产品描述:
Riociguat is a stimulator of soluble guanylate cyclase (sGC).{36864},{26751} It stimulates recombinant sGC in a concentration-dependent manner in vitro by up to 73-fold when used at a concentration of 100 μM or by up to 112-fold when used in combination with the nitric oxide (NO) donor DEA NONOate (Item No. 82100).{36864} It has no effect on phosphodiesterases PDE1-9 and PDE11 when used at concentrations up to 3 μM. Riociguat (1 and 10 mg/kg) reduces pulmonary and systemic arterial pressure in a rabbit model of acute pulmonary arterial hypertension (PAH) induced by U-46619 (Item No. 16450). It also inhibits increases in right ventricular systolic pressure, right heart hypertrophy, and pulmonary artery muscularization in hypoxia-induced mouse and monocrotaline-injected rat models of chronic PAH when administered at a dose of 10 mg/kg. Formulations containing riociguat have been used in the treatment of chronic thromboembolic pulmonary hypertension (CTEPH) and PAH.