It is a metabolite of the antianginal drug molsidomine and acts by releasing NO from the endothelial cells nonenzymatically.

It also hyperpolarizes the cell membrane through influencing the sodium-potassium pump and thereby rendering it less responsive to adrenergic stimulation.

Linsidomine injection at a dose of 1 mg produces usable erection[2] in about 70% of patients and full erection in up to 50% of patients.

[citation needed] Linsidomine is neurotoxic and promotes oxidative stress on neurons.

[3] Linsidomine is a peroxynitrite-generating compound involved in the pathogenesis of neurodegenerative diseases.