Neboglamine 10 mg – 60 capsules

Neboglamine 10 mg — 60 oral research capsules. Neboglamine (CR-2249, also known as nebostinel) is a modulator of the glycine co-agonist site of the NMDA receptor, developed as a cognition-enhancing research compound and advanced through Phase II clinical investigation. Unlike direct NMDA agonists, it acts on the regulatory glycine site and potentiates receptor signalling only where endogenous glutamate transmission is already present — the same functional class as D-serine and D-cycloserine, but with an oral, small-molecule profile that makes it a practical tool compound for glutamatergic research.

Research Overview

Neboglamine is a small-molecule modulator of the glycine-binding site of the N-methyl-D-aspartate (NMDA) receptor, the principal mediator of slow excitatory neurotransmission and synaptic plasticity in the mammalian brain. In published preclinical work it restored NMDA-mediated signalling under pharmacological blockade and produced antipsychotic-like behavioural profiles in rodent models, without the sedative or cataleptic signature of dopamine-receptor antagonists [1]. Its activity has also been characterised in animal cognition paradigms, where glycine-site modulation is associated with enhanced learning and memory performance [3]. The compound reached Phase II clinical investigation and remains a reference tool for studying glycine-site pharmacology alongside D-serine and D-cycloserine [2]. No therapeutic or clinical claims are made or implied.

Primary Research Areas

• NMDA receptor glycine-site modulation — the defining mechanism — studied for potentiation of NMDA-mediated signalling at the glycine co-agonist site, in the same functional class as D-serine and D-cycloserine [1,3].
• Antipsychotic-model behavioural research — evaluated in PCP-induced hyperlocomotion and rearing paradigms in the rat, a standard preclinical screen for antipsychotic-like pharmacological activity [1].
• Cognition and memory research — characterised in animal cognition paradigms for effects on learning and memory, consistent with the profile reported for glycine-site NMDA modulators [3].
• Forebrain neuronal activation mapping — applied in Fos-like immunoreactivity studies mapping activation in the prefrontal cortex, nucleus accumbens and lateral septal nucleus [1].
• Glutamatergic pathway pharmacology — used as a research comparator in work on glycine-binding-site stimulants and their influence on downstream dopaminergic signalling [2].

References

1. Chiusaroli R, Garofalo P, Espinoza S, Neri E, Caselli G, Lanza M. Antipsychotic-like effects of the N-methyl-D-aspartate receptor modulator neboglamine: an immunohistochemical and behavioural study in the rat. Pharmacol Res. 2010;61(5):430–436.
2. Shimizu S, Sogabe S, Yanagisako R, Inada A, Yamanaka M, Iha HA, Ohno Y. Glycine-binding site stimulants of NMDA receptors alleviate extrapyramidal motor disorders by activating the nigrostriatal dopaminergic pathway. Int J Mol Sci. 2017;18(7):1416.
3. Lanza M, Makovec F. Cognition enhancing profile of CR 2249, a new NMDA-glycine site modulator. CNS Drug Rev. 1997;3(3):245–259.