OT antagonist 1 (Compound 4) is a potent, selective Oxytocin antagonist with a Ki of 50 nM.
Oxytocin (OT) is a nonapeptide hormone that acts on the OT receptor, a seven-transmembrane (7TM) (Gq-coupled) receptor. The OT receptor has no subtypes but is related to the vasopressin receptors V1A, V1B and V2. OT antagonists have therapeutic potential in a number of areas including pre-term labour: Benign Prostatic Hyperplasia and sexual dysfunction. As a result there is significant interest in the identification of potent, selective, orally bioavailable OT antagonists[1].
[1]. Brown A, et al. Design and optimization of potent, selective antagonists of Oxytocin. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4278-81.