| Identification | Back Directory | [Name]
L-368,899hydrochloride | [CAS]
148927-60-0 | [Synonyms]
(2S)-2-amino-N-[(1R,3S,4S)-7,7-dimethyl-4-[[4-(2-methylphenyl)piperazin-1-yl]sulfonylmethyl]-3-bicyclo[2.2.1]heptanyl]-4-methylsulfonylbutanamide
(2S)-2-Amino-N-[(1S,2S,4R)-7,7-dimethyl-1-[[[4-(2-methylphenyl)-1-piperazinyl]sulfonyl]methyl]bicyclo[2.2.1]hept-2-yl]-4-(methylsulfonyl)butanamide | [Molecular Formula]
C26H42N4O5S2.ClH | [MOL File]
148927-60-0.mol | [Molecular Weight]
591.234 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at +4°C | [solubility ]
Chloroform (Slightly), Methanol (Slightly), Water (Slightly) | [form ]
Solid | [color ]
Off-White to Pale Yellow | [Stability:]
Hygroscopic |
| Hazard Information | Back Directory | [Biological Activity]
Potent, non-peptide and orally active oxytocin receptor antagonist (IC 50 = 8.9 nM) that displays > 40-fold selectivity over vasopressin V 1a and V 2 receptors (IC 50 values are 370 and 570 nM respectively). Antagonizes oxytocin-induced uterine contractions in vitro and in vivo . | [Uses]
L-368,899 Dihydrochloride is an oxytoxin antagonist and may be used in the treatment of early pregnancy failure. | [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 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. |
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