LIT-001 is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 improves social interaction in a mouse model of autism[1].
In vitro signaling experiments, LIT-001 is a nonbiased OT-R agonist on the two main signaling pathways of this receptor, with minor antagonist effect on V1a and agonist effect on V1b receptors, observed at high concentrations only[1].
LIT-001 (10-20 mg/kg; i.p.) alleviates core symptoms in the context of autism spectrum disorders (ASD )[1]. Animal Model: Oprm1-/- mice (bred in house on a 50% 129SVPas-50% C57BL/6J hybrid background)[1]
[1]. Frantz MC, et al. LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism. J Med Chem. 2018 Oct 11;61(19):8670-8692.