the plasma
membrane. The reduction of nuclear [ 125 I]T 3
binding by 10 µM verapamil or nifedipine was proportional to the
reduction of cellular [ 125 I]T 3 uptake.
Diltiazem (1-100 µM) had no dose-dependent effect on
[ 125 I]T 3 uptake but reduced
[ 125 I]T 4 uptake by 45% ( P < 0.05) at each concentration tested. Neither the presence of 20 mM
K + nor the presence of low Ca 2+ in the medium
affected [ 125 I]T 3 uptake. In conclusion, the
inhibitory effects of Ca 2+ channel blockers on
T 3 uptake in cardiomyocytes are not secondary to their
effects on Ca 2+ influx but, rather, reflect interference
with the putative T 3 carrier in the plasma membrane.
heart; culture; ATP; free hormone fraction</description><subject>Adenosine Triphosphate - metabolism</subject><subject>Animals</subject><subject>Animals, Newborn</subject><subject>Biological Transport - drug effects</subject><subject>Calcium - pharmacology</subject><subject>Calcium Channel Blockers - pharmacology</subject><subject>Cell Membrane - metabolism</subject><subject>Cells, Cultured</subject><subject>Diltiazem - pharmacology</subject><subject>Iodine Radioisotopes</subject><subject>Muscle Fibers, Skeletal - cytology</subject><subject>Muscle Fibers, Skeletal - drug effects</subject><subject>Muscle Fibers, Skeletal - metabolism</subject><subject>Myocardium - cytology</subject><subject>Nifedipine - pharmacology</subject><subject>Potassium - pharmacology</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Thyroxine - pharmacokinetics</subject><subject>Triiodothyronine - pharmacokinetics</subject><subject>Verapamil - pharmacology</subject><issn>0363-6135</issn><issn>1522-1539</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2001</creationdate><recordtype>article</recordtype><recordid>eNp1kE1vFSEUhonR2Gv1LxjcuJspH5f5iCvTWNukiZu6Jgwc7tAywwhMdP691HvVuhAWLM77vIc8CL2jpKZUsAt1v4ygYq4ZIbRmHa1FfU37TjxDuzJnFRW8f452hDe8aigXZ-hVSveEENE2_CU6o7RpOiL6HTrczKMbXA5xw2At6JxwsFgrr906YT2qeQaPBx_0A8Qym3EetxicwWOIU5gBr0tWD4DdjGcIs8rK46hyqYjGhWkLesuQXqMXVvkEb07vOfp69enu8rq6_fL55vLjbaX3oskVmEExRZhtWzOUu2dUtGpoOeGCG2qtInYvmNWcEtEQw60R-76nA7SioV3Lz9H7Y-8Sw7cVUpaTSxq8V-Vza5ItK6frWAn2x6COIaUIVi7RTSpukhL5aFn-tiwfLctiWQr5y3Jh356WrMME5i950loCF8fA6A7jdxdBLuOWXPDhsD3p_afyw_-Jq9X7O_iR_6BPSLkYy38CCnGkPQ</recordid><startdate>20011101</startdate><enddate>20011101</enddate><creator>Verhoeven, Frank A</creator><creator>Moerings, Ellis P. C. M</creator><creator>Lamers, Jos M. J</creator><creator>Hennemann, Georg</creator><creator>Visser, Theo J</creator><creator>Everts, Maria E</creator><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>20011101</creationdate><title>Inhibitory effects of calcium channel blockers on thyroid hormone uptake in neonatal rat cardiomyocytes</title><author>Verhoeven, Frank A ; Moerings, Ellis P. C. M ; Lamers, Jos M. J ; Hennemann, Georg ; Visser, Theo J ; Everts, Maria E</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c456t-edba2a02f77dbdbd42157ab730353d1ffa0f452fc310560d3fd54991be7561873</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2001</creationdate><topic>Adenosine Triphosphate - metabolism</topic><topic>Animals</topic><topic>Animals, Newborn</topic><topic>Biological Transport - drug effects</topic><topic>Calcium - pharmacology</topic><topic>Calcium Channel Blockers - pharmacology</topic><topic>Cell Membrane - metabolism</topic><topic>Cells, Cultured</topic><topic>Diltiazem - pharmacology</topic><topic>Iodine Radioisotopes</topic><topic>Muscle Fibers, Skeletal - cytology</topic><topic>Muscle Fibers, Skeletal - drug effects</topic><topic>Muscle Fibers, Skeletal - metabolism</topic><topic>Myocardium - cytology</topic><topic>Nifedipine - pharmacology</topic><topic>Potassium - pharmacology</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Thyroxine - pharmacokinetics</topic><topic>Triiodothyronine - pharmacokinetics</topic><topic>Verapamil - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Verhoeven, Frank A</creatorcontrib><creatorcontrib>Moerings, Ellis P. C. M</creatorcontrib><creatorcontrib>Lamers, Jos