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编 号：F616062
分子式：C26H42N4O5S2
分子量：554.77
分子式：C26H42N4O5S2
分子量：554.77
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CAS No: 148927-60-0
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生物活性：
L-368,899 is an orally active and selective OT (oxytocin ) receptor antagonist, with IC50s of 8.9 and 26 nM for uterus of rat and human, respectively. L-368,899 can cross the blood-brain barrier (BBB). L-368,899 inhibits oxytocin-stimulated uterine contractions in rats and can be used in study of preterm labor.
体内研究：
L-368,899 (0.1, 0.3, 1 mg/kg; infused i.v.; single) shows a dose-related antagonism of OT-stimulated uterine contractions with an AD50 value of 0.35 mg/kg in vivo.L-368,899 (3, 10, 30 mg/kg; i.d.; single) inhibits the contractile effects of OT (AD50= 7 mg/kg) with a long (>4 h) duration of action in vivo (AD50: the dose of L-368,899 required to reduce the response to OT by 50%).L-368,899 (10 mg/kg, p.o.; single) shows bioavailability (AUC 0-6 h) of 35%.L-368,899 (0.54, 1.8, 5.4 mg/kg; i.v.; single) reduces both oxytocin-induced and endogenous increases in plasma PGFM concentration.Animal Model:Adult female Sprague-Dawley rats (250-350 g).
Dosage:0.1, 0.3, 1 mg/kg
Administration:Infused intravenous injection; single.
Result:Inhibited OT-stimulated uterine contractions with an AD50 value of 0.35 mg/kg.
Animal Model:Adult female Sprague-Dawley rats (250-350 g).
Dosage:3, 10, 30 mg/kg
Administration:Intraduodenal; single.
Result:Exhibited a antagonism of OT-stimulated uterine contractions with an AD50 of 7 mg/kg and duration of action more than 4 h.
Animal Model:Adult female Sprague-Dawley rats (250-350 g).
Dosage:10 mg/kg
Administration:Oral administration, single.
Result:Showed orally active with bioavailability (AUC 0-6 h) of 35%.
Animal Model:Mature Dorset cross ewes (53-57 kg; Removal of ovaries).
Dosage:0.54, 1.8, 5.4 mg/kg (3, 10 and 30 μg/kg/min for 3 h; dissolved in 0.9% saline).
Administration:Intravenous infusion; single.
Result:Led to a significant decrease in both the frequency (from 2.2 to 1.0 episodes/ewe) and amplitude (from 68.8 to 31.8 pg/mL) of episodes of increased plasma concentration of PGFM.
L-368,899 is an orally active and selective OT (oxytocin ) receptor antagonist, with IC50s of 8.9 and 26 nM for uterus of rat and human, respectively. L-368,899 can cross the blood-brain barrier (BBB). L-368,899 inhibits oxytocin-stimulated uterine contractions in rats and can be used in study of preterm labor.
体内研究：
L-368,899 (0.1, 0.3, 1 mg/kg; infused i.v.; single) shows a dose-related antagonism of OT-stimulated uterine contractions with an AD50 value of 0.35 mg/kg in vivo.L-368,899 (3, 10, 30 mg/kg; i.d.; single) inhibits the contractile effects of OT (AD50= 7 mg/kg) with a long (>4 h) duration of action in vivo (AD50: the dose of L-368,899 required to reduce the response to OT by 50%).L-368,899 (10 mg/kg, p.o.; single) shows bioavailability (AUC 0-6 h) of 35%.L-368,899 (0.54, 1.8, 5.4 mg/kg; i.v.; single) reduces both oxytocin-induced and endogenous increases in plasma PGFM concentration.Animal Model:Adult female Sprague-Dawley rats (250-350 g).
Dosage:0.1, 0.3, 1 mg/kg
Administration:Infused intravenous injection; single.
Result:Inhibited OT-stimulated uterine contractions with an AD50 value of 0.35 mg/kg.
Animal Model:Adult female Sprague-Dawley rats (250-350 g).
Dosage:3, 10, 30 mg/kg
Administration:Intraduodenal; single.
Result:Exhibited a antagonism of OT-stimulated uterine contractions with an AD50 of 7 mg/kg and duration of action more than 4 h.
Animal Model:Adult female Sprague-Dawley rats (250-350 g).
Dosage:10 mg/kg
Administration:Oral administration, single.
Result:Showed orally active with bioavailability (AUC 0-6 h) of 35%.
Animal Model:Mature Dorset cross ewes (53-57 kg; Removal of ovaries).
Dosage:0.54, 1.8, 5.4 mg/kg (3, 10 and 30 μg/kg/min for 3 h; dissolved in 0.9% saline).
Administration:Intravenous infusion; single.
Result:Led to a significant decrease in both the frequency (from 2.2 to 1.0 episodes/ewe) and amplitude (from 68.8 to 31.8 pg/mL) of episodes of increased plasma concentration of PGFM.
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