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LIT-001 is the first non-peptide oxytocin receptor agonist that reaches the brain and changes behaviour after an ordinary injection into the body, rather than having to be delivered into the skull. Oxytocin itself is a therapeutic dead end for brain use for three separate reasons, and this molecule was built to defeat all three at once. It has never been given to a human being.
- Reaches the brain after peripheral dosing, which oxytocin itself cannot do
- A full agonist rather than a partial one, at 96 percent of oxytocin's own maximum
- Restored social interaction in a mouse model of autism
- A single injection gave durable relief of inflammatory pain in rats
- Partially reversed social and cognitive deficits in a rat model of schizophrenia
Mechanism
LIT-001 is a full at the human oxytocin receptor, reaching 96 percent of oxytocin's own maximum effect with a half-maximal concentration of 25 nanomolar in a calcium-release assay. That is the number that matters: many oxytocin-receptor ligands are partial agonists, and a partial agonist at a receptor this context-dependent behaves differently from the hormone it is imitating.
Selectivity is about fiftyfold over the vasopressin V1a receptor and similar over V2. ⚠️ The detail most write-ups drop is that LIT-001 is not silent at V1a; it produces almost no activation there, but it BLOCKS that receptor with a half-maximal concentration of 100 nanomolar. So at overlapping concentrations it is simultaneously an oxytocin and a vasopressin V1a , and V1a is itself deeply involved in social and territorial behaviour. Anything this molecule does socially is the sum of both actions, not the first one alone.
The property that makes it interesting at all is measured rather than inferred: after an intraperitoneal dose in mice, the compound is present in brain tissue at a measurable exposure over four hours. Oxytocin the cannot do that. Its in blood is about five minutes, its oral absorption is negligible, and it does not cross into the brain in useful amounts.
receptor fingerprint
Oxytocin receptor (OXTR)Full agonist; 96 percent of oxytocin's maximum effect, half-maximal at 25 nanomolar in a calcium-release assay in human cells
penetrationMeasured directly rather than inferred: brain exposure of 399 minute-nanograms per gram in mice after a 10 mg/kg intraperitoneal dose
Vasopressin V1a receptorFunctional ANTAGONIST rather than a silent site; almost no activation, but it blocks the receptor at 100 nanomolar, which overlaps the concentrations at which it activates oxytocin receptors
Vasopressin V2 receptorWeak binding, no functional role described
Safetyrisks and cautions, not medical advice
There is no published toxicology of any kind. No repeat-dose study, no genotoxicity work, no cardiac safety assessment, no reproductive toxicology, and no human exposure at any dose.
⚠️ The uterine question is structural to the pharmacology rather than incidental to it. The oxytocin receptor is the target of the drug used to induce labour, and it is expressed throughout the myometrium. LIT-001's entire design goal is a systemically available, brain-penetrant, full agonist at that receptor. That combination has an obvious uterotonic liability and nobody has characterised it.
⚠️ And the behavioural pharmacology carries its own warning. In prairie voles, LIT-001 given before a cohabitation period helped a pair bond form; the same dose given after cohabitation, during the expression of the bond, prevented partner preference from showing. Same drug, same dose, same species, opposite direction, depending only on when in a social sequence it was given. Two separate studies also found its social effects in males and not in females.
Regulatory status: none. It is not an approved drug anywhere, not a supplement ingredient, and has no investigational filing. Anything sold under this name is a research chemical with no human safety data at all.
Subjective profileweighing the evidence above
A genuinely interesting molecule with nothing behind it yet. LIT-001 solves the three problems that make oxytocin useless as a brain drug, and it does so with measured brain exposure rather than a hopeful assumption. But no human has taken it, no toxicology exists, and its own literature shows the social effect reversing direction depending on when it is given. Worth watching closely; not worth taking.
Resources
No suppliers are provided for compounds like this. This entry is here for reference.
Research
- 2018first citedLIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a M…
- 2024most recentEffects of oxytocin receptor agonism on acquisition and expression of pair bonding in male prai…
- 1.LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism
- 2.A Nonpeptide Oxytocin Receptor Agonist for a Durable Relief of Inflammatory Pain
- 3.Male-selective effects of oxytocin agonism on alcohol intake: behavioral assessment in socially housed prairie voles and involvement of RAGE
- 4.Oxytocin and its receptor: molecular and therapeutic approaches
- 5.Pro-social and pro-cognitive effects of LIT-001, a novel oxytocin receptor agonist in a neurodevelopmental model of schizophrenia
- 6.Effects of oxytocin receptor agonism on acquisition and expression of pair bonding in male prairie voles
6 listed here; entry last updated August 2026
Reviews
My notesprivate to this device
FAQ
Is LIT-001 the same as taking oxytocin?
No, and the difference is the reason it exists. Oxytocin has a half-life of about five minutes in blood, is barely absorbed orally, and does not reach the brain in useful amounts. LIT-001 is a small molecule built to do the same job at the same receptor while surviving long enough and crossing into the brain, which has been measured directly in mice.
Has anyone taken it?
No. There is no registered clinical trial anywhere and no published human exposure of any kind. Everything known about it comes from mice, rats and prairie voles.
Does it only affect oxytocin receptors?
No. It is about fiftyfold selective for the oxytocin receptor over vasopressin V1a by binding, but at V1a it acts as a blocker at concentrations that overlap the ones at which it activates oxytocin receptors. Vasopressin V1a is itself involved in social behaviour, so anything it does socially is the sum of both actions.
Why do the social results keep depending on sex and timing?
That is the most interesting and least comfortable finding in its literature. In prairie voles it helped a pair bond form when given beforehand and prevented partner preference from showing when given afterwards. Separate studies found effects on social interaction and alcohol intake in males and not females. Whatever it does is conditional on state rather than uniform.
Limitations of the evidence
- No human has ever taken it, at any dose, in any study
- No toxicology of any kind has been published: no repeat-dose, genotoxicity, cardiac or reproductive work
- Its social effect reverses direction depending on when in a bonding sequence it is given
- Two studies found the social and alcohol effects in male animals and not in female ones
- It blocks the vasopressin V1a receptor at overlapping concentrations, so its behavioural effects are not oxytocin agonism alone
- The oxytocin receptor is the target of the drug used to induce labour, and the uterine liability has never been characterised
Notes and cautions
- Named for the Laboratoire d'Innovation Therapeutique in Strasbourg, where it was made; it is an academic compound number rather than a pharmaceutical development code.