L-371,257

Biological Activity

L-371,257 is a potent, high affinity human oxytocin (OT) receptor antagonist (K_i = 4.6 nM) that displays > 800-fold selectivity over human arginine vasopressin receptors V_1a 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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Hindbrain oxytocin receptors contribute to the effects of circulating oxytocin on food intake in male rats.
   Ho J, Anekonda V, Thompson B, Zhu M, Curry R, Hwang B, Morton G, Schwartz M, Baskin D, Appleyard S, Blevins J
   Endocrinology, 2014;155(8):2845-57.
2. Comparison of vasopressin binding sites in human uterine and vascular smooth muscle cells.
   Tahara et al.
   Eur.J.Pharmacol., 1999;378:137
3. 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 oxyt. antagonist.
   Williams et al.
   J.Med.Chem., 1995;38:4634
4. Pharmacologic characterization of the oxyt. receptor in human uterine smooth muscle cells.
   Tahara et al.
   Br.J.Pharmacol., 2000;129:131

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