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L-371,257

Cat. No. 2410

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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 (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. 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.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Williams et al (1995) 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. J.Med.Chem. 38 4634. PMID: 7473590.

Tahara et al (1999) Comparison of vasopressin binding sites in human uterine and vascular smooth muscle cells. Eur.J.Pharmacol. 378 137. PMID: 10478574.

Tahara et al (2000) Pharmacologic characterization of the oxytocin receptor in human uterine smooth muscle cells. Br.J.Pharmacol. 129 131. PMID: 10694212.

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Keywords: L-371,257, supplier, Potent, selective, oxytocin, receptors, antagonists, OT, Receptors, L371257

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7-TM Receptor Signaling

Written by T. Kenakin et al

'Seven Transmembrane Receptor Signaling' highlights the multiple behaviors of 7-TMs including G-protein-dependent and -independent signaling as well as the concept of collateral efficacy