Phenelzine sulfate

Phenelzine is an inhibitor of monoamine oxidase (MAO; IC₅₀ = 0.9 μM using rat brain mitochondrial preparations).¹ It potentiates the effects of tryptamine on isolated rat fundus (EC₅₀ = 90 nM) and increases tryptamine toxicity in mice with LD₅₀ values of 85 and 500 mg/kg in the presence and absence of phenelzine, respectively. Phenelzine (20 mg/kg) increases GABA, dopamine, serotonin , and norepinephrine levels in the hippocampus and cortex of socially isolated rats and rats treated with the NMDA receptor antagonist (+)-MK-801 .² It also increases 5-HT levels in the ventral horn of the spinal cord, improves gross motor ability in a rotarod test, and increases locomotor activity in an open field test in mice with experimental autoimmune encephalomyelitis when administered at a dose of 30 mg/kg.³

1.Maxwell, D.R., Gray, W.R., and Taylor, E.M.Relative activity of some inhibitors of mono-amine oxidase in potentiating the action of tryptamine in vitro and in vivoBr. J. Pharmacol. Chemother.17(3)310-320(1961) 2.Simpson, S.M., Hickey, A.J., Baker, G.B., et al.The antidepressant phenelzine enhances memory in the double Y-maze and increases GABA levels in the hippocampus and frontal cortex of ratsPharmacol. Biochem. Behav.102(1)109-117(2012) 3.Musgrave, T., Benson, C., Wong, G., et al.The MAO inhibitor phenelzine improves functional outcomes in mice with experimental autoimmune encephalomyelitis (EAE)Brain Behav. Immun.25(8)1677-1688(2011)