Linsidomine Explained

Linsidomine (3-morpholinosydnonimine or SIN-1^[1]) is a vasodilator. 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. Linsidomine does not appear to be associated with priapism.

Linsidomine is neurotoxic and promotes oxidative stress on neurons.^[3] Linsidomine is a peroxynitrite-generating compound involved in the pathogenesis of neurodegenerative diseases.^[4]

Notes and References

1. Wen TC, Rogido MR, Moore JE, Genetta T, Peng H, Sola A . Cardiotrophin-1 protects cortical neuronal cells against free radical-induced injuries in vitro . Neuroscience Letters . 387 . 1 . 38–42 . October 2005 . 16084018 . 10.1016/j.neulet.2005.07.018 .
2. Lemaire A, Buvat J . [Erectile response to intracavernous injection of linsidomine in 38 impotent patients. Comparison with prostaglandin E1] . Progres en Urologie . 8 . 3 . 388–91 . June 1998 . 9689672 .
3. Wallace DR, Dodson S, Nath A, Booze RM . Estrogen attenuates gp120- and tat1-72-induced oxidative stress and prevents loss of dopamine transporter function . Synapse . 59 . 1 . 51–60 . January 2006 . 16237680 . 10.1002/syn.20214 .
4. Jang JH, Aruoma OI, Jen LS, Chung HY, Surh YJ . Ergothioneine rescues PC12 cells from beta-amyloid-induced apoptotic death . Free Radical Biology & Medicine . 36 . 3 . 288–99 . February 2004 . 15036348 . 10.1016/j.freeradbiomed.2003.11.005 .