L-371,257

L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, 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].

Product Specifications

CAS Number

[162042-44-6]

UNSPSC

12352005

Target

Oxytocin Receptor; Vasopressin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Endocrinology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/l-371-257.html

Purity

99.90

Solubility

DMSO : 8.33 mg/mL (ultrasonic)

Smiles

O=C(OC1)N(C2CCN(C(C3=C(OC)C=C(OC4CCN(C(C)=O)CC4)C=C3)=O)CC2)C5=C1C=CC=C5

Molecular Formula

C28H33N3O6

Molecular Weight

507.58

References & Citations

[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.|[3]Jacqueline M Ho, et al. Hindbrain oxytocin receptors contribute to the effects of circulating oxytocin on food intake in male rats. Endocrinology. 2014 Aug;155 (8) :2845-57.