M. J</creatorcontrib><creatorcontrib>Hennemann, Georg</creatorcontrib><creatorcontrib>Visser, Theo J</creatorcontrib><creatorcontrib>Everts, Maria E</creatorcontrib><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>American journal of physiology. Heart and circulatory physiology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Verhoeven, Frank A</au><au>Moerings, Ellis P. C. M</au><au>Lamers, Jos M. J</au><au>Hennemann, Georg</au><au>Visser, Theo J</au><au>Everts, Maria E</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Inhibitory effects of calcium channel blockers on thyroid hormone uptake in neonatal rat cardiomyocytes</atitle><jtitle>American journal of physiology. Heart and circulatory physiology</jtitle><addtitle>Am J Physiol Heart Circ Physiol</addtitle><date>2001-11-01</date><risdate>2001</risdate><volume>281</volume><issue>5</issue><spage>H1985</spage><epage>H1991</epage><pages>H1985-H1991</pages><issn>0363-6135</issn><eissn>1522-1539</eissn><abstract>Departments of 1 Internal Medicine III and
2 Biochemistry, Erasmus University Medical School, 3000 DR
Rotterdam; and 3 Department of Veterinary Anatomy and
Physiology, Utrecht University, 3508 TD Utrecht, The Netherlands
The effects of the
Ca 2+ channel blockers verapamil, nifedipine, and diltiazem
on triiodothyronine (T 3 ) and thyroxine (T 4 )
uptake were tested in cultured cardiomyocytes from 2-day-old rats.
Experiments were performed at 37°C in medium with 0.5% BSA for
[ 125 I]T 3 (100 pM) or 0.1% BSA for
[ 125 I]T 4 (350 pM). The 15-min uptake of
[ 125 I]T 3 was 0.124 ± 0.013 fmol/pM free
T 3 ( n = 6);
[ 125 I]T 4 uptake was 0.032 ± 0.003 fmol/pM free T 4 ( n = 12). Neither T 3 nor T 4 uptake was affected by 1% DMSO
(diluent for nifedipine and verapamil). Uptake of
[ 125 I]T 3 but not of
[ 125 I]T 4 was dose dependently reduced by
incubation with 1-100 µM verapamil (49-87%,
P < 0.05) or nifedipine (53-81%,
P < 0.05). The relative decline in
[ 125 I]T 3 uptake after 4 h of incubation
with 10 µM verapamil or nifedipine was less than after 15 min or
1 h, indicating that the major inhibitory effect of the
Ca 2+ channel blockers occurred at the level of the plasma
membrane. The reduction of nuclear [ 125 I]T 3
binding by 10 µM verapamil or nifedipine was proportional to the
reduction of cellular [ 125 I]T 3 uptake.
Diltiazem (1-100 µM) had no dose-dependent effect on
[ 125 I]T 3 uptake but reduced
[ 125 I]T 4 uptake by 45% ( P < 0.05) at each concentration tested. Neither the presence of 20 mM
K + nor the presence of low Ca 2+ in the medium
affected [ 125 I]T 3 uptake. In conclusion, the
inhibitory effects of Ca 2+ channel blockers on
T 3 uptake in cardiomyocytes are not secondary to their
effects on Ca 2+ influx but, rather, reflect interference
with the putative T 3 carrier in the plasma membrane.
heart; culture; ATP; free hormone fraction</abstract><cop>United States</cop><pmid>11668059</pmid><doi>10.1152/ajpheart.2001.281.5.H1985</doi><oa>free_for_read</oa></addata></record> |
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identifier | ISSN: 0363-6135 |
ispartof | American journal of physiology. Heart and circulatory physiology, 2001-11, Vol.281 (5), p.H1985-H1991 |
issn | 0363-6135 1522-1539 |
language | eng |
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source | American Physiological Society Free |
subjects | Adenosine Triphosphate - metabolism Animals Animals, Newborn Biological Transport - drug effects Calcium - pharmacology Calcium Channel Blockers - pharmacology Cell Membrane - metabolism Cells, Cultured Diltiazem - pharmacology Iodine Radioisotopes Muscle Fibers, Skeletal - cytology Muscle Fibers, Skeletal - drug effects Muscle Fibers, Skeletal - metabolism Myocardium - cytology Nifedipine - pharmacology Potassium - pharmacology Rats Rats, Wistar Thyroxine - pharmacokinetics Triiodothyronine - pharmacokinetics Verapamil - pharmacology |
title | Inhibitory effects of calcium channel blockers on thyroid hormone uptake in neonatal rat cardiomyocytes |
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