AMPA + kainate glutamate receptor modulation

Category: signaling

Overview

AMPA receptors carry the fast-glutamate excitatory current that underlies most synaptic transmission. Pharmacological enhancement (AMPAkines / positive allosteric modulators) is a long-standing nootropic + cognitive-enhancement target. Mechanism evidence is patchier than benzodiazepine-site GABA-A modulation but several molecules act here. Racetams (piracetam, aniracetam, oxiracetam, pramiracetam, phenylpiracetam, coluracetam, fasoracetam) — original piracetam (Giurgea 1972) coined the "nootropic" category; mechanism nominally AMPA-allosteric + cholinergic facilitation; modest clinical signal except for breath-holding spells + myoclonus. Sunifiram + idra-21 are research-stage AMPAkines. Noopept is a peptidic dipeptide claimed to be a more potent racetam-like agent with BDNF modulation. AMPA negative allosteric modulator perampanel — covered in CNS-1.

Organ Systems

Pathway Steps

Known Modulators