Document Report Card

ID: ALA1126550

Journal: J Med Chem

Title: Nanomolar-affinity, non-peptide oxytocin receptor antagonists.

Authors: Evans BE, Lundell GF, Gilbert KF, Bock MG, Rittle KE, Carroll LA, Williams PD, Pawluczyk JM, Leighton JL, Young MB.

Abstract: Non-peptide antagonists of the peptide hormone oxytocin (OT) with nanomolar OT receptor affinities are described. These compounds incorporate novel amido- and amidoalkylcamphor variations to the lead structure L-366,509 (1) to achieve receptor affinity enhancements of 2-3 orders of magnitude over that compound. The new OT antagonist L-367,773 (35) is shown to be an orally bioavailable agent with good duration in vivo and to inhibit OT-stimulated uterine contractions effectively in several in vitro and in vivo models.

CiteXplore: 8258821

DOI: 10.1021/jm00077a002