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NMDA Receptor containing NR2B subunit

Negative allosteric modulators (NAMs) targeting the NR2B subunit of the NMDA receptor, like InFlectis drugs, have gained interest due to several advantages over first-generation NMDAR NAMs used as analgesics. These first-generation of NAMs often had unacceptable side effects, including hallucinations and cognitive impairment. Here are the key reasons:

Selectivity: NR2B-specific NAMs selectively target the GluN2B subunit of NMDARs. This specificity allows for more precise modulation without affecting other NMDAR subtypes that contain different subunits (such as NR2A, NR2C, etc.). In contrast, first-generation NAMS lacked this selectivity, leading to broader effects.

Reduced Side Effects: By specifically antagonizing NR2B-containing NMDARs, these modulators avoid the adverse effects associated with first-generation NAMs due to their non-specific action. The clinical safety of the InFlectis drug candidate IFB-088 has been assessed in human healthy volunteers and is devoid of adverse effects associated with first-generation NMDAR NAMs.

NR2B-specific NAMs hold promise for treating various neurological disorders, including neurodegenerative diseases and their often-associated symptoms, like chronic pain and depression. By antagonizing NMDA receptors containing the NR2B subunit, InFlectis drugs offer a more refined approach to selectively inhibit glutamate-mediated excitotoxicity which leads to mitochondrial dysfunction and calcium-dependent neurotoxicity, while minimizing side effects.

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