Neboglamine — Safety, Research, Risks & Legal Status

Not medical advice. Neboglamine is discussed here for informational and harm-reduction purposes only. We do not endorse use, and any dosing context is informational, not a protocol.

Also known as	CR-2249, CR 2249, XY-2401, nebostinel (former name); chemically (S)-4-amino-N-(4,4-dimethylcyclohexyl)glutaramic acid
Category	Research Chemical
Drug class	NMDA receptor glycine-site positive allosteric / functional modulator
Developer	Rottapharm (development codes CR-2249, XY-2401)
Highest development phase	Phase II (schizophrenia and cocaine dependence); not approved
CAS / UNII	CAS 163000-63-3; UNII 12EA34U5B8
Chemistry	(S)-4-amino-N-(4,4-dimethylcyclohexyl)glutaramic acid; C13H24N2O3, ~256.35 g/mol
Human efficacy	Not demonstrated; no positive Phase II results published
US legal status	Investigational drug with no marketing approval anywhere. Neboglamine is not an FDA-approved medicine and is not a dietary supplement. It reached Phase II clinical testing (developed by Rottapharm) but was never approved and appears to be dormant or discontinued. It has no legal status as a consumer product in the United States; material sold under this name is offered only as a "for research use only, not for human consumption" laboratory chemical. We do not sell it. This page is informational only.

What is Neboglamine?

Neboglamine is a small-molecule glutamic-acid derivative that acts as a positive allosteric modulator (functional modulator) at the glycine co-agonist site of the NMDA glutamate receptor. It was developed by Rottapharm and studied primarily as a potential treatment for schizophrenia (targeting negative and cognitive symptoms) and, secondarily, for cocaine dependence. It is an obscure investigational compound: the publicly available evidence is largely preclinical plus limited early-phase clinical activity, and no positive human efficacy results have been published. Treat any strong claim about its benefits in humans as unproven.

How it works

Neboglamine binds the strychnine-insensitive glycine co-agonist site of the NMDA receptor complex and acts as a positive allosteric / functional modulator, facilitating glycine- and D-serine-dependent NMDA receptor activation without directly agonizing the glutamate binding site. The therapeutic rationale is the NMDA-hypofunction hypothesis of schizophrenia: by enhancing physiologic NMDA signaling rather than forcing channel opening, a glycine-site modulator is proposed to correct receptor hypofunction while avoiding the excitotoxicity associated with direct glutamate-site agonism. A reported binding potency on the order of ~10 microM (Ki) has been cited. Separately, preclinical microdialysis has suggested a secondary effect of raising extracellular norepinephrine via a norepinephrine-transporter (desipramine-like) mechanism. These mechanisms are drawn from binding and animal studies; they are not confirmed clinical mechanisms of benefit in humans.

Background & history

Neboglamine originated at Rottapharm (Italy) under the development code CR-2249 (also XY-2401), and was earlier assigned the name nebostinel. It was characterized in the 1990s and 2000s as an NMDA glycine-site modulator with cognition-enhancing and antipsychotic-like properties in animal models, and is the subject of patents covering its use as an antipsychotic and neuroprotective agent. After Phase I, it advanced to Phase II clinical evaluation for schizophrenia and for cocaine dependence, with the last widely reported status update around mid-2015. No approval followed, and there is no visible evidence of continued advancement, leaving it best described as a stalled or discontinued investigational compound.

What the research says

The published record is dominated by animal and mechanistic work; robust human data are lacking. Preclinical studies in rodents reported cognition- and memory-enhancing effects, reversal of NMDA-antagonist (PCP)-induced hyperlocomotion and behavioral disruption, and increased Fos-like immunoreactivity in the prefrontal cortex, nucleus accumbens, and lateral septal nucleus, consistent with an antipsychotic-like preclinical signature. The compound advanced to Phase II trials (reported status as of mid-2015) for schizophrenia and cocaine abuse after completing Phase I, but no peer-reviewed Phase II efficacy or safety results appear to have been published, and development has not visibly progressed since. There are no known large randomized controlled trials demonstrating clinical benefit. Evidence quality for any human use should be considered very limited and preliminary.

