Journal: Pharmacy and Therapeutics

Article Title: Riociguat (Adempas): a Novel Agent For the Treatment of Pulmonary Arterial Hypertension and Chronic Thromboembolic Pulmonary Hypertension

doi:

Figure Lengend Snippet: Adverse Events Reported in at Least 5% of Riociguat-Treated Patients And at a Frequency Greater Than Placebo in Phase 3 Clinical Trials 24 , 25

Article Snippet: 3 In October 2013, the Food and Drug Administration approved riociguat (Adempas, Bayer Healthcare Pharmaceuticals), the first agent in a novel therapeutic class called soluble guanylate cyclase (sGC) stimulators.

Techniques: Clinical Proteomics, Reflux, Infection

Journal: PLoS ONE

Article Title: Effects of Stimulation of Soluble Guanylate Cyclase on Diabetic Nephropathy in Diabetic eNOS Knockout Mice on Top of Angiotensin II Receptor Blockade

doi: 10.1371/journal.pone.0042623

Figure Lengend Snippet: Experimental progress of blood pressure and blood glucose in diabetic eNOS knockout mice treated with riociguat (3 mg/kg/d), telmisartan (1 mg/kg/d), both (3 mg/kg/d and 1 mg/kg/d) or vehicle.

Article Snippet: Riociguat [BAY 63-2521; Methyl 2-[1-2(-fluorobenzyl)-1 H -pyrazolo[3,4- b ]pyridin-3-yl]-4,6—diaminopyrimidin-5-ylmethylcarbamat] was synthesized by Bayer Pharma AG as described and dissolved in Transcutol®/Cremophor®/water (10/20/70).

Techniques: Knock-Out

Journal: PLoS ONE

Article Title: Effects of Stimulation of Soluble Guanylate Cyclase on Diabetic Nephropathy in Diabetic eNOS Knockout Mice on Top of Angiotensin II Receptor Blockade

doi: 10.1371/journal.pone.0042623

Figure Lengend Snippet: Final urinary albumin as well as organ weights and histology of diabetic mice after 11 weeks of treatment with riociguat (3 mg/kg/d), telmisartan (1 mg/kg/d), riociguat and telmisartan (3 mg/kg/d and 1 mg/kg/d) or vehicle and of non-diabetic control mice, respectively.

Article Snippet: Riociguat [BAY 63-2521; Methyl 2-[1-2(-fluorobenzyl)-1 H -pyrazolo[3,4- b ]pyridin-3-yl]-4,6—diaminopyrimidin-5-ylmethylcarbamat] was synthesized by Bayer Pharma AG as described and dissolved in Transcutol®/Cremophor®/water (10/20/70).

Techniques: Control

Journal: Cardiology Research

Article Title: Pharmacological Alteration of Cellular Mechanical Properties in Pulmonary Arterial Smooth Muscle Cells of Idiopathic Pulmonary Arterial Hypertension

doi: 10.14740/cr1282

Figure Lengend Snippet: Mechanical properties of pulmonary arterial smooth muscle cells (PASCMCs) derived from a patient with idiopathic pulmonary arterial hypertension (PAH-PASMCs) in response to macitentan and riociguat treatment. (a) The apparent Young’s modulus normalized with that of untreated cells, log E 0 /log E c of PAH-PASMCs in response to macitentan treatment. (b) α of macitentan-treated PAH-PASMCs. (c) The log E 1 of macitentan-treated PAH-PASMCs. (d) The log E 0 /log E c of riociguat-treated PAH-PASMCs. (e) α of riociguat-treated PAH-PASMCs. (f) The log E 1 of riociguat-treated PAH-PASMCs. (g) The log E 0 /log E c of PAH-PASMCs with combination treatment. (h) α of PAH-PASMCs with combination treatment. (i) The log E 1 of PAH-PASMCs with combination treatment. *P < 0.05 vs. DMSO-treated PASMCs by ANOVA. **P < 0.05 by Student’s t -test. DMSO: dimethylsulfoxide; ANOVA: analysis of variance.

