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L-371257

Names

[ CAS No. ]:
162042-44-6

[ Name ]:
L-371257

[Synonym ]:
l-371,257

Biological Activity

[Description]:

L-371,257 is an orally bioavailable, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM)[1][2].

[Related Catalog]:

Research Areas >> Endocrinology
Signaling Pathways >> GPCR/G Protein >> Vasopressin Receptor
Signaling Pathways >> GPCR/G Protein >> Oxytocin Receptor

[Target]

Ki: 19 nM (oxytocin receptor), 3.7 nM (vasopressin V1a receptor)[2]


[References]

[1]. Williams PD, et al. 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. 1995 Nov 10;38(23):4634-6.

[2]. Tunstall BJ, et al. Oxytocin blocks enhanced motivation for alcohol in alcohol dependence and blocks alcohol effects on GABAergic transmission in the central amygdala. PLoS Biol. 2019 Apr 16;17(4):e2006421.

Chemical & Physical Properties

[ Molecular Formula ]:
C28H33N3O6

[ Molecular Weight ]:
507.58

[ Exact Mass ]:
507.23700

[ PSA ]:
88.62000

[ LogP ]:
3.78710

[ Storage condition ]:
-20°C

Related Compounds