Chloride channel blockers inhibit the Na+/I- symporter in thyroid follicles in culture.
Porcine thyroid cells in culture are able to reorganize into well-polarized follicle-like structures in the presence of cAMP analogs. These follicles exhibit on their basolateral membrane domain the Na+/I- symporter which allows iodide to accumulate in the thyrocytes. The initial rate of iodide influx through the Na+/I- symporter is inhibited up to 98% by the chloride channel blockers. 5 nitro-2(3-phenylpropylamino)benzoic acid and 3',5-Dichlorodiphenylamine-2-carboxylic acid are the most effective inhibitors, with a K0.5 value of 60 microM. This inhibition is not secondary to inhibition of chloride transport. Other chloride transporter blockers have been studied but showed lesser activities.
Gerard
C
C
INSERM, Unité 270, Faculté de Médecine Nord, Marseille, France.
Rigot
V
V
Penel
C
C
D017878:4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid / Q000494:pharmacology; D015124:8-Bromo Cyclic Adenosine Monophosphate / Q000031:analogs & derivatives / Q000494:pharmacology; D000818:Animals; D002259:Carbonyl Cyanide p-Trifluoromethoxyphenylhydrazone / Q000494:pharmacology; D002352:Carrier Proteins / Q000037:antagonists & inhibitors*; D002478:Cells, Cultured; D018118:Chloride Channels / Q000037:antagonists & inhibitors*; D004159:Diphenylamine / Q000031:analogs & derivatives / Q000494:pharmacology; D005665:Furosemide / Q000494:pharmacology; D006997:Hypochlorous Acid / Q000494:pharmacology; D007454:Iodides / Q000378:metabolism; D007457:Iodine Radioisotopes; D007700:Kinetics; D008565:Membrane Proteins / Q000037:antagonists & inhibitors*; D009579:Nitrobenzoates / Q000494:pharmacology; D011339:Probenecid / Q000494:pharmacology; D012964:Sodium / Q000378:metabolism; D013448:Sulfobromophthalein / Q000494:pharmacology; D013552:Swine; D027981:Symporters; D013961:Thyroid Gland / Q000187:drug effects / Q000378:metabolism*; D000099209:Sodium-Iodide Symporters
D017878:4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid; D015124:8-Bromo Cyclic Adenosine Monophosphate; D002259:Carbonyl Cyanide p-Trifluoromethoxyphenylhydrazone; D002352:Carrier Proteins; D018118:Chloride Channels; D004159:Diphenylamine; D005665:Furosemide; D006997:Hypochlorous Acid; D007454:Iodides; D007457:Iodine Radioisotopes; D008565:Membrane Proteins; D009579:Nitrobenzoates; D011339:Probenecid; D012964:Sodium; D013448:Sulfobromophthalein; D027981:Symporters; D000099209:Sodium-Iodide Symporters; C059537:3',5-dichlorodiphenylamine-2-carboxylic acid; C058176:5-nitro-2-(3-phenylpropylamino)benzoic acid; C044258:8-chloro-cyclic adenosine monophosphate