Neboglamine
NMDA glycine-site positive modulator and cognition enhancer; preclinical and early-phase data only.
Pharmacology
Contents
WHAT IS NEBOGLAMINE?
Detailed overview
Neboglamine (development code CR 2249) is a positive allosteric modulator of the glycine site on the NMDA glutamate receptor. Rather than mimicking glutamate directly, it enhances the effectiveness of the co-agonist glycine at the strychnine-resistant glycine site, strengthening the NMDA-mediated neurotransmission involved in learning and memory. In rodent models it improved memory retention and learning, increased hippocampal noradrenaline release, and showed antipsychotic-like activity. The compound reached early (Phase II) clinical trials as an adjunct for the negative and cognitive symptoms of schizophrenia but was never approved anywhere, and human data remain sparse.
Mechanism
NMDA glycine-site positive modulator
Evidence
Mostly preclinical (early-phase human)
Legal status
Unapproved investigational compound
Receptor profile
- NMDA receptor glycine site (positive modulator)Strong
- NMDA-mediated glutamatergic neurotransmissionModerate
- Hippocampal noradrenaline releaseModerate
Safety
Side effects, stop signs, contraindications
Side effects · 4
- Poorly characterized safety profile: human data are sparse and most knowledge comes from preclinical studies
- Theoretical risk of NMDA facilitation: excessive glutamatergic excitation and excitotoxicity at high doses
- Unknown long-term safety in humans
- Detailed tolerability data from early-phase clinical trials are not adequately published
Contraindications · 4
- Pregnancy and breastfeeding: safety not established, avoid
- Epilepsy or lowered seizure threshold: NMDA facilitation may theoretically increase seizure risk
- Interaction expected alongside NMDA-antagonist therapy (e.g. ketamine, memantine), avoid
- Not an approved medicine; an investigational compound, not recommended without clinical supervision
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Antipsychotic-like effects of the N-methyl-D-aspartate receptor modulator neboglamine: an immunohistochemical and behavioural study in the rat
Chiusaroli R, Piccinelli M, Comi E, et al
Characterization of a novel putative cognition enhancer mediating facilitation of glycine effect on strychnine-resistant sites coupled to NMDA receptor complex
Lanza M, Makovec F, Cavanni P, et al
The 'kynurenate test', a biochemical assay for putative cognition enhancers
Pittaluga A, Pattarini R, Raiteri M
CR 2249: a new putative memory enhancer. Behavioural studies on learning and memory in rats and mice
Garofalo P, Colombo S, Lanza M, et al
FAQ
FAQ
NMDA glycine-site positive modulator and cognition enhancer; preclinical and early-phase data only.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.