Subtlety of the Structure− Affinity and Structure− Efficacy Relationships around a Nonpeptide Oxytocin Receptor Agonist

…, L Boudier, T Durroux, B Mouillac…

Index: Frantz, Marie-Celine; Rodrigo, Jordi; Boudier, Laure; Durroux, Thierry; Mouillac, Bernard; Hibert, Marcel Journal of Medicinal Chemistry, 2010 , vol. 53, # 4 p. 1546 - 1562

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Citation Number: 11

Abstract

Very few nonpeptide oxytocin agonists have currently been reported, and none of them seem suitable for the in vivo investigation of the oxytocin mediated functions. In an attempt to rationalize the design of better tools, we have systematically studied the structural determinants of the affinity and efficacy of representative ligands of the V1a, V2, and OT receptor subtypes. Despite apparently obvious similarity between the ligand structures on ...