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Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin
Author(s) -
Chini Bice,
Mouillac Bernard,
Balestre Marie-Nöelle,
Trumpp-Kallmeyer Susanne,
Hoflack Jan,
Hibert Marcel,
Andriolo Maria,
Pupier Sandrine,
Jard Serge,
Barberis Claude
Publication year - 1996
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/s0014-5793(96)01135-0
Subject(s) - vasopressin , agonist , oxytocin , partial agonist , arginine vasopressin receptor 1b , vasopressin receptor , receptor , endocrinology , oxytocin receptor , arginine vasopressin receptor 2 , chemistry , arginine , medicine , endogenous agonist , pharmacology , biology , biochemistry , amino acid , antagonist , dopamine receptor d1
We 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.