Cayman Isocarboxazid

Isocarboxazid is an inhibitor of monoamine oxidase (MAO; IC₅₀ = 4.8 μM for rat brain MAO). It induces a 4-fold increase in tryptamine action in isolated rat fundal strips at a concentration of 50 nM. In vivo, isocarboxazid potentiates tryptamine toxicity (LD₅₀ = 8 mg/kg following subcutaneous administration of 250 mg/kg tryptamine). It inhibits 90% of MAO activity in isolated rat hearts and reduces cardiomegaly induced by isoproterenol (Item No. ) in rats at a dose of 20 mg/kg. Oral administration of isocarboxazid (10 mg/kg) increases levels of dopamine and norepinephrine and reduces levels of the monoamine metabolites DOPAC, homovanillic acid (HVA; Item No. ), and 5-hydroxy indole-3-acetic acid (5-HIAA; Item No. ) by 43, 32, and 28%, respectively, in mouse brain. Formulations containing isocarboxazid have been used for the treatment of minor depression.

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