Isosorbide mononitrate (ISMN) is a nitric oxide (NO) donor with cardioprotective activity.1,2,3 It induces relaxation of precontracted isolated rat mesenteric artery rings with and without endothelium (EC50s = 87 and 30.1 ?M, respectively).1 ISMN (150 mg/kg) prevents increases in blood pressure and plasma levels of thromboxane A2 (TXA2), as well as reduces platelet aggregation in a rat model of hypertension induced by cyclosporin A when administered prior to CsA.2 However, ISMN exacerbates the CsA-induced cardiac phenotype in rats when administered seven weeks after initial CsA administration. ISMN (200 mg/kg) decreases aortic superoxide production, reduces intima-media thickness of the thoracic aorta, and improves endothelium-dependent vasorelaxation in a rabbit model of cholesterol-enriched diet-induced atherosclerosis.3 It also prolongs survival time of mice in a normobaric hypoxia test.4 Formulations containing ISMN have been used in the treatment of angina in patients with coronary artery disease.
1.Stepanovi?-Petrovi?, R.M., V., S., Tomi?, M.A., et al.Comparison of vasorelaxant effect and tolerance profile of a novel isosorbide-5-mononitrate derivative with its stereoisomer and parent drug on rat mesenteric arteryArznei-forschung60(4)189-197(2010) 2.Reis, F., Ponte, L., Teixeira-Lemos, E., et al.Curative isosorbide-5-mononitrate treatment, in opposition to the beneficial preventive one, aggravates the prothrombotic and proconstrictor state in cyclosporine-induced hypertensive ratsClin. Exp. Pharmacol. Physiol.32(8)640-648(2005) 3.Müller , S., K?nig, I., Meyer, W., et al.Inhibition of vascular oxidative stress in hypercholesterolemia by eccentric isosorbide mononitrateJ. Am. Coll. Cardiol.44(3)624-631(2004) 4.Fan, P.-C., Ma, H.-P., Jiang, W., et al.Anti-hypoxia activity of the novel NO donor acetyl ferulic isosorbide mononitrate in acute high-altitude hypoxia miceBiol. Pharm. Bull.38(9)1280-1289(2015)