title: The K channel blocker, tetraethylammonium, displaces beta-endorphin and naloxone from T-cell binding sites.
abstract: Beta-endorphin and naloxone bind to Jurkat cell membrane preparations and can mutually displace each other from membrane binding sites. Tetraethylammonium ion, a potassium channel blocker, competitively displaces beta-endorphin and naloxone from membrane binding sites. Mitogen stimulated calcium ion flux is inhibited by tetraethyl ammonium and this inhibition is relieved by naloxone. With data derived from whole cell calcium ion flux studies, we accurately calculated the competitive displacement of beta-endorphin and naloxone from membrane preparations by tetraethylammonium thus showing that the action of these agents on potassium channels does not require second messengers. Using the resuspension induced ion flux technique, we find that beta-endorphin competes against naloxone for binding to Jurkat cells and naloxone competes against charybdotoxin, a potassium channel inhibitor, which like tetraethylammonium, is known to bind to the outer vestibule of the channel. Patch clamp electrophysiological studies show that beta-endorphin and naloxone exert complex actions on potassium channels in the presence or absence of mitogens. We conclude that one molecule of beta-endorphin or naloxone, but not both at the same time, bind to an area near the charybdotoxin/tetraethylammonium binding locus of Jurkat potassium channels.
authors.affiliation: New Ideas Co., Rockville, MD 20852, USA.
authors.forename: D B
authors.initials: DB
authors.lastname: Millar
authors.forename: D L
authors.initials: DL
authors.lastname: Mazorow
authors.forename: C
authors.initials: C
authors.lastname: Hough
mesh_terms: D001665:Binding Sites; D001667:Binding, Competitive; D002121:Calcium Channel Blockers / Q000494:pharmacology; D018999:Charybdotoxin / Q000494:pharmacology; D004594:Electrophysiology; D008934:Mitogens / Q000494:pharmacology; D009270:Naloxone / Q000378:metabolism* / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000378:metabolism* / Q000494:pharmacology; D026902:Potassium Channel Blockers; D015221:Potassium Channels / Q000187:drug effects / Q000502:physiology; D016271:Proto-Oncogene Proteins c-myc / Q000378:metabolism; D000644:Quaternary Ammonium Compounds / Q000494:pharmacology; D013601:T-Lymphocytes / Q000378:metabolism*; D019789:Tetraethylammonium; D013757:Tetraethylammonium Compounds / Q000378:metabolism* / Q000494:pharmacology; D014407:Tumor Cells, Cultured; D001615:beta-Endorphin / Q000378:metabolism* / Q000494:pharmacology
chemical_list: D002121:Calcium Channel Blockers; D008934:Mitogens; D009292:Narcotic Antagonists; D026902:Potassium Channel Blockers; D015221:Potassium Channels; D016271:Proto-Oncogene Proteins c-myc; D000644:Quaternary Ammonium Compounds; D013757:Tetraethylammonium Compounds; D018999:Charybdotoxin; D009270:Naloxone; D001615:beta-Endorphin; D019789:Tetraethylammonium; C027917:tetramethylammonium