Target nature :
CAS n° :
Mecanism of action :
Binding affinity of the probe on Oxytocin receptor in cells was determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged OT receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.
Physico-chemical properties :
pKi 6.7 (Ki 2.26x10-7 M)
Probe availability :
Available at LIT (Laboratoire d'innovation thérapeutique) Illkirch, France
Princeps reference :
Frantz MC, Pellissier L, Pflimlin E, Loison S, Gandia J, Marsol C, Durroux T, Mouillac B, Becker J, Le Merrer J, Valencia C, Villa P, Bonnet D, Hibert M. (2018) LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism. J. Med. Chem. 2018, 61, 8670¿8692
More bibliography :
Other available information on the probe :
LIT-001 is a non-peptide oxytocin (OT) receptor agonist. The compound is brain penetrant and active in vivo by intraperitoneal injection. OT receptor agonists are predicted to promote prosocial effects in individuals with disorders such as autism spectrum disorders (ASD), who exhibit social interaction deficits. LIT-001 provides an in vivo pharmacological tool compound that is suitable for furthering the study of the effects of OT receptor agonism in autism.
Other information on the target :
Selectivity profile :
Activation of V2 receptors by LIT-001 is unlikely to impact social behaviour as V2 receptors are not expressed in the central nervous system, but it may contribute to fluid retention.
In vivo data :
Peripheral intraperitoneal administration of LIT-001 leads to a reduction in social interaction deficits in the Oprm1-/- mouse model of autism.
In vitro data :
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