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[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 AD50 value 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 AD50 of 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. |