Article Snippet: PASMCs were treated with three commercially available drugs for PAH: sildenafil, riociguat, and macitentan (all purchased from Cayman Chemical, MI, USA).

Techniques: Derivative Assay

Journal: BioMed Research International

Article Title: Effect of Riociguat and Sildenafil on Right Heart Remodeling and Function in Pressure Overload Induced Model of Pulmonary Arterial Banding

doi: 10.1155/2018/3293584

Figure Lengend Snippet: Effect of sildenafil and riociguat on RV function in pressure overload model . Hemodynamic and MRI assessment on pulmonary artery banding (PAB) mice treated with sildenafil and riociguat. (a) Right ventricular systolic pressure (RVSPsys, mmHg). (b) Systemic blood pressure (SPBsys, mmHg). (c) Ratio of right ventricular (RV) weight to body weight (RV/BW, mg/g). (d) Ratio of RV weight to LV + septum weight (RV/LV + S, mg/mg). (e) Right ventricular end diastolic volume (RVED, μ l). (f) Right ventricular end systolic volume (RVES, μ l). (g) Right ventricular stroke volume ( μ l). (h) Right ventricular ejection fraction (%). Values are means ± SD. ∗ P < 0.05, ∗∗ P < 0.01, ∗∗∗ P < 0.001, ∗∗∗∗ P < 0.0001, and n = 5 mice per group.

Article Snippet: Our group has previously shown the positive effects of both riociguat and sildenafil on reduction of RV pressure and RVH with concomitant augmentation of RV function in SUGEN (SU5416) associated with chronic hypoxia (SUHx) model of PH [ ].

Techniques:

Journal: BioMed Research International

Article Title: Effect of Riociguat and Sildenafil on Right Heart Remodeling and Function in Pressure Overload Induced Model of Pulmonary Arterial Banding

doi: 10.1155/2018/3293584

Figure Lengend Snippet: Effects of sildenafil and riociguat and on RV cardiomyocyte size and collagen content after PAB . (a, b) Representative pictures and quantification of cardiomyocyte cross-sectional area based on a cell plasma membrane staining with wheat germ agglutinin- (WGA-) FITC (mean ± SD, 5 mice per group, P < 0.05). Scale bar 100 μ m. (c, d) Representative images and assessment of RV collagen area (%), representing reduced collagen content in riociguat-treated samples (mean ± SD, 5 mice per group, ∗∗∗ P < 0.001, ∗∗∗∗ P < 0.0001). Scale bar 100 μ m.

Article Snippet: Our group has previously shown the positive effects of both riociguat and sildenafil on reduction of RV pressure and RVH with concomitant augmentation of RV function in SUGEN (SU5416) associated with chronic hypoxia (SUHx) model of PH [ ].

Techniques: Clinical Proteomics, Membrane, Staining

Journal: BioMed Research International

Article Title: Effect of Riociguat and Sildenafil on Right Heart Remodeling and Function in Pressure Overload Induced Model of Pulmonary Arterial Banding

doi: 10.1155/2018/3293584

Figure Lengend Snippet: Effects of sildenafil and riociguat on collagen production and phospho-Smad2/3 expression in TGF-beta stimulated RV cardiac fibroblasts . (a) Effects of the sildenafil and riociguat on collagen secretion in RV cardiac fibroblasts (mean ± SD, n = 6 independent experiments, ∗ P < 0.05, ∗∗∗∗ P < 0.0001). (b) Western Blot images p-SMAD2/SMAD2, p-SMAD3/SMAD3, and Pan-actin from the proteins isolated from RV cardiac fibroblasts. The blot is representative of the three independent runs/experiments.

Article Snippet: Our group has previously shown the positive effects of both riociguat and sildenafil on reduction of RV pressure and RVH with concomitant augmentation of RV function in SUGEN (SU5416) associated with chronic hypoxia (SUHx) model of PH [ ].

Techniques: Expressing, Western Blot, Isolation