Drug intelligence / Profile preview

l-368,899

Development stage
Discontinued
Lead developer
Merck
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

L-368,899 is a selective, orally bioavailable, non-peptide antagonist of the oxytocin receptor with much lower activity at vasopressin receptors, making it a key tool in research for selectively blocking oxytocin-mediated signaling. It was originally developed in the 1990s by Merck for potential use in preventing preterm labor, but its primary use is now in scientific research—especially for investigating oxytocin's roles in social behavior, pair bonding, and related central nervous system functions. Studies have demonstrated that L-368,899 can reduce oxytocin-driven behaviors such as food sharing, sexual activity, and infant care in primates and has been used to probe oxytocin's effects in other mammals such as coyotes and rodents[1][4]. The drug rapidly penetrates the brain and accumulates in limbic system regions, facilitating the study of oxytocin's central effects[1][4]. L-368,899 is not approved for human use and is available only for research purposes[2].

Other names
(2S)-2-amino-N-[(2S)-7,7-dimethyl-1-[[4-(2-methylphenyl)piperazin-1-yl]sulfonylmethyl]-2-bicyclo[2.2.1]heptanyl]-4-methylsulfonylbutanamide hydrochloride1-((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo[2,2,1]heptan-1(S)-yl)methylsulfonyl)-4-(2-methylphenyl)piperazine hydrochloride160312-62-9
02

Targets

AVPR1A (Arginine vasopressin receptor 1A)Oxytocin receptor

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