Reported effects

Reported in animal models only: cognition- and memory-enhancing effects on learning/memory tasks
Preclinical reversal of NMDA-antagonist (PCP)-induced behavioral abnormalities, an antipsychotic-like signature
Hypothesized enhancement of NMDA-receptor signaling in cortical and limbic circuits (mechanistic, not a demonstrated human outcome)
Increased regional neuronal activation markers (Fos-like immunoreactivity) in prefrontal cortex, nucleus accumbens, and lateral septum in rats
No established, replicated clinical effects in humans; human efficacy is unproven

Dosing & administration (informational)

Informational only, not a protocol and not medical advice. No validated human dose exists because neboglamine was never approved and no Phase II dosing regimen has been published in the accessible literature. Any figures circulating online are not backed by demonstrated safety or efficacy in humans. We do not provide a dose. Anyone with a clinical question about NMDA-modulating agents should consult a licensed physician.

This is general research/context information, not medical advice or a recommended protocol.

Safety & side effects

No adequate human safety data are published; the long-term safety profile in people is essentially unknown
Not approved by any regulatory agency and not intended for human consumption
Mechanistically modulates NMDA receptor signaling, a pathway involved in excitotoxicity, seizure threshold, and cognition; theoretical CNS risks cannot be excluded without human data
Preclinical microdialysis suggests it can raise extracellular norepinephrine (a desipramine-like, norepinephrine-transporter-related effect), which raises theoretical concerns about interactions with other noradrenergic or serotonergic drugs
Purity, identity, and dose of any material sold as neboglamine are unverified; contamination and mislabeling are realistic risks for an obscure research chemical
Anyone considering any NMDA-modulating substance should consult a licensed clinician first

Drug & supplement interactions

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Who should avoid it

Anyone who is pregnant, may become pregnant, or is breastfeeding
People with a seizure disorder or other significant neurological or psychiatric condition, given unknown CNS effects
Anyone taking psychiatric, antidepressant, stimulant, or other centrally acting medications, because interactions are uncharacterized
People seeking an approved, evidence-based treatment for schizophrenia or substance-use disorder, who should use approved therapies under clinician care instead
Anyone expecting a proven cognitive or antipsychotic benefit, since human efficacy is unestablished

How it is commonly combined

There is no evidence base for combining neboglamine with any other substance in humans, and we do not recommend it. Stacking an unapproved NMDA-modulating research chemical with other centrally active compounds compounds unknown risks, including potential additive effects on glutamatergic and noradrenergic signaling. Any framing of neboglamine as a nootropic "stack" component is unsupported by human data.

Legal & regulatory. Investigational drug with no marketing approval anywhere. Neboglamine is not an FDA-approved medicine and is not a dietary supplement. It reached Phase II clinical testing (developed by Rottapharm) but was never approved and appears to be dormant or discontinued. It has no legal status as a consumer product in the United States; material sold under this name is offered only as a "for research use only, not for human consumption" laboratory chemical. We do not sell it. This page is informational only.

Quality & harm reduction

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Frequently asked questions

Is neboglamine an approved medicine?

No. It is an investigational compound that reached Phase II trials for schizophrenia and cocaine dependence but was never approved by any regulatory agency and appears to have stalled. It is not available as a prescription drug or as a supplement.

Does it actually improve cognition or treat schizophrenia in people?

That is unproven. The encouraging results are from animal models and mechanistic studies. No published human trial has demonstrated clinical benefit, so any claim of a cognitive or antipsychotic effect in people is not supported by the available evidence.

What dose should I take?

We do not provide dosing. There is no validated human dose, no published Phase II regimen, and no established safety margin. Any numbers found online are unsupported. If you have a clinical question, consult a licensed physician.

Is it safe?

Its safety in humans is essentially unknown because adequate human safety data have not been published. It is not intended for human consumption, and material sold under this name is an unregulated research chemical of uncertain identity and purity.

How is it different from D-serine, sarcosine, or D-cycloserine?

All of these act at or feed the NMDA glycine co-agonist site, but D-serine and glycine are direct co-agonists, sarcosine is a glycine-reuptake (GlyT1) inhibitor, and D-cycloserine is a partial agonist. Neboglamine is described as an allosteric/functional modulator of that site. Those better-studied agents have far more human data than neboglamine, though none is an established cure for schizophrenia.

Can I still buy it, and is that legal?

It may be listed by some laboratory chemical suppliers as a research-use-only material, not as a consumer product. It is not legal to sell for human consumption. We do not sell it, and this page is informational only.

References & further reading

PubMed: neboglamine NMDA glycine site schizophrenia
PubMed: neboglamine CR-2249 antipsychotic-like immunohistochemical behavioural rat
PubMed: CR 2249 cognition enhancing NMDA glycine site modulator
ClinicalTrials.gov: neboglamine schizophrenia
ClinicalTrials.gov: neboglamine cocaine dependence