Oxytocin receptor agonist

An oxytocin receptor agonist is a compound that acts as an agonist of the oxytocin receptor. They include peptides like oxytocin and carbetocin and small-molecules like LIT-001. Peptide oxytocin receptor agonists are used medically to induce labor, promote lactation, and for certain other uses.

Oxytocin receptor agonists are of theoretical interest for the potential treatment of neuropsychiatric disorders with social symptoms, such as autism, social anxiety, and psychopathy. Small-molecule oxytocin receptor agonists are considered to be more promising for such uses due to better potential pharmacokinetic profiles, such as blood–brain barrier permeability, elimination half-lives, and oral bioavailability.

List of oxytocin receptor agonists

Peptides

• Carbetocin
• Demoxytocin
• Lipo-oxytocin-1
• Merotocin
• Oxytocin
• Vasotocin

Non-peptides

• LIT-001 — improved social deficits in mice; non-selective over vasopressin receptors
• LIT-002 – highly potent, under formal development
• TC OT 39 – non-selective over vasopressin receptors
• WAY-267,464 – anxiolytic in mice; possibly non-selective over vasopressin receptors

In April 2025, a series of novel and highly potent small-molecule oxytocin receptor agonists with high selectivity over the vasopressin V_1A receptor (up to >5,000-fold) were patented and described.

Unknown

• NP-1031

Indirect

• KNX-100 (SOC-1) – pro-social and anti-addictive effects

References