Catalog Number: 2410
Chemical Name: 1-[4-[(1-Acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]-4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidine
Biological Activity
Potent, high affinity human oxytocin (OT) receptor antagonist (Ki = 4.6 nM) that displays > 800-fold selectivity over human arginine vasopressin receptors V1a and V2. Antagonizes oxytocin-induced contractions in isolated rat uterine tissue (pA2 = 8.44) and in anesthetised rats following intravenous and intraduodenal administration. Decreases length of U-87MG cell projections induced by retinoic acid (Cat.No.0695). Orally active.
Technical Data
  • M.Wt:
    507.59
  • Formula:
    C28H33N3O6
  • Solubility:
    Soluble to 10 mM in DMSO with gentle warming
  • Purity:
    >99%
  • Storage:
    Store at RT
  • CAS No:
    162042-44-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. 1-{1-[4-[N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4-yl}-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.
    Williams et al.
    J.Med.Chem., 1995;38:4634
  2. Comparison of vasopressin binding sites in human uterine and vascular smooth muscle cells.
    Tahara et al.
    Eur.J.Pharmacol., 1999;378:137
  3. Pharmacologic characterization of the oxytocin receptor in human uterine smooth muscle cells.
    Tahara et al.
    Br.J.Pharmacol., 2000;129:131
Citations:

The citations listed below are publications that use Tocris products. Selected citations for L-371,257 include:

2 Citations: Showing 1 - 2
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  1. Downregulation of oxytocin receptor decreases the length of projections stimulated by retinoic acid in the U-87MG cells.
    Authors: Lestanova Et al.
    Neurochem.Res. 2017;42:1006
  2. Alteration of antral and proximal colonic motility induced by chronic psychological stress involves central urocortin 3 and vasopressin in rats.
    Authors: Ataka Et al.
    Am J Physiol Gastrointest Liver Physiol 2012;303:G519

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