Oxytocin Receptor Antagonist

L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC₅₀s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 hydrochloride used as a tocolytic agent.

Atosiban (RW22164; RWJ22164) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research.

Atosiban-d₅ TFA (RW22164-d₅ TFA) is the deuterium labeled Atosiban TFA. Atosiban (RW22164; RWJ22164) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research.

Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents^[1][2].

Atosiban acetate (RW22164 acetate;RWJ22164 acetate) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research.

L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (K_i=19 nM) and vasopressin V1a receptor (K_i=3.7 nM).

Retosiban (GSK221149A) is a potent, selective, and orally active oxytocin receptor antagonist (K_i (hOT) = 0.65 nM, K_i (rOT) = 4.1 nM) with no detectable agonist activity. Retosiban has nanomolar affinity for the oxytocin receptor with >1400-fold selectivity over the closely related vasopressin receptors. Retosiban inhibits spontaneous and induces uterine contractions. Retosiban can be studied in research for preterm labour.

5β-Dihydroprogesterone (5βDHP) is the metabolite of Progesterone (HY-N0437). 5β-Dihydroprogesterone binds to oxytocin receptor, reduces the Oxytocin (HY-17571)-induced calcium signal transduction, thereby exhibiting the tocolytic activity.

SHR1653 is a highly potent, selective and brain penetrated oxytocin receptor (OTR) antagonist, with an IC₅₀ of 15 nM for hOTR.

L-372662 is a potent and orally active non-peptide oxytocin antagonist with a K_i value of 4.8. The K_d value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V_1aR.

OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist.

OT-R antagonist 2 is a nonpeptide low molecular weight OT-R antagonist.

(d(CH2)51,Tyr(Me)2,Orn8)-Oxytocin (OVT) is an oxytocin receptor antagonist. (d(CH2)51,Tyr(Me)2,Orn8)-Oxytocin can be used for the research of neurological disease.

(S)-Retosiban is the isomer of Retosiban (HY-14778), and can be used as an experimental control. Retosiban (GSK221149A) is a potent and selective oxytocin antagonist with a K_i of 0.65 nM.

Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pK_i of 9.9 for human oxytocin receptor.

L 366509 is a spiroindenylpiperidine camphorsulfonamide oxytocin (OT) antagonist. Modifications led to a new series of o-tolylpiperazine (TP) camphorsulfonamides, exhibiting high affinity for OT receptors and selectivity over arginine vasopressin receptors. Notably, compound 7 (L-368,899) showed excellent OT receptor affinity, potency in inhibiting OT-stimulated uterine contractions, good aqueous solubility, and oral bioavailability in multiple species. Compound 7 has entered clinical testing as an oral and intravenous tocolytic agent. Molecular modeling suggests the TP camphorsulfonamide structure mimics the D-AA2-Ile3 dipeptide, crucial in potent OT antagonists.

Erlosiban (OBE001) is an orally active non-peptide type oxytocin receptor antagonist. Erlosiban inhibits the increase of intracellular calcium concentration, thereby reducing uterine smooth muscle contraction. Erlosiban can be used for research on premature birth and to improve embryo implantation and pregnancy rate in assisted reproductive technology (AR).

OT antagonist 3 is an oxytocin (OT) antagonist extracted from patent WO2007017752A1.

Barusiban (FE-200440) is an oxytocin receptor (OT-R) antagonist (K_i=0.8 nM), inhibits OT-induced contraction. Barusiban can be used in preterm labor (PTL), in vitro fertilisation (IVF) and infertility research.

OT antagonist 3 analog is an analog of OT antagonist 3.