Chini B, Mouillac B, Balestre M N, Trumpp-Kallmeyer S, Hoflack J, Hibert M, Andriolo M, Pupier S, Jard S, Barberis C
CNR Cellular and Molecular Pharmacology Center, Milan, Italy.
FEBS Lett. 1996 Nov 18;397(2-3):201-6. doi: 10.1016/s0014-5793(96)01135-0.
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.
我们研究了调节精氨酸加压素（AVP）/催产素（OT）受体系统中激动剂效力的机制。在本文中，我们提供证据表明，加压素受体的完全激动剂AVP对催产素受体起部分激动剂的作用。我们还发现，当催产素受体的两个芳香族残基被加压素受体亚型中相应位置的残基取代时，AVP就会变成完全激动剂。我们的结果表明，这两个残基调节催产素受体对部分激动剂AVP的反应。
