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Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin

By Bice Chini, Bernard Mouillac, Marie-Nöelle Balestre, Susanne Trumpp-Kallmeyer, Jan Hoflack, Marcel Hibert, Maria Andriolo, Sandrine Pupier, Serge Jard and Claude Barberis

Abstract

AbstractWe investigated the mechanisms that regulate the efficacy of agonists in the arginine-vasopressin (AVP)/oxytocin (OT) receptor system. In this paper, we present evidence that AVP, a full agonist of the vasopressin receptors, acts as a partial agonist on the oxytocin receptor. We also found that AVP becomes a full agonist when two aromatic residues of the oxytocin receptor are replaced by the residues present at equivalent positions in the vasopressin receptor subtypes. Our results indicate that these two residues modulate the response of the oxytocin receptor to the partial agonist AVP

Publisher: Published by Elsevier B.V.
Year: 1996
DOI identifier: 10.1016/S0014-5793(96)01135-0
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