162042-44-6

162042-44-6 structure

Name: L-371257
Chemical Name: 1-[1-[4-(1-acetylpiperidin-4-yl)oxy-2-methoxybenzoyl]piperidin-4-yl]-4H-3,1-benzoxazin-2-one
CAS Number: 162042-44-6
Molecular Formula: C₂₈H₃₃N₃O₆
Molecular Weight: 507.58
Catalog: Signaling Pathways GPCR/G Protein Oxytocin Receptor
Create Date: 2017-01-08 11:03:48
Modify Date: 2024-01-11 23:04:59
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].

Name	1-[1-[4-(1-acetylpiperidin-4-yl)oxy-2-methoxybenzoyl]piperidin-4-yl]-4H-3,1-benzoxazin-2-one
Synonyms	l-371,257

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.