L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist. It has IC50s of 8.9 nM for rat uterus and 26 nM for human uterus oxytocin receptor. This compound is used as a tocolytic agent.
- Potent oxytocin receptor antagonist.
- Selective for oxytocin receptor.
- Orally bioavailable.
- Non-peptide structure.
- Used as a tocolytic agent.
- Less active on VP receptor in human liver and kidney, and rat liver and kidney.
- Exhibits similar pharmacokinetics in rats and dogs with a t1/2 of 2 hours after a single IV injection.
- Plasma clearance between 23 and 36 ml/min/kg in rats or dogs.
- Vdss values of 2.0 and 2.6 liters/kg for rats and 3.4 to 4.9 liters/kg for dogs.
- Oral bioavailabilities in rats: 14% (female) and 18% (male) at 5 mg/kg; 17% (female) and 41% (male) at 25 mg/kg.