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Category:
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7TM Receptors Peptides (Hypothalamic/Pituitary Hormones)Vasopressin and Oxytocin Receptors
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Cat.No.
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Product Name
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2410 |
L-371,257
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Price and Availability
Click here for full price details of
L-371,257
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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 |
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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.
Antagonises oxytocin-induced contractions in isolated rat uterine tissue (pA2
= 8.44) and in anaesthetised rats following intravenous and intraduodenal
administration. Orally active.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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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. Tahara et al (1999) Comparison
of vasopressin binding sites in human uterine and vascular smooth muscle cells.
Eur.J.Pharmacol. 378 137. Tahara et al (2000)
Pharmacologic characterization of the oxytocin receptor in human uterine smooth
muscle cells. Br.J.Pharmacol. 129 131.
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Keywords: L-371,257, Peptides (Hypothalamic / Pituitary Hormones), Potent & Selective Oxytocin Receptor Antagonist, L371,257, Tocris Bioscience
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