Nitrous Oxide - Neuropharmacology

Neuropharmacology

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, GABA_C, and 5-HT₃ receptors, and slightly potentiates GABA_A 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 be related to its analgesic and anxiolytic properties.