L-368,899 hydrochloride
Chemical Name: (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 dihydrochloride
Purity: ≥97%
Biological Activity
L-368,899 hydrochloride is a potent, non-peptide and orally active oxytocin receptor antagonist (IC50 = 8.9 nM) that displays > 40-fold selectivity over vasopressin V1a and V2 receptors (IC50 values are 370 and 570 nM respectively). Antagonizes oxytocin-induced uterine contractions in vitro and in vivo.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
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Attenuation of PGE2α release in ewes infused with the oxyt. antagonist L-368,899.
Mann et al.
Domest.Anim.Endocrinol., 2003;25:255 -
Discovery and development of a new class of potent, selective, orally active oxyt. receptor antagonist.
Quattropani et al.
J.Med.Chem., 2005;48:7882 -
Oral oxyt. antagonists.
Borthwick
J.Med.Chem., 2010;53:6525 -
1-(((7,7-dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo[2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperazine (L-368,899): an orally bioavailable, non-peptide oxyt. antagonist with potential util
Williams et al.
J.Med.Chem., 1994;37:565
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Citations for L-368,899 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for L-368,899 hydrochloride include:
4 Citations: Showing 1 - 4
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OXT functions as a spatiotemporal filter for excitatory synaptic inputs to VTA DA neurons.
Authors: Xiao Et al.
Elife 2018;7
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Biased OXTergic Modulation of Midbrain DA Systems.
Authors: Xiao Et al.
Neuron 2017;95:368
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Oxytocin-stimulated NFAT transcriptional activation in human myometrial cells.
Authors: Pont Et al.
Mol.Endocrinol. 2012;26:1743
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The fat-induced satiety factor oleoylethanolamide suppresses feeding through central release of oxyt.
Authors: Gaetani Et al.
Nat Commun 2010;30:8096
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