The pharmacological mechanism of action of N2O in medicine is not fully known. However, it has been shown to directly modulate a broad range of ligand-gated ion channels, and this likely plays a major role in many of its effects. It moderately blocks NMDA and β2-subunit-containing nACh channels, weakly inhibits AMPA, kainate, GABAC, and 5-HT3 receptors, and slightly potentiates GABAA and glycine receptors. It has also been shown to activate two-pore-domain K+ channels. While N2O affects quite a few ion channels, its anesthetic, hallucinogenic, and euphoriant effects are likely caused predominantly or fully via inhibition of NMDAR-mediated currents. In addition to its effects on ion channels, N2O may act to imitate nitric oxide (NO) in the central nervous system as well, and this may relate to its analgesic and anxiolytic properties.
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