L-368,899 是一种口服有效的选择性催产素受体 oxytocin receptor 拮抗剂，对大鼠和人子宫 oxytocin receptor 的IC50值分别为 8.9 和 26 nM。L-368,899 可穿过血脑屏障。L-368,899 能抑制大鼠和恒河猴中催产素刺激的子宫收缩，可用于早产的研究。
| 生物活性 | L-368,899 is an orally active and selectiveOT (oxytocin ) receptorantagonist, withIC50s 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[1][2][3]. |
| IC50& Target | IC50: 8.9 nM (rat uterus), 26 nM (human uterus)[3]. |
体内研究
(In Vivo) | 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 AD50value of 0.35 mg/kg in vivo[1].
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%)[1].
L-368,899 (10 mg/kg, p.o.; single) shows bioavailability (AUC 0-6 h) of 35%[1].
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[2].
| Animal Model: | Adult female Sprague-Dawley rats (250-350 g)[1]. | | Dosage: | 0.1, 0.3, 1 mg/kg | | Administration: | Infused intravenous injection; single. | | Result: | Inhibited OT-stimulated uterine contractions with an AD50value of 0.35 mg/kg. |
| Animal Model: | Adult female Sprague-Dawley rats (250-350 g)[1]. | | Dosage: | 3, 10, 30 mg/kg | | Administration: | Intraduodenal; single. | | Result: | Exhibited a antagonism of OT-stimulated uterine contractions with an AD50of 7 mg/kg and duration of action more than 4 h. |
| Animal Model: | Adult female Sprague-Dawley rats (250-350 g)[1]. | | 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)[2]. | | 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. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
m.cnreagent.com