L-368,899 HYDROCHLORIDE性质、用途与生产工艺
L-368,899 hydrochloride 是一种有效的，选择性的，可口服的，非肽类催产素受体 oxytocin receptor 拮抗剂，对大鼠和人子宫 oxytocin receptor 的 IC50 值分别为 8.9 nM 和 26 nM，为抗早产剂。
IC50: 8.9 nM (rat uterus oxytocin receptor), 26 nM (human uterus oxytocin receptor)
L-368,899 hydrochloride is a potent, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC
50
s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 is less active on VP receptor in human liver and kidney, rat liver and kidney (IC
50
, 510 nM, 960 nM, 890 nM, 2400 nM, respectively).
L-368,899 exhibits similar pharmacokinetics in rats and dogs. After a single iv. injection, L-368,899 had a t
1/2
of 2 hr in both species. Additionally, L-368,899 has a plasma clearance between 23 and 36 ml/min/kg in rats or dogs. L-368,899 exhibits V
dss
values of 2.0 and 2.6 liters/kg and 3.4 to 4.9 liters/kg for dogs, respectively.
L-368,899 is orally available. In the rat, at the 5 mg/kg dose, the oral bioavailabilities are 14% and 18% for female and male rats, respectively. Additionally, the oral bioavailabilities are 17% and 41% for female and male rats, respectively at the dosage of 25 mg/kg.
L-368,899 HYDROCHLORIDE
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