Drug intelligence / Profile preview

linsidomine

Development stage
Unknown
Modality
Small Molecules
Administration
Intracoronary, Intracavernosal
01

Overview

Linsidomine (3-morpholinosydnonimine, SIN-1) is a small molecule vasodilator and the direct hepatic metabolite of molsidomine. It acts primarily by nonenzymatically releasing nitric oxide (NO) from endothelial cells, which stimulates soluble guanylate cyclase in smooth muscle cells, increasing intracellular cyclic GMP and leading to smooth muscle relaxation. This mechanism underlies its antianginal and vasodilatory effects. Linsidomine also hyperpolarizes cell membranes by influencing the sodium-potassium pump, reducing responsiveness to adrenergic stimulation. Clinically, it has been used for coronary angiography and investigated for erectile dysfunction due to its ability to induce penile erection via NO-mediated pathways. Additionally, linsidomine inhibits platelet aggregation through increased cGMP levels in platelets. However, it is neurotoxic and can promote oxidative stress on neurons as a peroxynitrite-generating compound[1][4][5][7].

Brand names
SIN-1ASIN1ASIN 1A
Other names
3-morpholinosydnonimineSIN-1SIN1SIN 1
02

Targets

sGC (Soluble Guanylyl Cyclase)

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