Epelsiban (GSK557296), a pyridyl-2,5-diketopiperazine, is a potent, highly selective, and orally bioavailable non-peptide oxytocin receptor antagonist. GlaxoSmithKline was developing epelsiban for the treatment of women infertility due to adenomyosis and premature ejaculation.

Merotocin (FE-202767 or carba-1-[4-FBzlGly(7)]dOT) is a selective peptidic oxytocin receptor agonist. It is currently in clinical development for the treatment of preterm mothers requiring lactation support.

PF-3274167 (Cligosiban) is a potent, selective, brain penetrant oxytocin receptor antagonist. Cligosiban interrupts the expulsion phase of ejaculation by reducing the normal bulbospongiosum burst pattern and reducing the expulsions that accompany bursts. Cligosiban represents a promising compound to test the clinical hypothesis that antagonism of central oxytocin receptors may be of therapeutic benefit in the treatment of premature ejaculation. [11C]PF-3274167 is not a suitable tracer for imaging of OTR in rat brain, probably because of a too low affinity for this receptor in addition to a poor brain penetration. PF-3274167 had been in phase I clinical trial for the treatment of sexual function disorders and urinary incontinence. However, this research has been discontinued.

Erlosiban (OBE-001 or Nolasiban) is an oral oxytocin receptor antagonist. Erlosiban inhibits myometrium contractions and inflammation elicited by oxytocin. Erlosiban has the potential to decrease contractions and improve uterine blood flow hence enhancing the receptivity of the endometrium to embryo implantation. This may increase the rates of successful implantation, clinical pregnancy, and live-births among patients undergoing ART, or more specifically IVF procedures.

WAY 267464 dihydrochloride is a potent and selective agonist at the oxytocin receptor (OTR). WAY 267464 has been shown to cross the blood-brain-barrier to a significantly greater extent than exogenously applied oxytocin. WAY 267464 dose-dependently reduced anxiety on the four-plate test and prevented the deficits in prepulse inhibition induced by MK-801 or amphetamine. The ability of WAY 267464 to function as a V1AR antagonist may limit its potential therapeutic use in humans, as it would conceivably prevent the improvements in social behavior and social cognition that may be assumed to arise from a primary OTR agonist action.

TC OT 39 was developed as potent non-peptide oxytocin receptor partial agonist and V2 vasopressin receptor agonist. Also was a V1a vasopressin receptor antagonist.

OPC-21268, a non-peptide vasopressin V1 receptor antagonist, inhibited oxytocin- and vasopressin-induced contractions of myometrial strips from rats and from full-term pregnant women. OPC-21268, because of its non-peptide structure, is orally active and has been shown to lower blood pressure in a patient with congestive heart failure and in spontaneously hypertensive rats. It also attenuates vasopressin induced bradycardia in rabbits and pressor responses in rats. It has been demonstrated that OPC-21268 exerts its inhibitory action through binding to the vasopressin V1 receptors in rat liver and kidney. Finally, OPC-21268 was reported to be safe and non-toxic in healthy humans. Merck scientists showed that OPC-21268 had significant affinity for the rOTR and the hOTR. OPC-21268 has been in phase II clinical trials by Otsuka for the treatment of heart failure and hypertension. However, this research has been discontinued.

L-368,899 is a potent and selective oxytocin (OT) receptor antagonist, which was developed by Merc as a promising non peptide OT antagonist. However, this compound failed in clinical development; phase II, for the treatment of premature labour. Merck subsequently abandoned its non peptide OT antagonist program.

Carbetocin is a synthetic analogue of human peptide hormone, oxytocin. Like oxytocin, it stimulate oxytocin receptors and is used to facilitate childbirth. The drug is being marketed in Europe under the name Pabal for the prevention of uterine atony following delivery of the infant by Caesarean section. If untreated by carbetocin, uterine atony may lead to postpartum haemorrhage.